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Artykuły w czasopismach na temat „Inhibitor Activity”

Autor: Grafiati

Data publikacji: 6 września 2023

Data aktualizacji: 19 lipca 2025

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1

Böhm, Martina, Manuela Krause, Charis Von Auer, Wolfgang Miesbach, and Inge Scharrer. "The Frequency and the Significance of ADAMTS-13 Neutralising Inhibitors in 62 Patients with Non-Familial Thrombotic Thrombocytopenic Purpura." Blood 104, no. 11 (2004): 3945. http://dx.doi.org/10.1182/blood.v104.11.3945.3945.

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Abstract Neutralising inhibitors against ADAMTS-13 are detected in 51–67% of patients with Thrombotic Thrombocytopenic Purpura (TTP). These ADAMTS-13 inhibitors have not been very well characterised and the diagnostic or the prognostic value of these inhibitors is not established. In the present study, we measured ADAMTS-13 activity and the corresponding inhibitor titer in 96 samples from 62 patients with TTP at various stages of their disease. All patients presented with non-familial TTP. For patients with severe ADAMTS-13 activity without detectable inhibitor heritable ADAMTS-13 deficiency w

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VARGA, Andrei, Camelia URDĂ, Ramona Dina GALBEN, et al. "Soybean Trypsin Inhibitor Activity - a review." Hop and Medicinal Plants 31, no. 1-2 (2023): 151–60. https://doi.org/10.15835/hpm.v31i1-2.14745.

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Soybean (Glycine max) is one of the most important source of protein for food and feed globally. Complete utilization of protein in human and animal digestion can be reduced by certain trypsin inhibitory (TI) substances present in fresh soybeans. Two classes of protease inhibitors (polypeptides) are found in soybeans: Kunitz trypsin inhibitor (KTI) and Bowman-Birk trypsin inhibitor (BBI). KTI is primarily responsible for its trypsin inhibitory activity, while BBI has been reported to have nutraceutical properties. The content of TI in soybean depends on the soybean genotype, environmental fact

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Domoney, C., and T. Welham. "Trypsin inhibitors in Pisum: variation in amount and pattern of accumulation in developing seed." Seed Science Research 2, no. 3 (1992): 147–54. http://dx.doi.org/10.1017/s0960258500001276.

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AbstractA survey of Pisum genotypes for seed trypsin inhibitors revealed a tenfold range in the extent of inhibition. Approximately 90% of trypsin inhibitory activity was associated with two albumin fractions in selected variant lines. The differences among extreme variants were consistent in three environments, between two sources of trypsin tested and whether expressed on a unit protein or dry weight basis.A study of the appearance of trypsin inhibitors during seed development in selected highand low-inhibitor lines showed differences in the accumulation pattern of active inhibitors. An endo

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4

Sumanadasa, Subathdrage D. M., Christopher D. Goodman, Andrew J. Lucke, et al. "Antimalarial Activity of the Anticancer Histone Deacetylase Inhibitor SB939." Antimicrobial Agents and Chemotherapy 56, no. 7 (2012): 3849–56. http://dx.doi.org/10.1128/aac.00030-12.

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ABSTRACTHistone deacetylase (HDAC) enzymes posttranslationally modify lysines on histone and nonhistone proteins and play crucial roles in epigenetic regulation and other important cellular processes. HDAC inhibitors (e.g., suberoylanilide hydroxamic acid [SAHA; also known as vorinostat]) are used clinically to treat some cancers and are under investigation for use against many other diseases. Development of new HDAC inhibitors for noncancer indications has the potential to be accelerated by piggybacking onto cancer studies, as several HDAC inhibitors have undergone or are undergoing clinical

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Pintus, Francesca, Delia Spanò, Angela Corona, and Rosaria Medda. "Antityrosinase activity ofEuphorbia characiasextracts." PeerJ 3 (October 13, 2015): e1305. http://dx.doi.org/10.7717/peerj.1305.

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Tyrosinase is a well-known key enzyme in melanin biosynthesis and its inhibitors have become increasingly important because of their potential use as hypopigmenting agents. In the present study, the anti-melanogenic effect of aqueous and ethanolic extracts fromEuphorbia characiasleaves, stems, and flowers in cell-free and cellular systems was examined. All the extracts showed inhibitory effects against mushroom tyrosinase with leaf extracts exhibiting the lowest IC50values of 24 and 97 µg/mL for aqueous and ethanolic extracts respectively. Enzyme kinetic analysis indicated that leaf aqueous ex

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6

Milner, Malgorzata, Jadwiga Chroboczek, and Wlodzimierz Zagorski-Ostoja. "Engineered resistance against proteinases." Acta Biochimica Polonica 54, no. 3 (2007): 523–36. http://dx.doi.org/10.18388/abp.2007_3226.

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Exogenous proteinase inhibitors are valuable and economically interesting protective biotechnological tools. We examined whether small proteinase inhibitors when fused to a selected target protein can protect the target from proteolytic degradation without simultaneously affecting the function and activity of the target domain. Two proteinase inhibitors were studied: a Kazal-type silk proteinase inhibitor (SPI2) from Galleria mellonella, and the Cucurbita maxima trypsin inhibitor I (CMTI I). Both inhibitors target serine proteinases, are small proteins with a compact structure stabilized by a

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7

Jang, Seong, Bill Strickland, Lynda Finis, et al. "Abstract 4014: Comparative biochemical kinase activity analysis identifies rivoceranib as the most selective VEGFR-2 inhibitor compared with other TKIs with known activity against VEGFR-2." Cancer Research 83, no. 7_Supplement (2023): 4014. http://dx.doi.org/10.1158/1538-7445.am2023-4014.

