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Journal articles on the topic 'Relative insulin potency'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Bindu, Rama Bhat, Girish, and Krishna Prasad. "RELATIVE POTENCY OF ANTI-DIABETIC COSTUS SPECIOSUSPLANT EXTRACT IN MOUSE FIBROBLAST CELL LINE." International Journal of Research -GRANTHAALAYAH 4, no. 3 (2016): 99–107. http://dx.doi.org/10.29121/granthaalayah.v4.i3.2016.2790.

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Plant-derived compounds have been used clinically to treat type 2 diabetes for many years as they also exert additional beneficial effects on various other disorders. PI3K pathway is the major pathway activated by insulin receptor (IR). It induces glucose uptake, glycogen synthesis, protein synthesis, cell growth and differentiation. Hence metabolic assay was employed to assess glucose uptake based on the property of 3T3-L 1 cells to differentiate into adipocytes which can take up the glucose in medium due to the effect of insulin or insulin like molecules. The results of the current study sho

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2

C, Bindu, Rama Bhat P., Krishna Prasad G., and C. Girish B. "RELATIVE POTENCY OF ANTIDIABETIC EFFECT OF COSTUS SPECIOSUS (KOEN. EX RETZ.) SMITH PLANT EXTRACT IN MOUSE FIBROBLAST CELL LINE." International Journal of Research – Granthaalayah 4, no. 3 (2017): 99–106. https://doi.org/10.5281/zenodo.847009.

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Plant-derived compounds have been used clinically to treat type 2 diabetes for many years as they also exert additional beneficial effects on various other disorders. PI3K pathway is the major pathway activated by insulin receptor (IR). It induces glucose uptake, glycogen synthesis, protein synthesis, cell growth and differentiation. Hence metabolic assay was employed to assess glucose uptake based on the property of 3T3-L1 cells to differentiate into adipocytes which can take up the glucose in medium due to the effect of insulin or insulin like molecules. The results of the current research s

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3

Bajaj, M., T. L. Blundell, R. Horuk, et al. "Coypu insulin. Primary structure, conformation and biological properties of a hystricomorph rodent insulin." Biochemical Journal 238, no. 2 (1986): 345–51. http://dx.doi.org/10.1042/bj2380345.

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Insulin from a hystricomorph rodent, coypu (Myocaster coypus), was isolated and purified to near homogeneity. Like the other insulins that have been characterized in this Suborder of Rodentia, coypu insulin also exhibits a very low (3%) biological potency, relative to pig insulin, on lipogenesis in isolated rat fat-cells. The receptor-binding affinity is significantly higher (5-8%) in rat fat-cells, in rat liver plasma membranes and in pig liver cells, indicating that the efficacy of coypu insulin on receptors is about 2-fold lower than that of pig insulin. The primary structures of the oxidiz

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4

Chrudinová, Martina, Lenka Žáková, Aleš Marek, et al. "A versatile insulin analog with high potency for both insulin and insulin-like growth factor 1 receptors: Structural implications for receptor binding." Journal of Biological Chemistry 293, no. 43 (2018): 16818–29. http://dx.doi.org/10.1074/jbc.ra118.004852.

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Insulin and insulin-like growth factor 1 (IGF-1) are closely related hormones involved in the regulation of metabolism and growth. They elicit their functions through activation of tyrosine kinase–type receptors: insulin receptors (IR-A and IR-B) and IGF-1 receptor (IGF-1R). Despite similarity in primary and three-dimensional structures, insulin and IGF-1 bind the noncognate receptor with substantially reduced affinity. We prepared [d-HisB24, GlyB31, TyrB32]-insulin, which binds all three receptors with high affinity (251 or 338% binding affinity to IR-A respectively to IR-B relative to insuli

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Richardson, S. B., T. Laya, and M. VanOoy. "Similarities between hamster pancreatic islet beta (HIT) cell vasopressin receptors and V1b receptors." Journal of Endocrinology 147, no. 1 (1995): 59–65. http://dx.doi.org/10.1677/joe.0.1470059.

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Abstract Vasopressin (VP) elicits almost identical insulin-stimulatory dose responses in isolated mouse islets and hamster β (HIT) cells. We have further pharmacologically characterized HIT cell VP receptors by comparing the potencies of a series of VP agonists including the novel V1b agonist, desamino(d-3-(3′-pyridyl)-Ala2,Arg8)VP (d(d-3-Pal)VP), in stimulating insulin secretion and inositol phosphate (IP) production. The relative orders of potency of VP analogues were parallel in both respects: desamino-Arg-VP (dAVP)>Arg-vasotocin (AVT)= VP>oxytocin (OXY)>desamino-d-Arg-VP (ddAVP)&g

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Molano, Ruth Damaris, Antonello Pileggi, Hubert M. Tse, Cherie L. Stabler, and Christopher A. Fraker. "A static glucose-stimulated insulin secretion (sGSIS) assay that is significantly predictive of time to diabetes reversal in the human islet bioassay." BMJ Open Diabetes Research & Care 12, no. 2 (2024): e003897. http://dx.doi.org/10.1136/bmjdrc-2023-003897.

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IntroductionStatic incubation (static glucose-stimulated insulin secretion, sGSIS) is a measure of islet secretory function. The Stimulation Index (SI; insulin produced in high glucose/insulin produced in low glucose) is currently used as a product release criterion of islet transplant potency.Research design and methodsOur hypothesis was that the Delta, insulin secreted in high glucose minus insulin secreted in low glucose, would be more predictive. To evaluate this hypothesis, sGSIS was performed on 32 consecutive human islet preparations, immobilizing the islets in a slurry of Sepharose bea

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Vienberg, Sara G., Stephan D. Bouman, Heidi Sørensen, et al. "Receptor-isoform-selective insulin analogues give tissue-preferential effects." Biochemical Journal 440, no. 3 (2011): 301–8. http://dx.doi.org/10.1042/bj20110880.

