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Artykuły w czasopismach na temat „HAT Activators”

Autor: Grafiati

Data publikacji: 3 czerwca 2025

Data aktualizacji: 31 lipca 2025

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1

Carrozza, Michael J., Sam John, Alok Kumar Sil, James E. Hopper, and Jerry L. Workman. "Gal80 Confers Specificity on HAT Complex Interactions with Activators." Journal of Biological Chemistry 277, no. 27 (2002): 24648–52. http://dx.doi.org/10.1074/jbc.m201965200.

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Peng, Guang-Hua, and Shiming Chen. "Crx activates opsin transcription by recruiting HAT-containing co-activators and promoting histone acetylation." Human Molecular Genetics 16, no. 20 (2007): 2433–52. http://dx.doi.org/10.1093/hmg/ddm200.

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Selvi, B. Ruthrotha, Jean-Christophe Cassel, Tapas K. Kundu, and Anne-Laurence Boutillier. "Tuning acetylation levels with HAT activators: Therapeutic strategy in neurodegenerative diseases." Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms 1799, no. 10-12 (2010): 840–53. http://dx.doi.org/10.1016/j.bbagrm.2010.08.012.

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Chen, Chi-Ju, Zhong Deng, Alex Y. Kim, Gerd A. Blobel, and Paul M. Lieberman. "Stimulation of CREB Binding Protein Nucleosomal Histone Acetyltransferase Activity by a Class of Transcriptional Activators." Molecular and Cellular Biology 21, no. 2 (2001): 476–87. http://dx.doi.org/10.1128/mcb.21.2.476-487.2001.

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ABSTRACT The transcriptional coactivator CREB binding protein (CBP) possesses intrinsic histone acetyltransferase (HAT) activity that is important for gene regulation. CBP binds to and cooperates with numerous nuclear factors to stimulate transcription, but it is unclear if these factors modulate CBP HAT activity. Our previous work showed that CBP interacts with the Epstein-Barr virus-encoded basic region zipper (b-zip) protein, Zta, and augments its transcriptional activity. Here we report that Zta strongly enhances CBP-mediated acetylation of nucleosomal histones. Zta stimulated the HAT acti

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5

Hassan, Ahmed H., Salma Awad, Zeina Al-Natour, Samah Othman, Farah Mustafa, and Tahir A. Rizvi. "Selective recognition of acetylated histones by bromodomains in transcriptional co-activators." Biochemical Journal 402, no. 1 (2007): 125–33. http://dx.doi.org/10.1042/bj20060907.

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Bromodomains are present in many chromatin-associated proteins such as the SWI/SNF and RSC chromatin remodelling and the SAGA HAT (histone acetyltransferase) complexes, and can bind to acetylated lysine residues in the N-terminal tails of the histones. Lysine acetylation is a histone modification that forms a stable epigenetic mark on chromatin for bromodomain-containing proteins to dock and in turn regulate gene expression. In order to better understand how bromodomains read the ‘histone code’ and interact with acetylated histones, we have tested the interactions of several bromodomains withi

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6

Liu, Yuxuan, Jole Fiorito, Yulissa Gonzalez, et al. "Development of First-in-Class Histone Acetyltransferase (HAT) Activators for Precision Targeting of Epigenetic Derangements in Lymphoma." Blood 132, Supplement 1 (2018): 37. http://dx.doi.org/10.1182/blood-2018-99-110447.

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Abstract Monoalleleic inactivating mutations in histone acetyltransferase (HAT) enzymes promote lymphomagenesis in germinal center derived B-cell lymphomas, follicular lymphoma (FL) and diffuse large B cell lymphoma (DLBCL), occurring in about 40% of patients. The intact wild-type allele offers an opportunity to leverage the normal enzyme to overcome the pathogenic impact of the mutated allele. We hypothesize that if inactivating mutations in HATs are critical to FL and DLBCL lymphomagenesis, then drugs capable of inducing enhanced function of the wild-type HAT allele product should be cytotox

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7

Liu, Yuxuan, Jole Fiorito, Yulissa Gonzalez, et al. "Strategy for Overcoming Crebbp and EP300 Mutations in Lymphoma: Development of First-in-Class HAT Activators." Blood 134, Supplement_1 (2019): 4068. http://dx.doi.org/10.1182/blood-2019-125983.