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Abstract Introduction: Vascular endothelial growth factor receptor 2 (VEGFR-2) is a key regulator of tumor angiogenesis that is highly expressed in several tumor types and is a known target for anti-cancer therapy. Yet the clinical use of VEGFR-2 inhibitors has been challenged by limited efficacy and various side effects, potentially due to the low selectivity of these TKIs for VEGFR-2. Thus, potent VEGFR-2 inhibitors with improved selectivity are needed. Rivoceranib is an oral tyrosine kinase inhibitor (TKI) that potently and selectively inhibits VEGFR-2. A comparison of the potency and selec

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8

Korn, J. H., K. M. Brown, E. Downie, Z. H. Liao, and D. L. Rosenstreich. "Augmentation of IL 1-induced fibroblast PGE2 production by a urine-derived IL 1 inhibitor." Journal of Immunology 138, no. 10 (1987): 3290–94. http://dx.doi.org/10.4049/jimmunol.138.10.3290.

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Abstract IL 1, a monocyte-derived cytokine, has potent biologic effects in a variety of target tissues. The existence of naturally occurring inhibitors of IL 1 activity has been recently described; these inhibitors blocked one IL 1 effect: stimulation of thymocyte responses to mitogens. We examined the effect of one well-characterized inhibitor of IL 1, isolated from the urine of febrile patients, on a second IL 1 effect, stimulation of fibroblast PGE synthesis. In this system, purified preparations of the urinary inhibitor that completely blocked murine thymocyte proliferative responses to mi

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9

Muller, Florian, Selvi Kunnimalaiyaan, Parth Mangrolia, and Jill Olson. "Abstract 5913: TEAD1/4 inhibitors exhibit deeper biological impact and broader activity compared to TEAD1-only inhibitors in both monotherapy and combination without additional kidney toxicity." Cancer Research 84, no. 6_Supplement (2024): 5913. http://dx.doi.org/10.1158/1538-7445.am2024-5913.

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Abstract The TEAD transcription factors in association with the YAP/TAZ co-activators drive the expression of pro-proliferative and pro-oncogenic genes that underlies the transformed phenotype of many carcinomas. In addition, YAP-TEAD transcriptional activity is emerging as a major resistance mechanism for diverse precision oncology drugs, with the most extensive data for resistance to drugs targeting the MAPK pathway. There is a strong interest in generating inhibitors of YAP/TEAD transcriptional activity with TEAD palmitic acid site inhibitors having demonstrated encouraging pre-clinical act

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10

Han, Di, Huiqun Wang, Wei Cui, Beibei Zhang, and Bo-Zhen Chen. "Computational insight into the mechanisms of action and selectivity of Afraxis PAK inhibitors." Future Medicinal Chemistry 12, no. 5 (2020): 367–85. http://dx.doi.org/10.4155/fmc-2019-0273.

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Aim: The p21-activated kinases (PAKs) are involved in many important biological activity regulations. FRAX019, FRAX414, FRAX597, FRAX1036 and G-5555 were identified as PAKs inhibitors. Their detailed inhibitory mechanisms deserve further investigation. Results: Molecular dynamics simulations and further calculations for the PAK1/inhibitor and PAK4/inhibitor complexes indicate that their binding free energies are basically consistent with the trend of experimental activity data. Conclusion: The anchoring of residues Leu347PAK1 and Leu398PAK4 is the structural basis for designing Afraxis PAK inh

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11

Pujirahayu, Niken, Debu Kumar Bhattacharjya, Toshisada Suzuki та Takeshi Katayama. "α-Glucosidase Inhibitory Activity of Cycloartane-Type Triterpenes Isolated from Indonesian Stingless Bee Propolis and Their Structure–Activity Relationship". Pharmaceuticals 12, № 3 (2019): 102. http://dx.doi.org/10.3390/ph12030102.

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This study reports on the antioxidant activity and α-glucosidase inhibitory activity of five cycloartane-type triterpenes isolated from Indonesian stingless bee (Tetragonula sapiens Cockerell) propolis and their structure–activity relationships. The structure of the triterpenes was determined to include mangiferolic acid (1), Cycloartenol (2), ambonic acid (3), mangiferonic acid (4), and ambolic acid (5). The inhibitory test results of all isolated triterpenes against α-glucosidase showed a high potential for inhibitory activity with an IC50 range between 2.46 and 10.72 µM. Among the compounds

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12

Ganea, D., D. Cearlock, J. Minowada, and S. Dray. "A serine proteinase inhibitor produced by an HTLV I virus-transformed human T lymphocyte line." Journal of Immunology 138, no. 4 (1987): 1208–14. http://dx.doi.org/10.4049/jimmunol.138.4.1208.

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Abstract A previous report from our laboratory indicated that a proteinase inhibitor is produced by rabbit T lymphocytes. We now report that a human T cell line, C91/PL, produces a proteinase inhibitor which inhibits the enzymatic activity of trypsin and kallikrein. This newly identified proteinase inhibitor (LPI 1) did not inhibit the enzymatic activity of four other serine proteinases (thrombin, plasmin, chymotrypsin, or pancreatic elastase), a thiol proteinase (papain), or a carboxyl proteinase (pepsin). Active synthesis of LPI 1 by the C91/PL cell line was shown by the appearance of simila

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13

Bishop, P. B., J. Young, T. Peng, and J. F. Richards. "An inhibitor of ornithine decarboxylase in the thymus and spleen of dexamethasone-treated rats." Biochemical Journal 226, no. 1 (1985): 105–12. http://dx.doi.org/10.1042/bj2260105.