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The relative expression patterns of the two IR (insulin receptor) isoforms, +/− exon 11 (IR-B/IR-A respectively), are tissue-dependent. Therefore we have developed insulin analogues with different binding affinities for the two isoforms to test whether tissue-preferential biological effects can be attained. In rats and mice, IR-B is the most prominent isoform in the liver (>95%) and fat (>90%), whereas in muscles IR-A is the dominant isoform (>95%). As a consequence, the insulin analogue INS-A, which has a higher relative affinity for human IR-A, had a higher relative potency [compare

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8

Shibasaki, Y., H. Sakura, M. Odawara, et al. "Glucocorticoids increase insulin binding and the amount of insulin-receptor mRNA in human cultured lymphocytes." Biochemical Journal 249, no. 3 (1988): 715–19. http://dx.doi.org/10.1042/bj2490715.

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The effect of steroid hormones on insulin binding and the amount of insulin-receptor mRNA was examined in IM-9 lymphocytes. Cortisol and cortexolone, but not oestrogen, increased both the binding of insulin and the amount of insulin-receptor mRNA in a time- and dose-dependent manner. Cortisol was most potent, and induced a 2-fold increase in insulin binding and a 4-fold increase in mRNA. The elevation in binding was due to an increased number of insulin receptors at the cell surface. The increase in mRNA involved all four of the insulin-receptor mRNAs and could not be inhibited by cycloheximid

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9

Tang, J., W. Pugh, K. S. Polonsky, and H. Zhang. "Preservation of insulin secretory responses to P2 purinoceptor agonists in Zucker diabetic fatty rats." American Journal of Physiology-Endocrinology and Metabolism 270, no. 3 (1996): E504—E512. http://dx.doi.org/10.1152/ajpendo.1996.270.3.e504.

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The role of P2 purinoceptor agonists in regulatory insulin secretion in Zucker diabetic fatty (ZDF) rats was studied using the isolated perfused pancreas and intracellular Ca2+ concentration ([Ca2+]i) microfluorimetry. The relative potency of different purinoceptor agonists to stimulate the insulin secretory process was consistent with the conclusion that responses in [Ca2+]i and insulin secretion are mediated by the P2y subtype of purinoceptors. Additional studies using specific antagonists of the Ca2+ signaling pathway indicated that activation of P2y purinoceptor releases Ca2+ from intracel

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10

Jonas, H. A., and A. J. Cox. "Insulin-like growth factor binding to the atypical insulin receptors of a human lymphoid-derived cell line (IM-9)." Biochemical Journal 266, no. 3 (1990): 737–42. http://dx.doi.org/10.1042/bj2660737.

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The cells of the IM-9 human lymphocyte-derived line contain a sub-population of insulin-binding sites whose immunological and hormone-binding characteristics closely resemble those of the atypical insulin-binding sites of human placenta. These binding sites, which have moderately high affinity for multiplication-stimulating activity [MSA, the rat homologue of insulin-like growth factor (IGF) II] and IGF-I, are identified on IM-9 cells by 125I-MSA binding. They account for approximately 30% of the total insulin-receptor population, and do not react with a monoclonal antibody to the type I IGF r

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11

Ahrén, Bo, Per Sauerberg, and Christian Thomsen. "Increased insulin secretion and normalization of glucose tolerance by cholinergic agonism in high fat-fed mice." American Journal of Physiology-Endocrinology and Metabolism 277, no. 1 (1999): E93—E102. http://dx.doi.org/10.1152/ajpendo.1999.277.1.e93.

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Increased insulinotropic activity by the cholinergic agonist carbachol exists in insulin-resistant high fat-fed C57BL/6J mice. We examined the efficiency and potency of carbachol to potentiate glucose-stimulated insulin secretion and to improve glucose tolerance in these animals. Intravenous administration of carbachol (at 15 and 50 nmol/kg) markedly potentiated glucose (1 g/kg)-stimulated insulin secretion in mice fed both a control and a high-fat diet (for 12 wk), with a higher relative potentiation in high fat-fed mice measured as increased (1–5 min) acute insulin response and area under th

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12

Nielsen, Emilie Prang, Søren Andersen, Christian Lehn Brand, and Susanne Ditlevsen. "Applying historical data in a nonlinear mixed-effects model can reduce the number of control rats required for calculation of the relative potency of insulin analogues." PLOS ONE 17, no. 6 (2022): e0257750. http://dx.doi.org/10.1371/journal.pone.0257750.

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This paper examines how to reduce the number of control animals in preclinical hyperinsulemic glucose clamp studies if we make use of information on historical studies. A dataset consisting of 59 studies in rats to investigate new insulin analogues for diabetics, collected in the years 2000 to 2015, is analysed. A simulation experiment is performed based on a carefully built nonlinear mixed-effects model including historical information, comparing results (for the relative log-potency) with the standard approach ignoring previous studies. We find that by including historical information in the

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13

Tomas, FM, PE Walton, FR Dunshea, and FJ Ballard. "IGF-I variants which bind poorly to IGF-binding proteins show more potent and prolonged hypoglycaemic action than native IGF-I in pigs and marmoset monkeys." Journal of Endocrinology 155, no. 2 (1997): 377–86. http://dx.doi.org/10.1677/joe.0.1550377.