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Epigenetic dysregulation is a hallmark of germinal center derived B cell lymphomas. In particular, the monoallelic mutations in histone acetyltransferases (HATs), p300 and CBP are present in approximately 40% of DLBCL and FL patients. The haploinsufficiency of CBP leads to loss of MHC which contributes to both immune escape and lymphomagenesis. The intact wild-type allele offers an opportunity to leverage the normal enzyme to overcome the pathogenic impact of the mutated allele. We reported our lead compound YF2 out of a library (n=70) of HAT activators led to significant cytotoxic effect in l

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8

Imoberdorf, Rachel Maria, Irini Topalidou, and Michel Strubin. "A Role for Gcn5-Mediated Global Histone Acetylation in Transcriptional Regulation." Molecular and Cellular Biology 26, no. 5 (2006): 1610–16. http://dx.doi.org/10.1128/mcb.26.5.1610-1616.2006.

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ABSTRACT Transcriptional activators often require histone acetyltransferases (HATs) for full activity. The common explanation is that activators directly recruit HATs to gene promoters to locally hyperacetylate histones and thereby facilitate transcription complex formation. However, in addition to being targeted to specific loci, HATs such as Gcn5 also modify histones genome-wide. Here we provide evidence for a role of this global HAT activity in regulated transcription. We show that activation by direct recruitment of the transcriptional machinery neither recruits Gcn5 nor induces changes in

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9

Wang, L., C. Mizzen, C. Ying, et al. "Histone acetyltransferase activity is conserved between yeast and human GCN5 and is required for complementation of growth and transcriptional activation." Molecular and Cellular Biology 17, no. 1 (1997): 519–27. http://dx.doi.org/10.1128/mcb.17.1.519.

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Yeast and human ADA2 and GCN5 (y- and hADA2 and y- and hGCN5, respectively) have been shown to potentiate transcription in vivo and may function as adaptors to bridge physical interactions between DNA-bound activators and the basal transcriptional machinery. Recently it was shown that yGCN5 is a histone acetyltransferase (HAT), suggesting a link between enzymatic modification of nucleosomes and transcriptional activation. In this report, we demonstrate that hGCN5 is also an HAT and has the same substrate specificity as yGCN5. Since hGCN5 does not complement functional defects caused by deletio

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10

Panne, Daniel. "Chromatin recognition and regulation of the acetyltransferase CBP/p300." Acta Crystallographica Section A Foundations and Advances 70, a1 (2014): C1586. http://dx.doi.org/10.1107/s2053273314084137.

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Gene regulation in higher eukaryotes requires recruitment of the transcriptional co-activators CBP/p300 that associate with transcriptional regulators and integrate a large number of signal transduction pathways. Recruitment of CBP/p300 results in acetylation and remodeling of inhibitory chromatin. Recently we have determined the 2.8Å crystal structure of the catalytic core of p300 containing its Bromodomain, the CH2 region and HAT domain in complex with the bi-substrate inhibitor, Lys-CoA. Unexpectedly the structure reveals that the CH2 region contains a discontinuous PHD domain which is inte

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11

Jacobson, Sandra, and Lorraine Pillus. "The SAGA Subunit Ada2 Functions in Transcriptional Silencing." Molecular and Cellular Biology 29, no. 22 (2009): 6033–45. http://dx.doi.org/10.1128/mcb.00542-09.

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ABSTRACT The cellular role of the Ada2 coactivator is currently understood in the context of the SAGA histone acetyltransferase (HAT) complex, where Ada2 increases the HAT activity of Gcn5 and interacts with transcriptional activators. Here we report a new function for Ada2 in promoting transcriptional silencing at telomeres and ribosomal DNA. This silencing function is the first characterized role for Ada2 distinct from its involvement with Gcn5. Ada2 binds telomeric chromatin and the silencing protein Sir2 in vivo. Loss of ADA2 causes the spreading of Sir2 and Sir3 into subtelomeric regions

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12

Vermeulen, Michiel, Wendy Walter, Xavier Le Guezennec, et al. "A Feed-Forward Repression Mechanism Anchors the Sin3/Histone Deacetylase and N-CoR/SMRT Corepressors on Chromatin." Molecular and Cellular Biology 26, no. 14 (2006): 5226–36. http://dx.doi.org/10.1128/mcb.00440-06.