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A marked decrease in activity of ornithine decarboxylase in thymus and spleen occurs soon after treatment of rats with a glucocorticoid. In the present study, evidence was obtained that extracts of these tissues prepared 5 h after administration of dexamethasone, when the enzyme activity is very low, contain an inhibitor of ornithine decarboxylase. The inhibitor is also present at 12 h after treatment and, in lesser amount, at 2.5 h, but was not evident at 24 h. The inhibitory activity was destroyed by treatment with heat or with trypsin, and was not lost on dialysis of the extract. Preliminar

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14

Yan, Daojing, Jiakun Xu, Xiang Wang, et al. "Spiro-Oxindole Skeleton Compounds Are Efficient Inhibitors for Indoleamine 2,3-Dioxygenase 1: An Attractive Target for Tumor Immunotherapy." International Journal of Molecular Sciences 23, no. 9 (2022): 4668. http://dx.doi.org/10.3390/ijms23094668.

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Indoleamine 2,3-dioxygenase 1 (IDO1) is an attractive heme enzyme for its significant function in cancer immunotherapy. Potent IDO1 inhibitors have been discovered for decades, whereas no clinical drugs are used for cancer treatment up to now. With the goal of developing medically valuable IDO inhibitors, we performed a systematic study of SAR405838 analogs with a spiro-oxindole skeleton in this study. Based on the expression and purification of human IDO1, the inhibitory activity of spiro-oxindole skeleton compounds to IDO1 was evaluated by IC50 and Ki values. The results demonstrated that in

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15

Arita, Minetaro, Takaji Wakita, and Hiroyuki Shimizu. "Cellular kinase inhibitors that suppress enterovirus replication have a conserved target in viral protein 3A similar to that of enviroxime." Journal of General Virology 90, no. 8 (2009): 1869–79. http://dx.doi.org/10.1099/vir.0.012096-0.

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Previously, we identified a cellular kinase inhibitor, GW5074, that inhibits poliovirus (PV) and enterovirus 71 replication strongly, although its target has remained unknown. To identify the target of GW5074, we searched for cellular kinase inhibitors that have anti-enterovirus activity similar or related to that of GW5074. With this aim, we performed screenings to identify cellular kinase inhibitors that could inhibit PV replication cooperatively with GW5074 or synthetically in the absence of GW5074. We identified MEK1/2 inhibitors (SL327 and U0126), an EGFR inhibitor (AG1478) and a phosphat

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16

Aghaali, Negar, Mohammad Ghadamyari, Vahid Hosseininaveh, and Nasir Saberi Riseh. "PROTEASE INHIBITOR FROM THE CRUDE EXTRACT OF PLANT SEEDS AFFECTS THE DIGESTIVE PROTEASES IN HYPHANTRIA CUNEA (LEP.: ARCTIIDAE)." Journal of Plant Protection Research 53, no. 4 (2013): 338–46. http://dx.doi.org/10.2478/jppr-2013-0051.

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Abstract Proteases are one of the most important digestive enzymes in the midgut of Hyphantria cunea Drury. Proteases are responsible for protein digestion. In the present study, we evaluated the efficiency of some plant inhibitors on proteases in the gut of the H. cunea. Last instar larvae were collected from mulberry trees. The digestive system of the larvae was used as an enzyme source. The total proteolytic and trypsin activity were assessed by the hemoglobin and BApNA, respectively, as the substrate. The evaluation of the total proteolytic and trypsin activities in various pHs showed the

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17

Javaid, Bushra. "Anti-trypsin and antihypertensive activity of protein extracts from Nigella sativa seeds." Pakistan Journal of Agricultural Sciences 58, no. 04 (2021): 1237–43. http://dx.doi.org/10.21162/pakjas/21.204.

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Protease inhibitors (PIs) are a ubiquitous, diverse group of molecules present in multiple forms in all organisms. These inhibitors inactivate proteases from predators/pathogens in addition to regulating intracellular proteolysis. In addition to intracellular localization, storage organs of plants are also a potential site of protease inhibitors. Proteins with trypsin inhibitory activity were isolated from Nigella sativa seed extracts by ammonium sulphate precipitation. Extraction conditions were optimized by choosing an optimum solvent, temperature and incubation period. The highest inhibitor

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Fujii, Hidetoshi, Moeno Ito, Kentaro Nishioka, et al. "Isolation of Allosteric Tryptase Inhibitor from Methanol Extract of Rhubarb and Enhancement of Its Tryptase Inhibitory Activity by Compounds That Were Screened by In Silico Screening." Molecules 30, no. 6 (2025): 1341. https://doi.org/10.3390/molecules30061341.

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Tryptase, which is abundant in human mast cells and is involved in allergic inflammations such as asthma, is a serine protease. We isolated a tryptase inhibitor, procyanidin B8 3,3′-di-O-gallate (PB8GG’), a tannin, from the methanol extract of rhubarb (RHEI RHIDOMA), which is a traditional Chinese medicine (Kampo medicine in Japan). Since it did not inhibit another serine protease trypsin, PB8GG’ specifically inhibited tryptase. A standard kinetic analysis of the inhibitory fashion of PB8GG’ against tryptase suggested that PB8GG’ inhibited tryptase in an allosteric manner. We searched for othe

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Cao, Jiangying, Wei Zhao, Chunlong Zhao, et al. "Development of a Bestatin-SAHA Hybrid with Dual Inhibitory Activity against APN and HDAC." Molecules 25, no. 21 (2020): 4991. http://dx.doi.org/10.3390/molecules25214991.