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The relative acute hypoglycaemic potencies of IGF-I and several variants of IGF-I which bind poorly to the IGF-I binding proteins (IGFBPs) have been examined in marmosets (Callithrix jacchus) and the pig. In the marmoset study, IGF-I and des(1-3)IGF-I were compared in anaesthetised and conscious animals in a range of bolus doses from 42 to 270 micrograms/kg body weight. In the pig study, IGF-I was compared with four variants, des(1-3)IGF-I long-IGF-I, R3IGF-I and long-R3IGF-I (LR3IGF-I), which show reduced affinity for the IGFBPs as well as with insulin. Doses in the pig were 20 and 50 microgr

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14

ROSENBERG, MIRIAM, JAMES MAZELLA, and LINDA TSENG. "Relative Potency of Relaxin, Insulin-like Growth Factors, and Insulin on the Prolactin Production in Progestin-primed Human Endometrial Stromal Cells in Long-term Culture." Annals of the New York Academy of Sciences 622, no. 1 The Primate E (1991): 138–44. http://dx.doi.org/10.1111/j.1749-6632.1991.tb37857.x.

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15

Sebokova, Elena, Andreas D. Christ, Haiyan Wang, et al. "Taspoglutide, an Analog of Human Glucagon-Like Peptide-1 with Enhanced Stability and in Vivo Potency." Endocrinology 151, no. 6 (2010): 2474–82. http://dx.doi.org/10.1210/en.2009-1459.

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Taspoglutide is a novel analog of human glucagon-like peptide-1 [hGLP-1(7-36)NH2] in clinical development for the treatment of type 2 diabetes. Taspoglutide contains α-aminoisobutyric acid substitutions replacing Ala8 and Gly35 of hGLP-1(7-36)NH2. The binding affinity [radioligand binding assay using [125I]hGLP-1(7-36)NH2], potency (cAMP production in CHO cells stably overexpressing hGLP-1 receptor), and in vitro plasma stability of taspoglutide compared with hGLP-1(7-36)NH2 have been evaluated. Effects on basal and glucose-stimulated insulin secretion were determined in vitro in INS-1E cells

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16

Ezzat, Shahira, Mahitab Bishbishy, Solomon Habtemariam, et al. "Looking at Marine-Derived Bioactive Molecules as Upcoming Anti-Diabetic Agents: A Special Emphasis on PTP1B Inhibitors." Molecules 23, no. 12 (2018): 3334. http://dx.doi.org/10.3390/molecules23123334.

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Diabetes mellitus (DM) is a chronic metabolic disease with high morbimortality rates. DM has two types: type 1, which is often associated with a total destruction of pancreatic beta cells, and non-insulin-dependent or type 2 diabetes mellitus (T2DM), more closely associated with obesity and old age. The main causes of T2DM are insulin resistance and/or inadequate insulin secretion. Protein-tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling pathways and plays an important role in T2DM, as its overexpression may induce insulin resistance. Thus, since PTP1B may be a therapeuti

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17

Francis, G. L., M. Ross, F. J. Ballard, et al. "Novel recombinant fusion protein analogues of insulin-like growth factor (IGF)-I indicate the relative importance of IGF-binding protein and receptor binding for enhanced biological potency." Journal of Molecular Endocrinology 8, no. 3 (1992): 213–23. http://dx.doi.org/10.1677/jme.0.0080213.

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ABSTRACT An efficient expression system in Escherichia coli for several biologically active insulin-like growth factor-I (IGF-I) fusion peptide analogues is described. These novel IGF-I fusion protein analogues have properties that make them very useful reagents in the investigation of IGF-I action. The analogues comprise an IGF-I sequence and the first 11 amino acids of methionyl porcine growth hormone (pGH) and include [Met1]-pGH(1–11)-Val-Asn-IGF-I, which contains the authentic IGF-I sequence, and two analogues, [Met1]-pGH(1–11)-Val-Asn-[Gly3]-IGF-I and [Met1]-pGH(1–11)-Val-Asn-[Arg3]-IGF-I

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18

Francis, G. L., S. E. Aplin, S. J. Milner, K. A. McNeil, F. J. Ballard, and J. C. Wallace. "Insulin-like growth factor (IGF)-II binding to IGF-binding proteins and IGF receptors is modified by deletion of the N-terminal hexapeptide or substitution of arginine for glutamate-6 in IGF-II." Biochemical Journal 293, no. 3 (1993): 713–19. http://dx.doi.org/10.1042/bj2930713.

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Recombinant insulin-like growth factor-II (IGF-II) and two structural analogues, des(1-6)IGF-II and [Arg6]-IGF-II, were produced to investigate the role of N-terminal residues in binding to IGF-binding proteins (IGFBPs) and hence the biological properties of the modified peptides. The growth factors were modelled on two previously characterized variants of IGF-I, des(1-3)IGF-I and [Arg3]-IGF-I, which both show substantially decreased binding to IGFBPs and were expressed as fusion proteins in Escherichia coli. The biological activities of the corresponding analogues of IGF-I and IGF-II were com

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Gillespie, C., L. C. Read, C. J. Bagley, and F. J. Ballard. "Enhanced potency of truncated insulin-like growth factor-I (des(1–3)IGF-I) relative to IGF-I in lit/lit mice." Journal of Endocrinology 127, no. 3 (1990): 401–5. http://dx.doi.org/10.1677/joe.0.1270401.

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ABSTRACT The relative potencies of insulin-like growth factor (IGF-I) and the N-terminal truncated derivative, des(1–3)IGF-I, have been compared in lit/lit mice. Injection of 30 μg IGF-I, 30 μg des(1–3)IGF-I or 3 μg des(1–3)IGF-I daily for 3 weeks increased total length and nose-rump length of the animals substantially more than in controls or animals treated with 3 μg IGF-I daily. Body weight changes were not statistically significant. The lower dose of des(1–3)IGF-I, but not that of IGF-I, led to increases in kidney and heart weights relative to controls, while the higher dose of either IGF-

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20

Wang, Chen-Dong, Bao-Song Teng, Yan-Ming He, et al. "Effect of a novel proteoglycan PTP1B inhibitor from Ganoderma lucidum on the amelioration of hyperglycaemia and dyslipidaemia in db/db mice." British Journal of Nutrition 108, no. 11 (2012): 2014–25. http://dx.doi.org/10.1017/s0007114512000153.