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ABSTRACT Transcription in eukaryotes is governed in part by histone acetyltransferase (HAT)- and histone deacetylase (HDAC)-containing complexes that are recruited via activators and repressors, respectively. Here, we show that the Sin3/HDAC and N-CoR/SMRT corepressor complexes repress transcription from histone H3- and/or H4-acetylated nucleosomal templates in vitro. Repression of histone H3-acetylated templates was completely dependent on the histone deacetylase activity of the corepressor complexes, whereas this activity was not required to repress H4-acetylated templates. Following deacety

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13

Alamdari, Nima, Ira J. Smith, Zaira Aversa, and Per-Olof Hasselgren. "Sepsis and glucocorticoids upregulate p300 and downregulate HDAC6 expression and activity in skeletal muscle." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 299, no. 2 (2010): R509—R520. http://dx.doi.org/10.1152/ajpregu.00858.2009.

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Muscle wasting during sepsis is in part regulated by glucocorticoids. In recent studies, treatment of cultured muscle cells in vitro with dexamethasone upregulated expression and activity of p300, a histone acetyl transferase (HAT), and reduced expression and activity of the histone deacetylases-3 (HDAC3) and -6, changes that favor hyperacetylation. Here, we tested the hypothesis that sepsis and glucocorticoids regulate p300 and HDAC3 and -6 in skeletal muscle in vivo. Because sepsis-induced metabolic changes are particularly pronounced in white, fast-twitch skeletal muscle, most experiments w

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14

Govind, Chhabi K., Sungpil Yoon, Hongfang Qiu, Sudha Govind, and Alan G. Hinnebusch. "Simultaneous Recruitment of Coactivators by Gcn4p Stimulates Multiple Steps of Transcription In Vivo." Molecular and Cellular Biology 25, no. 13 (2005): 5626–38. http://dx.doi.org/10.1128/mcb.25.13.5626-5638.2005.

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ABSTRACT Transcriptional activation by Gcn4p is dependent on the coactivators SWI/SNF, SAGA, and Srb Mediator, which are recruited by Gcn4p and stimulate assembly of the preinitiation complex (PIC) at the ARG1 promoter in vivo. We show that recruitment of all three coactivators is nearly simultaneous with binding of Gcn4p at ARG1 and is followed quickly by PIC formation and elongation by RNA polymerase II (Pol II) through the open reading frame. Despite the simultaneous recruitment of coactivators, rapid recruitment of SWI/SNF depends on the histone acetyltransferase (HAT) subunit of SAGA (Gcn

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15

Liu, Xiaohui, Marina Vorontchikhina, Yuan-Liang Wang, Francesco Faiola, and Ernest Martinez. "STAGA Recruits Mediator to the MYC Oncoprotein To Stimulate Transcription and Cell Proliferation." Molecular and Cellular Biology 28, no. 1 (2007): 108–21. http://dx.doi.org/10.1128/mcb.01402-07.

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ABSTRACT Activation of eukaryotic gene transcription involves the recruitment by DNA-binding activators of multiprotein histone acetyltransferase (HAT) and Mediator complexes. How these coactivator complexes functionally cooperate and the roles of the different subunits/modules remain unclear. Here we report physical interactions between the human HAT complex STAGA (SPT3-TAF9-GCN5-acetylase) and a “core” form of the Mediator complex during transcription activation by the MYC oncoprotein. Knockdown of the STAF65γ component of STAGA in human cells prevents the stable association of TRRAP and GCN

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16

Roelfsema, Jeroen H., and Dorien J. M. Peters. "Rubinstein–Taybi syndrome: clinical and molecular overview." Expert Reviews in Molecular Medicine 9, no. 23 (2007): 1–16. http://dx.doi.org/10.1017/s1462399407000415.

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Rubinstein–Taybi syndrome is characterised by mental retardation, growth retardation and a particular dysmorphology. The syndrome is rare, with a frequency of approximately one affected individual in 100 000 newborns. Mutations in two genes –CREBBPandEP300– have been identified to cause the syndrome. These two genes show strong homology and encode histone acetyltransferases (HATs), which are transcriptional co-activators involved in many signalling pathways. Loss of HAT activity is sufficient to account for the phenomena seen in Rubinstein–Taybi patients. Although some mutations found inCREBBP

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17

Marsh, Graham P., Sean Goggins, Darko Bosnakovski, et al. "Abstract 3841: Development of p300-targeting PROTAC degraders with enhanced selectivity and onset of degradation." Cancer Research 83, no. 7_Supplement (2023): 3841. http://dx.doi.org/10.1158/1538-7445.am2023-3841.