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With five histone deacetylase (HDAC) inhibitors approved for cancer treatment, proteolysis-targeting chimeras (PROTACs) for degradation of HDAC are emerging as an alternative strategy for HDAC-targeted therapeutic intervention. Herein, three bestatin-based hydroxamic acids (P1, P2 and P3) were designed, synthesized and biologically evaluated to see if they could work as HDAC degrader by recruiting cellular inhibitor of apoptosis protein 1 (cIAP1) E3 ubiquitin ligase. Among the three compounds, the bestatin-SAHA hybrid P1 exhibited comparable even more potent inhibitory activity against HDAC1,

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Juárez-Mercado, K. Eurídice, Fernando D. Prieto-Martínez, Norberto Sánchez-Cruz, Andrea Peña-Castillo, Diego Prada-Gracia, and José L. Medina-Franco. "Expanding the Structural Diversity of DNA Methyltransferase Inhibitors." Pharmaceuticals 14, no. 1 (2020): 17. http://dx.doi.org/10.3390/ph14010017.

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Inhibitors of DNA methyltransferases (DNMTs) are attractive compounds for epigenetic drug discovery. They are also chemical tools to understand the biochemistry of epigenetic processes. Herein, we report five distinct inhibitors of DNMT1 characterized in enzymatic inhibition assays that did not show activity with DNMT3B. It was concluded that the dietary component theaflavin is an inhibitor of DNMT1. Two additional novel inhibitors of DNMT1 are the approved drugs glyburide and panobinostat. The DNMT1 enzymatic inhibitory activity of panobinostat, a known pan inhibitor of histone deacetylases,

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Li, Qi, Hongyu Yang, Jun Mo, et al. "Identification by shape-based virtual screening and evaluation of new tyrosinase inhibitors." PeerJ 6 (January 26, 2018): e4206. http://dx.doi.org/10.7717/peerj.4206.

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Targeting tyrosinase is considered to be an effective way to control the production of melanin. Tyrosinase inhibitor is anticipated to provide new therapy to prevent skin pigmentation, melanoma and neurodegenerative diseases. Herein, we report our results in identifying new tyrosinase inhibitors. The shape-based virtual screening was performed to discover new tyrosinase inhibitors. Thirteen potential hits derived from virtual screening were tested by biological determinations. Compound 5186-0429 exhibited the most potent inhibitory activity. It dose-dependently inhibited the activity of tyrosi

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Michisaka, Saki, Hitoshi Sase, Yukako Tachibana, et al. "Abstract 1664: Combination of LUNA18, a novel RAS inhibitor, with KRAS G12C inhibitors augments anti-tumor activity via inhibition of MAPK pathway reactivation." Cancer Research 84, no. 6_Supplement (2024): 1664. http://dx.doi.org/10.1158/1538-7445.am2024-1664.

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Abstract RAS gene alterations, found in approximately 15% of all cancers and known oncogenes, are recognized as promising therapeutic targets. KRAS G12C inhibitors were the first FDA-approved RAS targeting agent, but their efficacy of monotherapy is limited. Reactivation of the MAPK pathway is reported to be the one of the causes for attenuating efficacy of KRAS G12C inhibitors. LUNA18 is the cyclic peptide that binds to RAS mutants and wildtype, including KRAS, NRAS and HRAS, thereby inhibiting protein-protein interaction (PPI) between the inactive form of RAS and GEFs (guanine nucleotide exc

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Kubyshkin, A. V., and I. I. Fomochkina. "THE INFLUENCE OF INTRODUCTION OF PROTEINASE INHIBITORS ON EFFICIENCY FOR SUPPRESSION OF PROTEOLYTIC ACTIVATION OF PNEUMONIA." Fiziolohichnyĭ zhurnal 55, no. 1 (2009): 43–48. http://dx.doi.org/10.15407/fz55.01.043.

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We studied the influence of a way of introduction proteinase inhibitors on efficiency of suppression of proteolysis activation during pneumonia. Comparative study of efficiency of proteases inhibition in experimental pneumonia has shown higher efficacy of local introduction of drugs. Intravenous and intraperitoneal introduction of proteinase inhibitors exhibited inhibitory effect of a smaller degree on local and systemic proteases activation, did not decrease an acute phase of response of a-1-protease inhibitor in comparison with endotracheal instillation of Contrycal and Ingiprol. The study h

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Wang, Xing, Junfang Guo, Zhongqi Ning, and Xia Wu. "Discovery of a Natural Syk Inhibitor from Chinese Medicine through a Docking-Based Virtual Screening and Biological Assay Study." Molecules 23, no. 12 (2018): 3114. http://dx.doi.org/10.3390/molecules23123114.

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Spleen tyrosine kinase (Syk) is a critical target protein for treating immunoreceptor signalling-mediated allergies. In this study, a virtual screening of an in-house Chinese medicine database followed by biological assays was carried out to identify novel Syk inhibitors. A molecular docking method was employed to screen for compounds with potential Syk inhibitory activity. Then, an in vitro kinase inhibition assay was performed to verify the Syk inhibitory activity of the virtual screening hits. Subsequently, a β-hexosaminidase release assay was conducted to evaluate the anti-mast cell degran

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Wang, Tao, Yangyang Jiang, Xiaoling Chen, et al. "Ranacyclin-NF, a Novel Bowman–Birk Type Protease Inhibitor from the Skin Secretion of the East Asian Frog, Pelophylax nigromaculatus." Biology 9, no. 7 (2020): 149. http://dx.doi.org/10.3390/biology9070149.