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Protein tyrosine phosphatase 1B (PTP1B) is implicated in the negative regulation of the insulin signalling pathway by dephosphorylating the insulin receptor (IR) and IR substrates. Ganodermalucidum has traditionally been used for the treatment of diabetes in Chinese medicine; however, its anti-diabetic potency and mechanism in vivo is still unclear. Our previously published study reported a novel proteoglycan PTP1B inhibitor, named Fudan-Yueyang-Ganoderma lucidum (FYGL) from G. lucidum, with a half-maximal inhibitory concentration (IC50) value of 5·12 (sem 0·05) μg/ml, a protein:polyglycan rat

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21

Francis, G. L., F. M. Upton, F. J. Ballard, K. A. McNeil, and J. C. Wallace. "Insulin-like growth factors 1 and 2 in bovine colostrum. Sequences and biological activities compared with those of a potent truncated form." Biochemical Journal 251, no. 1 (1988): 95–103. http://dx.doi.org/10.1042/bj2510095.

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1. Insulin-like growth factors 1 and 2 (IGF-1 and IGF-2) together with a truncated form of IGF-1 were purified to homogeneity from bovine colostrum. 2. Two forms of IGF-1 were totally resolved from IGF-2 in the purification by h.p.l.c. involving cation-exchange and reverse-phase columns. 3. The complete amino acid sequences for all three forms of IGF were determined. The sequence of bovine IGF-1 was found to be identical with that of human IGF-1, and that of the variant lacked the N-terminal tripeptide Gly-Pro-Glu (-3N:IGF-1). Bovine IGF-2 was found to differ in three residues of the C-domain

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Naylor, Jacqueline, Arthur T. Suckow, Asha Seth та ін. "Use of CRISPR/Cas9-engineered INS-1 pancreatic β cells to define the pharmacology of dual GIPR/GLP-1R agonists". Biochemical Journal 473, № 18 (2016): 2881–91. http://dx.doi.org/10.1042/bcj20160476.

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Dual-agonist molecules combining glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) activity represent an exciting therapeutic strategy for diabetes treatment. Although challenging due to shared downstream signalling pathways, determining the relative activity of dual agonists at each receptor is essential when developing potential novel therapeutics. The challenge is exacerbated in physiologically relevant cell systems expressing both receptors. To this end, either GIP receptors (GIPR) or GLP-1 receptors (GLP-1R) were ablated via RNA-guided clustered regula

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Sharma, Rajni, Manju Kumari, Suman Mishra, et al. "Exosomes Secreted by Umbilical Cord Blood-Derived Mesenchymal Stem Cell Attenuate Diabetes in Mice." Journal of Diabetes Research 2021 (December 10, 2021): 1–15. http://dx.doi.org/10.1155/2021/9534574.

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Mesenchymal stem cell (MSC) therapy is an innovative approach in diabetes due to its capacity to modulate tissue microenvironment and regeneration of glucose-responsive insulin-producing cells. In this study, we investigated the role of MSC-derived exosomes in pancreatic regeneration and insulin secretion in mice with streptozotocin-induced diabetes. Mesenchymal stem cells (MSCs) were isolated and characterized from umbilical cord blood (UCB). Exosomes were isolated and characterized from these MSCs. Diabetes was induced in male C57Bl/6 mice by streptozotocin (STZ; 40 mg/kg body weight, i.p.)

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Phillips, Susan A., Jacqueline Kung, Theodore P. Ciaraldi, et al. "Selective regulation of cellular and secreted multimeric adiponectin by antidiabetic therapies in humans." American Journal of Physiology-Endocrinology and Metabolism 297, no. 3 (2009): E767—E773. http://dx.doi.org/10.1152/ajpendo.00378.2009.

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Adiponectin, an insulin-sensitizing factor secreted from adipose tissue, is decreased in individuals with type 2 diabetes (T2D) and increased in response to thiazolidinedione (TZD) therapy. Changes in its secretion and assembly into higher-order forms affect insulin sensitivity. To determine the relative potency of TZDs on intra-adipocyte multimerization and secretion of adiponectin, we assessed the impact of in vivo low- or high-dose rosiglitazone treatment alone or combined with metformin in subjects with T2D. T2D subjects received high-dose rosiglitazone (8 mg/day), high-dose metformin (2,0

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Haugaard-Jönsson, Linda M., Mohammed Akhter Hossain, Norelle L. Daly, David J. Craik, John D. Wade, and K. Johan Rosengren. "Structure of human insulin-like peptide 5 and characterization of conserved hydrogen bonds and electrostatic interactions within the relaxin framework." Biochemical Journal 419, no. 3 (2009): 619–27. http://dx.doi.org/10.1042/bj20082353.

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INSL5 (insulin-like peptide 5) is a two-chain peptide hormone related to insulin and relaxin. It was recently discovered through searches of expressed sequence tag databases and, although the full biological significance of INSL5 is still being elucidated, high expression in peripheral tissues such as the colon, as well as in the brain and hypothalamus, suggests roles in gut contractility and neuroendocrine signalling. INSL5 activates the relaxin family peptide receptor 4 with high potency and appears to be the endogenous ligand for this receptor, on the basis of overlapping expression profile

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Totomirova, Tzvetelina, and Mila Arnaudova. "HbA1c Is Not Potent Glucose Control Assessment Tool in Type 2 Diabetes Patients Treated With Insulin." Journal of the Endocrine Society 5, Supplement_1 (2021): A470. http://dx.doi.org/10.1210/jendso/bvab048.960.

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Abstract Glycated haemoglobin (HbA1c) is used for defining of glucose control in diabetic patients nevertheless its insufficiency to present overall control in some specific cases. Continuous Glucose Monitoring (CGM) is usually used for adjustment of insulin doses but the derived data are helpful for exact glucose control. We assess the potency of HbAc for defining of real glucose control in subgroup of type 2 diabetes patients treated with different insulin regimens. We studied 54 diabetic patients (33 men, 21 women; age 60.23±5.99 years, disease duration 12.64±5.02 years) - 33 with type 2 di

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PURUP, STIG, SØREN KROGH JENSEN, and KRIS SEJRSEN. "Differential effects of retinoids on proliferation of bovine mammary epithelial cells in collagen gel culture." Journal of Dairy Research 68, no. 2 (2001): 157–64. http://dx.doi.org/10.1017/s0022029901004782.

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The effects of increasing concentrations of retinol, retinal and retinoic acid on proliferation of bovine mammary epithelial cells were investigated in collagen gel cultures. All retinoids significantly inhibited proliferation of mammary epithelial cells. The relative inhibitory potency of the retinoids was: retinoic acid > retinal > retinol. Maximal inhibition at 10 μg/ml corresponded to a 75–95% inhibition of proliferation obtained in basal medium. Retinol, retinal and retinoic acid also inhibited proliferation of cells growth-stimulated with insulin-like growth factor-I (IGF-I). Retin

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Goyal, Rahul, S. Nagtilak, Vijay Thawani, and Shavetika Jindal. "Effect of natural polyphenols on diabetes mellitus (type-2) with myocardial infarction: a double-blind placebo controlled trial." International Journal of Advances in Medicine 6, no. 2 (2019): 351. http://dx.doi.org/10.18203/2349-3933.ijam20191140.

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Background: Diabetes Mellitus Type-2(T2D); is a leading disease in world wide. T2D is a clinical syndrome characterized by hyperglycaemia. Hyperglycemias are caused by an absolute or relative deficiency of insulin and due to insulin resistance. Diabetic patients are highly prone to Reactive Oxygen Species (ROS) and leads to Cardio vascular complications. Several medicines have been recommended to cure T2D; and still discovery of newer drugs are in process. Now a day, the focus of researches in diabetes includes discovery of newer anti-diabetic agents as well as isolating the active compounds f

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Waurich, R., J. Ringleb, B. C. Braun, and K. Jewgenow. "Embryonic gene activation in in vitro produced embryos of the domestic cat (Felis catus)." REPRODUCTION 140, no. 4 (2010): 531–40. http://dx.doi.org/10.1530/rep-10-0298.

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Accurate embryonic gene activation (EGA) is essential for the embryo's developmental potency and reflects the quality ofin vitroproduced embryos. To describe the dynamic and temporal patterns of EGA in the cat, the mRNA expression of developmentally important genes (DNA methyltransferases 1 and 3A,DNMT1andDNMT3A; gap junction protein α 1,GJA1; transcription factor octamer 4,POU5F1(OCT4); insulin-like growth factor (IGF) 1 and 2 receptors,IGF1RandIGF2R) was examined by RT-PCR techniques in preimplantation embryos obtained afterin vitromaturation and IVF. Furthermore, influences of ICSI and sper

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Seferovic, Maxim D., Rashad Ali, Hiroyasu Kamei, et al. "Hypoxia and Leucine Deprivation Induce Human Insulin-Like Growth Factor Binding Protein-1 Hyperphosphorylation and Increase Its Biological Activity." Endocrinology 150, no. 1 (2008): 220–31. http://dx.doi.org/10.1210/en.2008-0657.

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Fetal growth restriction is often caused by uteroplacental insufficiency that leads to fetal hypoxia and nutrient deprivation. Elevated IGF binding protein (IGFBP)-1 expression associated with fetal growth restriction has been documented. In this study we tested the hypothesis that hypoxia and nutrient deprivation induce IGFBP-1 phosphorylation and increase its biological potency in inhibiting IGF actions. HepG2 cells were subjected to hypoxia and leucine deprivation to mimic the deprivation of metabolic substrates. The total IGFBP-1 levels measured by ELISA were approximately 2- to 2.5-fold h

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Gray, Leon Earl, Christy S. Lambright, Justin M. Conley, et al. "Genomic and Hormonal Biomarkers of Phthalate-Induced Male Rat Reproductive Developmental Toxicity Part II: A Targeted RT-qPCR Array Approach That Defines a Unique Adverse Outcome Pathway." Toxicological Sciences 182, no. 2 (2021): 195–214. http://dx.doi.org/10.1093/toxsci/kfab053.

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Abstract Previously, we demonstrated that exposure to some diortho-phthalate esters during sexual differentiation disrupts male reproductive development by reducing fetal rat testis testosterone production (T Prod) and gene expression in a dose-related manner. The objectives of the current project were to expand the number of test compounds that might reduce fetal T Prod, including phthalates, phthalate alternatives, pesticides, and drugs, and to compare reductions in T Prod with altered testis mRNA expression. We found that PEs that disrupt T Prod also reduced expression of a unique “cluster”

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Barnard, R., S. W. Rowlinson, and M. J. Waters. "Soluble forms of the rabbit adipose tissue and liver growth hormone receptors are antigenically identical, but the integral membrane forms differ." Biochemical Journal 267, no. 2 (1990): 471–77. http://dx.doi.org/10.1042/bj2670471.

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Cytosolic, detergent-solubilized and membrane-bound growth hormone (GH) receptors from rabbit adipose tissue and liver were tested for reactivity with a panel of monoclonal antibodies (MAbs). The cytosolic and detergent-solubilized forms of adipose tissue and liver GH receptors were identically reactive with four precipitating and two hormone-binding-site-directed MAbs. However, the membrane-bound form of the adipose receptor was 1000-fold less reactive with one binding-site-directed MAb (MAb 7) than the membrane-bound liver GH receptor. Reactivity with another inhibitory MAb (MAb 263) was ide

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Dayyani, F., N. Parikh, J. H. Song, et al. "Effect of dual inhibition of the Src and insulin-like growth factor-1 receptor (IGF-1R) pathways on antitumor effects in prostate cancer (PCa)." Journal of Clinical Oncology 29, no. 7_suppl (2011): 21. http://dx.doi.org/10.1200/jco.2011.29.7_suppl.21.