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Serine protease inhibitors are found in plants, animals and microorganisms, where they play important roles in many physiological and pathological processes. Inhibitor scaffolds based on natural proteins and peptides have gradually become the focus of current research as they tend to bind to their targets with greater specificity than small molecules. In this report, a novel Bowman–Birk type inhibitor, named ranacyclin-NF (RNF), is described and was identified in the skin secretion of the East Asian frog, Pelophylax nigromaculatus. A synthetic replicate of the peptide was subjected to a series

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Jo, Sooheum, Jin-Hee Kim, Jiyeon Lee, Youngjun Park, and Jaebong Jang. "Azumamides A-E: Isolation, Synthesis, Biological Activity, and Structure–Activity Relationship." Molecules 27, no. 23 (2022): 8438. http://dx.doi.org/10.3390/molecules27238438.

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Cyclic peptides are one of the important chemical groups in the HDAC inhibitor family. Following the success of romidepsin in the clinic, naturally occurring cyclic peptides with a hydrophilic moiety have been intensively studied to test their function as HDAC inhibitors. Azumamides A-E, isolated from Mycale izuensis, are one of the powerful HDAC inhibitor classes. Structurally, azumamides A-E consist of three D-α-amino acids and unnatural β-amino acids such as 3-amino-2-methyl-5-nonenedioic acid-9-amide (Amnna) and 3-amino-2-methyl-5-nonenoic-1,9-diacid (Amnda). Moreover, azumamides have a re

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Hs, Ranjini, Padmanabha Udupa Eg, Shobha U. Kamath, Manjunath Setty, Basavaraj Hadapad, and Asha Kamath. "AN IN VITRO STUDY OF CINNAMOMUM ZEYLANICUM AS NATURAL INHIBITOR OF ANGIOTENSIN-CONVERTING ENZYME (ACE) ON SHEEP (OVIS ARIES) TISSUES." Asian Journal of Pharmaceutical and Clinical Research 9, no. 5 (2016): 249. http://dx.doi.org/10.22159/ajpcr.2016.v9i5.13424.

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ABSTRACTObjective: The present study was aimed to find the angiotensin-converting enzyme (ACE) inhibitory activity using the methanolic extract ofCinnamomum zeylanicum (as a natural inhibitor) on sheep tissues as the enzyme source.Methods: Hippuryl-histidyl-leucine (HHL) as a substrate, tissue ACE activity was measured spectrophotometrically at 228 nm. For an incubationperiod of 30 minutes at 37°C, the linearity of ACE activity of kidney, lung, and testis enzyme was established. A known medicinal plant C. zeylanicumwas used as natural inhibitor of ACE. In this enzyme assay, inhibitory effect o

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de Freitas, Sonia Maria, Luciano Paulino Silva, Jose Roberto S. A. Leite, and Carlos Bloch Jr. "Stability of a black eyed pea trypsin/chymotrypsin inhibitor (BTCI)." Protein & Peptide Letters 7, no. 6 (2000): 397–401. http://dx.doi.org/10.2174/092986650706221207164315.

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Abstract: The stability of BTCI has been investigated as function of pH and temperature, following its inhibitory activity against trypsin. The isolated inhibitor of 9,084 Oa is stable over pH 3 to 12 at 25°C. BTCI showed high thermal stability ranging from 25 to 95°C at pH 3 and 7. However, the protein lost about 20% of its inhibitory activity over 75°C at pH 8.2. The results indicated that BTCI is extremely stable to heat and pH as typical of Bowman-Birk inhibitors.

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Li, Wenchao, Bowen Pan, Yang Shi, et al. "Identification of poly(ADP-ribose)polymerase 1 and 2 (PARP1/2) as targets of andrographolide using an integrated chemical biology approach." Chemical Communications 57, no. 51 (2021): 6308–11. http://dx.doi.org/10.1039/d1cc02272e.

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Andrographolide is the first PARP natural product inhibitor that does not contain an amide structure and has an inhibitory activity in the nanomolar range. This chemical structure is significant for expanding the structural type of PARP inhibitors.

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Antonucci, T., J. S. Warmus, J. C. Hodges, and D. G. Nickell. "Characterization of the Antiviral Activity of Highly Substituted Pyrroles: A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitor." Antiviral Chemistry and Chemotherapy 6, no. 2 (1995): 98–108. http://dx.doi.org/10.1177/095632029500600204.

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As a result of mass screening of the Parke-Davis Pharmaceutical compound library for inhibitors of HIV-1 reverse transcriptase (RT) activity, a novel class of inhibitor, the pyrroles, was identified. Subsequently, a series of analogues was screened for inhibitory activity against HIV-1 and some structure-activity relationships were identified. Further characterization of the most potent pyrrole involved comparing its effects in peripheral blood lymphocytes (PBLs) with its effects in transformed cell lines; the pyrrole had the same efficacy (EC50 = approximately 2 μM) but was less toxic in PBLs

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Wang, Shuyi, Mingwei Zhu, Liyong Sun, Tao Huang, and Shuxian Li. "Putative Spatiotemporal Changes in Inhibitor Activity during Cold Stratification of Sapium sebiferum Seeds." Horticulturae 10, no. 3 (2024): 242. http://dx.doi.org/10.3390/horticulturae10030242.

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Sapium sebiferum is a tree with socioeconomic, environmental, and medicinal value. S. sebiferum seeds possess physiological dormancy, which is induced by endogenous inhibitors and can be broken by cold stratification. However, the putative spatiotemporal changes in inhibitor activity are currently unknown, which can hinder the propagation of S. sebiferum seeds. The objective of this study was to investigate the spatiotemporal dynamics of inhibitor activity and its effect on germination during the cold stratification of S. sebiferum seeds. An extractant consisting of 80% methanol was used to ex

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Potempa, J., J. J. Enghild та J. Travis. "The primary elastase inhibitor (elastasin) and trypsin inhibitor (contrapsin) in the goat are serpins related to human α1-anti-chymotrypsin". Biochemical Journal 306, № 1 (1995): 191–97. http://dx.doi.org/10.1042/bj3060191.