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21 Background: The Src and IGF-1R axes are aberrantly activated in both PCa and the microenvironment of bone metastases. Dasatinib and BMS-754807 are clinically promising small molecule inhibitors with high potency against Src family kinases and IGF-1R, respectively. The aim of this study was to establish antitumor co-operativity by combining IGF-1R and Src blockade in a preclinical PCa model. Methods: LNCaP and PC3 cells were used as models for androgen-dependent and independent PCa, respectively. Inhibition of Src and IGF-1R pathways was accomplished by pharmacologic agents (dasatinib agains

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Galanopoulou, A. S., N. G. Seidah, and Y. C. Patel. "Heterologous processing of rat prosomatostatin to somatostatin-14 by PC2: requirement for secretory cell but not the secretion granule." Biochemical Journal 311, no. 1 (1995): 111–18. http://dx.doi.org/10.1042/bj3110111.

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The role of PC2 in prosomatostatin (PSS) processing was investigated in GH3/GH4C1 pituitary cells. These cells are sparsely granulated, express different amounts of PC2 and no PC1. We described heterologous processing of rat PSS (rPSS) co-expressed with PC2 in stably transfected cells, correlate PC2 protein levels under different conditions of transfection with efficiency of PSS processing to somatostatin-14 (SS-14), determine the effect of modulating cell granularity on enzyme expression and PSS processing, and compare the relative potency of PC2 with that of PC1, PSS and cleavage products we

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Ferone, Diego, Marica Arvigo, Claudia Semino, et al. "Somatostatin and dopamine receptor expression in lung carcinoma cells and effects of chimeric somatostatin-dopamine molecules on cell proliferation." American Journal of Physiology-Endocrinology and Metabolism 289, no. 6 (2005): E1044—E1050. http://dx.doi.org/10.1152/ajpendo.00209.2005.

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To study somatostatin/dopamine (SS/D) synergy in a human cell system constitutively expressing SS and D receptors (SSR and DR, respectively), we characterized the expression of SSR and DR subtypes in the non-small-cell lung cancer line Calu-6, and then we evaluated the effect on cell proliferation of SS/D chimeric molecules (BIM-23A387 and BIM-23A370), which bind with high affinity both sst2 and D2R, and compared the results with those obtained by using SS-14 and subtype-selective SS analogs (SSA) and D agonists (DA). Because Calu-6 cells produce insulin-like growth factor (IGF) and IGF-bindin

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Le Meuth, V., N. Farjaudon, W. Bawab, et al. "Characterization of binding sites for VIP-related peptides and activation of adenylate cyclase in developing pancreas." American Journal of Physiology-Gastrointestinal and Liver Physiology 260, no. 2 (1991): G265—G274. http://dx.doi.org/10.1152/ajpgi.1991.260.2.g265.

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HPLC-purified 125I-labeled vasoactive intestinal peptide (VIP) bound in a specific, saturable, and reversible manner to pancreatic plasma membranes isolated from newborn calves, from milk-fed calves at 28 and 119 days, and from weaned calves at 119 days. A series of VIP analogues, including pituitary adenylate cyclase-activating polypeptide (PACAP), displaced 125I-VIP binding and activated adenylate cyclase in the same order of relative potency: PACAP-38 greater than helodermin greater than VIP, PACAP-27 greater than PHM (human peptide with NH2-terminal histidine and COOH-terminal methionine a

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Hoberman, Matt, Danh Dinh Truong, Roberto Cardenas Zuniga, and Joseph A. Ludwig. "Abstract 2929: LX-101, a novel, clinical stage, payload-bearing targeted therapy directed to the insulin-like growth factor receptor (IGF-1R), demonstrates potent anti-tumor activity in Ewing sarcoma animal models and desmoplastic small round cell tumor." Cancer Research 85, no. 8_Supplement_1 (2025): 2929. https://doi.org/10.1158/1538-7445.am2025-2929.

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Abstract Objective: Multiple aggressive cancers of unmet need have alterations involving the insulin-like growth factor 1 receptor (IGF-1R) pathway, including gene fusions and/or high IGF-1R expression, that correlate with poor outcomes. In Ewing sarcoma (ES) and desmoplastic small round cell tumor (DSRCT), the gene fusion-produced oncogenic proteins upregulate the IGF signaling pathway. Although prior attempts at inhibiting IGF-1R with non-payload bearing naked monoclonal antibodies or small molecules produced some tumor responses, none of these agents were ultimately approved, potentially du

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Fottner, C., D. Engelhardt, and MM Weber. "Regulation of steroidogenesis by insulin-like growth factors (IGFs) in adult human adrenocortical cells: IGF-I and, more potently, IGF-II preferentially enhance androgen biosynthesis through interaction with the IGF-I receptor and IGF-binding proteins." Journal of Endocrinology 158, no. 3 (1998): 409–17. http://dx.doi.org/10.1677/joe.0.1580409.

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Although the effect of insulin-like growth factors (IGFs) in fetal adrenocortical cells has been investigated extensively, the role of the IGF system in the adult human adrenal gland remains unclear. In the present study we investigated the effect of recombinant human IGF-I and IGF-II on cortisol, dehydroepiandrosterone sulfate (DHEA-S) and cAMP synthesis in adult human adrenocortical cells in primary culture. Both IGFs stimulate basal as well as adrenocorticotropin (ACTH)-induced steroid secretion in a time- and dose-dependent fashion. While both IGFs (6.5 nM) induced only a moderate 2-fold i

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Koncar, Robert, Mingzong Li, Jingyan Gao та ін. "Abstract P4-12-18: Discovery and characterization of ETX-636, a potential best-in-class, oral, small molecule, pan-mutant-selective PI3Kα inhibitor". Clinical Cancer Research 31, № 12_Supplement (2025): P4–12–18—P4–12–18. https://doi.org/10.1158/1557-3265.sabcs24-p4-12-18.

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Abstract PIK3CA, which encodes p110α, the catalytic subunit of phosphatidylinositol 3-kinase alpha (PI3Kα), is one of the most frequently mutated oncogenes, with activating mutations seen in ∼16% of all solid tumors and up to 40% of breast tumors, including hormone receptor-positive/HER2-negative, advanced breast cancer. The most frequent gain-of-function PI3Kα hotspot mutations, H1047R, E542K, and E545K, are well-recognized oncogenic drivers. Cancer cells with PIK3CA activating mutations are dependent on PI3Kα signaling and HR-positive, HER2-negative breast cancer patients with PIK3CA mutatio

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Bendapudi, Pavan K., Roelof H. Bekendam, Lin Lin, Mingdong Huang, Bruce Furie, and Robert Flaumenhaft. "ML359, a Small Molecule Inhibitor of Protein Disulfide Isomerase That Prevents Thrombus Formation and Inhibits Oxidoreductase but Not Transnitrosylase Activity." Blood 124, no. 21 (2014): 2880. http://dx.doi.org/10.1182/blood.v124.21.2880.2880.

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Abstract Vascular thiol isomerases comprise a family of enzymes including protein disulfide isomerase (PDI), ERp5, and ERp57 that are important in the process of thrombus formation. PDI is secreted at sites of vascular injury, and antibody-mediated PDI inhibition prevents thrombus formation in a mouse laser injury model. Our group has previously reported on the discovery of the small molecule PDI inhibitors quercetin-3-rutinoside and ML359. Identified as part of a high-throughput screen, ML359 is a second-generation PDI inhibitor that selectively blocks PDI oxidoreductase activity with approxi

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Lindgren, Björn F., Monica Isaksson, Ingrid Stern, and Kerstin Hall. "Insulin-like growth factor binding protein-1 from Hep G2 cells is potently inhibited by the truncated IGF-I analogue des-(1-3) IGF-I." Acta Endocrinologica 128, no. 1 (1993): 81–87. http://dx.doi.org/10.1530/acta.0.1280081.

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Des-(1-3) insulin-like growth factor-I (IGF-I) is an IGF analogue lacking aminoacid 1 to 3 which displays reduced binding to insulin-like growth factor binding protein-1 (IGFBP-1). A greater inhibition of immunoreactive IGFBP-1 was obtained with des-(1-3) IGF-I (10 ng/ml) in Hep G2 medium when incubated in Eagle's Modified Essential Medium (EMEM) without phenolred compared to EMEM with phenolred; EMEM without phenolred was chosen for further experiments. Des-(1-3)IGF-I decreases dose dependently the concentration of IGFBP-1, with a maximal effect at 3–10 μg/l when incubated for 24 h; 10 μg/l o

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Okawa, Yutaka, Teru Hideshima, Paul Steed, et al. "SNX-2112, a selective Hsp90 inhibitor, potently inhibits tumor cell growth, angiogenesis, and osteoclastogenesis in multiple myeloma and other hematologic tumors by abrogating signaling via Akt and ERK." Blood 113, no. 4 (2009): 846–55. http://dx.doi.org/10.1182/blood-2008-04-151928.

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AbstractHeat-shock protein 90 (Hsp90) acts as a molecular chaperone required for maintaining the conformational stability of client proteins regulating cell proliferation, survival, and apoptosis. Here we investigate the biologic significance of Hsp90 inhibition in multiple myeloma (MM) and other hematologic tumors using an orally available novel small molecule inhibitor SNX-2112, which exhibits unique activities relative to 17-allyamino-17-demethoxy-geldanamycin (17-AAG). SNX-2112 triggers growth inhibition and is more potent than 17-AAG against MM and other malignancies. It induces apoptosis

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Indrasari, Siti Dewi. "FAKTOR YANG MEMPENGARUHI INDEKS GLIKEMIK RENDAH PADA BERAS DAN POTENSI PENGEMBANGANNYA DI INDONESIA / Factors Affecting the Low Glycemic Index on Rice and Its Potential for Development in Indonesia." Jurnal Penelitian dan Pengembangan Pertanian 38, no. 2 (2019): 105. http://dx.doi.org/10.21082/jp3.v38n2.2019.p105-113.

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<p>Diabetes Mellitus (DM) is a disorder of glucose metabolism due to insulin deficiency both in absolute and relative terms caused by changes in dietary habits that result in obesity. Nationally in Indonesia, the prevalence of DM based on a doctor’s diagnosis in the population aged over or equal to 15 years is 2%. Consumption of rice with a low glycemic index is one way to regulate dietary patterns for people with type 2 diabetes. In Indonesia, rice varieties that have a low glycemic index (GI) value have been successfully identified. This paper aims to provide information and understand

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XING, WANCAI, WEI CHEN, YINING ZHANG, et al. "823-P: Molecular and Pharmacological Properties of GZR4, a Once-Weekly Insulin Analog." Diabetes 73, Supplement_1 (2024). http://dx.doi.org/10.2337/db24-823-p.

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Introduction: It was reported that the complex, formed between acylated insulin and human serum albumin (HSA), enters an essentially inactive albumin-bound depot, leading to a dramatically decreased potency. Objectives: This study was performed to develop a more potent once-weekly insulin analog GZR4 and investigate its molecular and pharmacological properties. Methods: In vitro assays were employed to characterize the biological attributes of GZR4 through its interactions with HSA and insulin receptor (IR), intracellular signaling, and cellular metabolic responses. In vivo efficacy was evalua

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Okorie, Charity Ebelechukwu, and Martin Afam Nwaokolo. "Determination of the Potency of Drugs used in Treatment of Type2 Diabete (A Case Study of Taraba State Specialist Hospital Jalingo)." African Scientific Reports, February 21, 2023, 63. http://dx.doi.org/10.46481/asr.2023.2.1.63.