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Two primary serine proteinase inhibitors in goat plasma have been isolated and characterized. The N-terminal sequence analysis of the purified proteins revealed that they are closely related to each other and are highly homologous to human alpha 1-anti-chymotrypsin rather than alpha 1-proteinase inhibitor. However, despite structural similarities the inhibitory specificity of the goat inhibitors differed from each other and from that of anti-chymotrypsin. In contrast with human anti-chymotrypsin, one of the goat inhibitors was shown to be a strong and specific inhibitor of trypsin (k(ass.) = 1

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R, Sangeetha, and Padmini R. "ANTIMICROBIAL ACTIVITY OF A PROTEASE INHIBITOR ISOLATED FROM THE RHIZOME OF CURCUMA AMADA." Asian Journal of Pharmaceutical and Clinical Research 10, no. 9 (2017): 131. http://dx.doi.org/10.22159/ajpcr.2017.v10i9.18257.

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Objective: Protease inhibitors (PIs) are effective antimicrobial agents, and this study was aimed to study the antibacterial efficacy of a PI isolated from the rhizome of Curcuma amada.Methods: A proteinaceous protease inhibitor was isolated from the rhizome of C. amada and purified by Sephadex G-50 gel permeation chromatography. The purified inhibitor was denoted as Curcuma amada protease inhibitor (CAPI). The antibacterial effect of CAPI against Gram-positive and Gram-negative bacteria, the minimal inhibitory concentration (MIC), and minimal bactericidal concentration (MBC) of CAPI was studi

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Pérez-Vizcaíno, Francisco, José G. López-López, Rocío Santiago, et al. "Postnatal maturation in nitric oxide-induced pulmonary artery relaxation involving cyclooxygenase-1 activity." American Journal of Physiology-Lung Cellular and Molecular Physiology 283, no. 4 (2002): L839—L848. http://dx.doi.org/10.1152/ajplung.00293.2001.

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The maturation in the vasodilator response to nitric oxide (NO) in isolated intrapulmonary arteries was analyzed in newborns and 15- to 20-day-old piglets. The vasodilator responses to NO gas but not to the NO donor sodium nitroprusside increased with age. The inhibitory effects of the superoxide dismutase inhibitor diethyldithiocarbamate and xanthine oxidase plus hypoxanthine and the potentiation induced by superoxide dismutase and MnCl2 of NO-induced vasodilatation were similar in the two age groups. Diphenyleneiodonium (NADPH oxidase inhibitor) potentiated the response to NO, and this effec

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Szutowski, Mirosław M., Katarzyna Zalewska, Marta Jadczak, and Monika Marek. "In vivo effect of diallyl sulfide and cimetidine on phenacetin metabolism and bioavailability in rat." Acta Biochimica Polonica 49, no. 1 (2002): 249–56. http://dx.doi.org/10.18388/abp.2002_3842.

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Numerous cytochrome P450 inhibitors have been described as effective modulators of cytochrome P450 isoforms activity in vitro. Their inhibitory efficiency may be considerably modified after in vivo application. The aim of this study was to examine the effect of oral administration of diallyl sulfide--a cytochrome P450 2E1 inhibitor and cimetidine--a cytochrome P450 2C6 and 2C11 inhibitor on rat serum concentration of phenacetin and its metabolite acetaminophen. Both inhibitors increased area under the curve (AUC(0-4 h)) for phenacetin by 50%. Only cimetidine reduced AUC(0-4 h) for acetaminophe

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Wang, Lei, Yinglu Chen, Feng Wu, Shasha Wu, Xiaojun Hu, and Yawei Shi. "LUTI: a double-function inhibitor isolated from naked flax seeds." Acta Biochimica et Biophysica Sinica 51, no. 10 (2019): 989–96. http://dx.doi.org/10.1093/abbs/gmz087.

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Abstract Acute glucose fluctuation during the postprandial period causes a risk for type 2 diabetes mellitus (T2DM). α-Glucosidase inhibitors have been approved as therapeutic agents for diabetes. In the present study, a protein with α-glucosidase inhibitory activity from Flax (Linum usitatissimum) seeds was isolated using a one-step purification with Q-Sepharose4B column, followed by Sephacryl S-200 size-exclusion chromatography. It was identified as a trypsin inhibitor, named L. usitatissimum trypsin inhibitor (LUTI). The half maximal inhibitory concentration (IC50) of LUTI was 113.92 μM for

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Shi, Qizhen, Erin L. Kuether, Jocelyn A. Schroeder, Crystal L. Perry, Scot A. Fahs, and Robert R. Montgomery. "Factor VIII Inhibitors: Von Willebrand Factor Makes A Difference In Vitro and In Vivo." Blood 116, no. 21 (2010): 709. http://dx.doi.org/10.1182/blood.v116.21.709.709.

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Abstract Abstract 709 The important association between von Willebrand factor (VWF) and factor VIII (FVIII) has been investigated for decades, but the effect of VWF on FVIII inhibitors is still controversial. Studies have demonstrated that some anti-FVIII inhibitory antibodies inhibit VWF-FVIII interaction, while others rely on the presence of VWF to inhibit FVIII activities. The influence of VWF on the Bethesda assay, which is routinely used in the clinic to determine the titer of FVIII-neutralizing inhibitors, is still uncertain because the plasma from hemophilia A patients with inhibitors c

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Tsuda, Yuko, Koushi Hidaka, Keiko Hojo, and Yoshio Okada. "Exploration of Active Site-Directed Plasmin Inhibitors: Beyond Tranexamic Acid." Processes 9, no. 2 (2021): 329. http://dx.doi.org/10.3390/pr9020329.