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Diabetes is a medical condition in which the body cannot produce enough insulin to process the glucose in the blood. Type 2 diabetes is mostly diagnosed in order adults but it is increasingly seen in children, adolescent and younger adult. It is discovered that the rate at which patients are diagnosed of diabetes has been on the increase despite the series of diabetic drugs that are available. This prompted the researchers to carry out this research so as to determine the potency of drugs used in the treatment of type 2 diabetes. Data were collected from Specialist Hospital, Jalingo Taraba Sta

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Bosch, Rolien, Marcella Petrone, Rosalin Arends, et al. "Characterisation of cotadutide's dual GLP‐1/glucagon receptor agonistic effects on glycaemic control using an in vivo human glucose regulation quantitative systems pharmacology model." British Journal of Pharmacology, February 25, 2024. http://dx.doi.org/10.1111/bph.16336.

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AbstractBackground and PurposeCotadutide is a dual GLP‐1 and glucagon receptor agonist with balanced agonistic activity at each receptor designed to harness the advantages on promoting liver health, weight loss and glycaemic control. We characterised the effects of cotadutide on glucose, insulin, GLP‐1, GIP, and glucagon over time in a quantitative manner using our glucose dynamics systems model (4GI systems model), in combination with clinical data from a multiple ascending dose/Phase 2a (MAD/Ph2a) study in overweight and obese subjects with a history of Type 2 diabetes mellitus (NCT02548585)

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Khanal, Hari, Abhishek Upadhyay, Nischal Gupta, and Ram Kishor Joshi. "AYURVEDIC RASAUSADHIES USED IN THE MANAGEMENT OF PRAMEHA W.S.R. TO DIABETES MELLITUS." AYUSHDHARA, August 12, 2020, 2725–34. http://dx.doi.org/10.47070/ayushdhara.v7i3.541.

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Diabetes Mellitus (DM) is a group of metabolic disorders characterised by hyperglycaemia due to absolute or relative deficiency of insulin. It is characterised by polyuria, polydipsia, polyphagia, rapid weight loss, fatigue etc. Based on similarities in signs and symptoms DM can be correlated with Prameha/Madhumeha in Ayurveda. Rasausadhies (metallic formulations) have been used in the treatment of Diabetes mellitus with its excellence for centuries but their scientific evaluation has not systematically established with modern tools. Rasausadhies have been popularly used since the period of gr

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PUTRA, Wira Eka, Intan Nilatus Shofiyah, Adelia Riezka Rahim, Arief Hidayatullah, and Muhaimin Rifa’i. "Ameliorative Effect of Jamaican Cherry (Muntingia calabura L.) Leaf Extract Toward Glucose Control and Immune Cells Modulation in High Fat Diet-Administrated Mice." Yüzüncü Yıl Üniversitesi Tarım Bilimleri Dergisi, October 28, 2023, 1–13. http://dx.doi.org/10.29133/yyutbd.1331257.

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Hyperglycemia is a dangerous condition in which too much glucose circulates in the blood plasma and is the leading cause of diabetes mellitus. It is a complex condition with varying degrees that can change over time, mainly owing to metabolic factors that reduce insulin secretion, decrease glucose use, and increase glucose production. This study aims to evaluate Muntingia calabura leaf extract's effect on glucose control and immune cell modulation in high-fat diet-administrated mice. According to the result, we found that M. calabura leaf extract significantly reduced the fasting blood sugar.

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WANJUN, GUO, HAIXIA ZOU, ZHIYI ZHU, et al. "793-P: Biased GLP-1 Analog Ecnoglutide (XW003) Has Improved Efficacy Relative to Unbiased Peptides." Diabetes 73, Supplement_1 (2024). http://dx.doi.org/10.2337/db24-793-p.

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Introduction & Objective: Ecnoglutide (XW003) is a cAMP-biased GLP-1 analog being developed for the treatment of type 2 diabetes mellitus (T2DM) and obesity. The objective of this analysis was to compare the preclinical and clinical efficacy of ecnoglutide to unbiased GLP-1 peptides. Methods: Ecnoglutide was assessed for cAMP production and β-arrestin recruitment in GLP-1R reporter cell lines. Glucose control was tested in db/db mice administered a single subcutaneous dose of GLP-1 analogs, with blood glucose recorded for 144 h. Body weight and insulin response were evaluated in db/db mice

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Kim, Jung Kuk, Yohan Kim, Byeongjin Ye, et al. "SAT149 In Vitro Characterization Of A Novel Long-acting Glucagon Analog (HM15136) And Its Potential Effect In Animal Models Of Chronic Hypoglycemic Diseases." Journal of the Endocrine Society 7, Supplement_1 (2023). http://dx.doi.org/10.1210/jendso/bvad114.1014.

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Abstract Disclosure: J. Kim: Employee; Self; Hanmi Pharm. Co., Ltd. Y. Kim: Employee; Self; Hanmi Pharm. Co., Ltd. B. Ye: Employee; Self; Hanmi Pharm. Co., Ltd. W. Kim: Employee; Self; Hanmi Pharm. Co., Ltd. J. Kim: Employee; Self; Hanmi Pharm. Co., Ltd. S. Bae: Employee; Self; Hanmi Pharm. Co., Ltd. D. Kim: Employee; Self; Hanmi Pharm. Co., Ltd. S. Lee: Employee; Self; Hanmi Pharm. Co., Ltd. I. Choi: Employee; Self; Hanmi Pharm. Co., Ltd. Glucagon plays an essential role in glucose homeostasis, and has been used to treat acute hypoglycemia in diabetic patients. However, due to poor solubility

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