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Plasmin (Plm), a trypsin-like serine protease, is responsible for fibrinolysis pathway and pathologic events, such as angiogenesis, tumor invasion, and metastasis, and alters the expression of cytokines. A growing body of data indicates that a Plm inhibitor is a potential candidate as an anti-inflammatory and anti-cancer agent. A class of active site-directed plasmin inhibitors containing tranexamic acid residue has been designed. As evidenced by docking studies, the inhibitor binds to the active site not to the lysine binding site (LBS) in plasmin, thus preventing plasmin from digesting the s

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Lechner, Christian, Maren Flaßhoff, Hannes Falke, et al. "[b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors." Molecules 24, no. 22 (2019): 4090. http://dx.doi.org/10.3390/molecules24224090.

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Since hyperactivity of the protein kinase DYRK1A is linked to several neurodegenerative disorders, DYRK1A inhibitors have been suggested as potential therapeutics for Down syndrome and Alzheimer’s disease. Most published inhibitors to date suffer from low selectivity against related kinases or from unfavorable physicochemical properties. In order to identify DYRK1A inhibitors with improved properties, a series of new chemicals based on [b]-annulated halogenated indoles were designed, synthesized, and evaluated for biological activity. Analysis of crystal structures revealed a typical type-I bi

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Bilan, Philip J., Jonathan B. Weitzman, Tracey Pflieger, C. Roy D. Lancaster, Alan Stafford, and Richard M. Epand. "Potent inhibitors of glucagon-stimulated adenylate cyclase associated with serum lipoprotein particles." Biochemistry and Cell Biology 67, no. 11-12 (1989): 759–62. http://dx.doi.org/10.1139/o89-114.

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Lipoprotein fractions from some individuals have inhibitory effects on rat liver adenylate cyclase. Precipitation of the lipoprotein fractions with acetone released an inhibitory factor, which was soluble in acetone–H2O (3:1, v/v). The inhibition was greater against glucagon-stimulated activity than against basal activity. Acetone extraction increased the potency of inhibition. All three lipoprotein fractions, i.e., very low, low, and high density lipoproteins, released some inhibitory component after acetone extraction. The inhibitor was concentrated in the lipoprotein fractions, since aceton

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Hong, Tran Thi, Ton That Huu Dat, Nguyen Phuong Hoa, et al. "Expression and characterization of a new serine protease inhibitory protein in Escherichia coli." Biomedical Research and Therapy 7, no. 2 (2020): 3633–44. http://dx.doi.org/10.15419/bmrat.v7i2.590.

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Introduction: Proteases are enzymes that catalyze the hydrolysis of peptide bonds and play an important role in almost all biological processes. However, excessive protein proteolysis can be implicated in several diseases, such as cancer, as well as cardiovascular, inflammatory, neurodegenerative, bacterial, viral and parasitic diseases. In these cases, protease inhibitors can be used as one of versatile tools for regulating proteolytic activity of target proteases as well as therapeutic applications. In this study, we expressed and characterized a new serine protease inhibitory protein (PI-QT

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Wang, Wei-Ya, Chien-Kei Wei, Che-Ming Teng, and Chin-Chung Wu. "Combined blockade of thrombin anion binding exosite-1 and PAR4 produces synergistic antiplatelet effect in human platelets." Thrombosis and Haemostasis 105, no. 01 (2011): 88–95. http://dx.doi.org/10.1160/th10-05-0305.

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SummaryThrombin exosite-1 mediates the specific binding of thrombin with fibrinogen and protease-activated receptor (PAR) 1. Exosite-1 inhibitors have been shown to effectively decrease the clotting activity of thrombin, while their antiplatelet effects are relatively weak. In the present study, the inhibitory effects of two exosite-1 inhibitors, hirugen and HD1, but not the exosite-2 inhibitor HD22, on thrombin-induced platelet aggregation and P-selectin expression were dramatically enhanced by a PAR4 antagonist, YD-3. In contrast, the PAR1 antagonist SCH-79797 did not affect the antiplatelet

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Miao, Yuxi, Guanzhu Chen, Xinping Xi, et al. "Discovery and Rational Design of a Novel Bowman-Birk Related Protease Inhibitor." Biomolecules 9, no. 7 (2019): 280. http://dx.doi.org/10.3390/biom9070280.

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Anuran amphibian skin secretions are a rich source of peptides, many of which represent novel protease inhibitors and can potentially act as a source for protease inhibitor drug discovery. In this study, a novel bioactive Bowman-Birk type inhibitory hexadecapeptide of the Ranacyclin family from the defensive skin secretion of the Fukien gold-striped pond frog, Pelophlax plancyi fukienesis, was successfully isolated and identified, named PPF-BBI. The primary structure of the biosynthetic precursor was deduced from a cDNA sequence cloned from a skin-derived cDNA library, which contains a consens

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Kelly, Julie A., Gaia A. Scalabrino, Gillian R. Slator, et al. "Structure–activity studies with high-affinity inhibitors of pyroglutamyl-peptidase II." Biochemical Journal 389, no. 2 (2005): 569–76. http://dx.doi.org/10.1042/bj20041722.

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Inhibitors of PPII (pyroglutamyl-peptidase II) (EC 3.4.19.6) have potential applications as investigative and therapeutic agents. The rational design of inhibitors is hindered, however, by the lack of an experimental structure for PPII. Previous studies have demonstrated that replacement of histidine in TRH (thyrotropin-releasing hormone) with asparagine produces a competitive PPII inhibitor (Ki 17.5 μM). To gain further insight into which functional groups are significant for inhibitory activity, we investigated the effects on inhibition of structural modifications to Glp-Asn-ProNH2 (pyroglut

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Dong, Shu Ting, Hong Zhang, Na Xu, Ping Li, Si Si Xu, and Chun Yu Xi. "Effects of Two Trypsin Inhibitors on Trypsin in Activity and Structure." Advanced Materials Research 1073-1076 (December 2014): 1824–27. http://dx.doi.org/10.4028/www.scientific.net/amr.1073-1076.1824.

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Two reversible trypsin inhibitors, Kunitz trypsin inhibitor (KTI) and Bowman-Birk trypsin inhibitor (BBI) were compared to find the more optimal one as the inhibit factor during trypsin immobilization. Fluorescence spectroscopy, UV–visible absorption spectroscopy and circular dichroism (CD) spectroscopy were used to explore the effects of the two inhibitors on trypsin in activity and structure. The results showed that both inhibitors combined with trypsin in 1:1. CD circular dichroism spectroscopy showed that KTI and BBI led to different changes in trypsin second structure. The results can hel

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Mahmood, Ahmed A. J., та Safaa P. Bahnam. "DOCKING, SYNTHESIS AND β-LACTAMASE INHIBITORY ACTIVITY EVALUATION FOR NEW AMIDE COMPOUNDS". Chemical Problems 22, № 2 (2024): 139–49. http://dx.doi.org/10.32737/2221-8688-2024-2-139-149.

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The beta-lactams are recognized as effective antibiotics for treating infections, yet bacterial production of β-lactamase, which hydrolyzes the beta-lactam ring, can render these drugs inactive. Combining these antibiotics with a β-lactamase inhibitor, such as clavulanic acid, mitigates this resistance. In a docking study involving Temoniera-1 (TEM-1), 1pzp, we induced the synthesis of eight amide compounds by reacting acid chloride derivatives with sulphathiazol or oxadiazol amine, forming an amide bond. The newly synthesized compounds were differentiated using physical and spectroscopic meth

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CHEN, Ching-Jiunn, Hui-Sheng HUANG, Yu-Tsong LEE, Chia-Yi YANG, and Wen-Chang CHANG. "Characterization and purification of a lipoxygenase inhibitor in human epidermoid carcinoma A431 cells." Biochemical Journal 327, no. 1 (1997): 193–98. http://dx.doi.org/10.1042/bj3270193.

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A lipoxygenase inhibitor in the cytosolic fraction of human epidermoid carcinoma A431 cells was characterized and purified. The cytosolic inhibitor lost the inhibitory activity upon heating at 75 °C for 15 min or pretreating with 1 mg/ml trypsin at 37 °C for 60 min. Cytosol, after dialysis, lost the inhibitory activity but its inhibitory activity recovered when 1 mM GSH was added to the dialysate. The inhibitory activity of cytosol was also abolished by treatment either with 1 mM iodoacetate at 4 °C for 1 h or with 0.5 mM H2O2. The pI of the inhibitor was approx. 7.0. In addition to 12-lipoxyg

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Asin-Milan, Odalis, Mohamed Sylla, Mohamed El-Far, et al. "Synergistic Combinations of the CCR5 Inhibitor VCH-286 with Other Classes of HIV-1 Inhibitors." Antimicrobial Agents and Chemotherapy 58, no. 12 (2014): 7565–69. http://dx.doi.org/10.1128/aac.03630-14.

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ABSTRACTHere, we evaluated thein vitroanti-HIV-1 activity of the experimental CCR5 inhibitor VCH-286 as a single agent or in combination with various classes of HIV-1 inhibitors. Although VCH-286 used alone had highly inhibitory activity, paired combinations with different drug classes led to synergistic or additive interactions. However, combinations with other CCR5 inhibitors led to effects ranging from synergy to antagonism. We suggest that caution should be exercised when combining CCR5 inhibitorsin vivo.

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Venkatachalam, Prerana, and Varalakshmi Kilingar Nadumane. "Purification and Characterization of a Protease Inhibitor with Anticancer Potential from Bacillus endophyticus JUPR15." Current Cancer Therapy Reviews 15, no. 1 (2019): 74–82. http://dx.doi.org/10.2174/1573394714666180321150605.

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Introduction:Introduction: Protease Inhibitors (PIs) constitute a group of proteins widely distributed among all organisms and their main function includes their ability to inhibit the proteolytic activity. PIs represent an important role in the regulation of various cellular physiological and biological processes, including cell cycle, cell death, differentiation and immune response.Material and Methods:Hence, in our search for novel anticancer compounds, we isolated microorganisms from various environmental sources and screened them for the production of protease inhibitors. Promising isolat

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OLU, Joshua, Lawrence Onyeoma MADU, Gbenga Samson OGUNMEFUN, Oluchi Cynthia ABIAMERE, Olugbenga Olumide OMOSEHIN, and Hajara Oyiza YUSUF. "Isolation and Partial characterization of Cysteine Protease Inhibitor from Water Melon (Citrullus lanatus) Seeds." Journal of Biochemistry and Molecular Biology 2, no. 1 (2024): 44–59. https://doi.org/10.36108/jbmb/4202.20.0150.

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Cysteine protease inhibitors (CPIs) have a vital role in the strict regulation and control of cysteine protease activity. In this work, a cysteine protease inhibitor (CPI) from watermelon (Citrullus lanatus) seeds was isolated, purified, and partially characterised. Ammonium sulfate precipitation was used to extract CPI, then size exclusion chromatography and ion exchange were used to further purify it. Papain was used to assess the inhibitory action, and identifying the ideal temperature stability and method of inhibition were part of the biochemical characterisation. The protein content of t

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