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Abstract CREB-binding protein (CBP, CREBBP, KAT3A) and E1A-binding protein (EP300, p300, KAT3B) are paralogous multi-domain proteins that act as chromatin regulators and transcriptional co-activators. They contain a histone acetyltransferase (HAT) domain that catalyzes the histone H3, lysine 27 acetylation (H3K27ac) mark at regulatory elements such as enhancers and promoters. Transcription factors associate with stretches of H3K27ac marks (known as ‘super-enhancer’ elements) and result in gene transcription that ultimately establishes cell identity and fate. They are implicated in cancer patho

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18

Martinez, Ernest, Vikas B. Palhan, Agneta Tjernberg, et al. "Human STAGA Complex Is a Chromatin-Acetylating Transcription Coactivator That Interacts with Pre-mRNA Splicing and DNA Damage-Binding Factors In Vivo." Molecular and Cellular Biology 21, no. 20 (2001): 6782–95. http://dx.doi.org/10.1128/mcb.21.20.6782-6795.2001.

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ABSTRACT GCN5 is a histone acetyltransferase (HAT) originally identified inSaccharomyces cerevisiae and required for transcription of specific genes within chromatin as part of the SAGA (SPT-ADA-GCN5 acetylase) coactivator complex. Mammalian cells have two distinct GCN5 homologs (PCAF and GCN5L) that have been found in three different SAGA-like complexes (PCAF complex, TFTC [TATA-binding-protein-free TAFII-containing complex], and STAGA [SPT3-TAFII31-GCN5L acetylase]). The composition and roles of these mammalian HAT complexes are still poorly characterized. Here, we present the purification a

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MEHRA-CHAUDHARY, Ritcha, Hideo MATSUI, and Rajendra RAGHOW. "Msx3 protein recruits histone deacetylase to down-regulate the Msx1 promoter." Biochemical Journal 353, no. 1 (2000): 13–22. http://dx.doi.org/10.1042/bj3530013.

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Msx1 promoter is known to be repressed by Msx1 protein [Shetty, Takahashi, Matsui, Iyengar and Raghow (1999) Biochem. J. 339, 751–758]. We show that in the transiently transfected C2C12 myoblasts, co-expression of Msx3 also causes potent repression of Msx1 promoter that can be relieved by exogenous expression of cAMP-response-element-binding protein-binding protein (CBP) and p300 in a dose-dependent manner. Co-immunoprecipitation and Western blot analyses revealed that Msx3 interacts with CBP and p300 and this interaction significantly decreases the histone acetyltransferase (HAT) activity of

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Sterner, David E., and Shelley L. Berger. "Acetylation of Histones and Transcription-Related Factors." Microbiology and Molecular Biology Reviews 64, no. 2 (2000): 435–59. http://dx.doi.org/10.1128/mmbr.64.2.435-459.2000.

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SUMMARY The state of chromatin (the packaging of DNA in eukaryotes) has long been recognized to have major effects on levels of gene expression, and numerous chromatin-altering strategies—including ATP-dependent remodeling and histone modification—are employed in the cell to bring about transcriptional regulation. Of these, histone acetylation is one of the best characterized, as recent years have seen the identification and further study of many histone acetyltransferase (HAT) proteins and their associated complexes. Interestingly, most of these proteins were previously shown to have coactiva

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La Bonte, Laura, and Darshan Sappal. "Abstract 6287: Selective CBP degradation shows superior potency and differentiated biological activity compared to small molecule inhibitors." Cancer Research 83, no. 7_Supplement (2023): 6287. http://dx.doi.org/10.1158/1538-7445.am2023-6287.

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Abstract CREB binding protein (CBP) and E1A binding protein (p300) are paralog histone acetyltransferases involved in many cellular processes via their activity as transcription factor co-activators. Dysregulation of one or both proteins has been implicated in a variety of cancers, and functional genomic screens have exhibited a bidirectional synthetic lethal relationship between the two genes in many cancer indications. Due to the high homology between CBP and p300, identification of selective chemical matter that specifically and directly targets CBP has proven challenging. Small molecule in

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Purbasari, Aprilina, Tjokorde Walmiki Samadhi, and Yazid Bindar. "The Effect of Alkaline Activator Types on Strength and Microstructural Properties of Geopolymer from Co-Combustion Residuals of Bamboo and Kaolin." Indonesian Journal of Chemistry 18, no. 3 (2018): 397. http://dx.doi.org/10.22146/ijc.26534.

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Geopolymer as a Portland cement substitute had been synthesized from alkaline activation of co-combustion residuals of bamboo and kaolin. Types of used alkaline activators were NaOH solution, KOH solution, a mixture of NaOH solution-water glass, and a mixture of KOH solution-water glass. Geopolymer with NaOH solution as activator had a compressive strength which was higher compared to geopolymer with KOH solution as an activator. However, geopolymer with NaOH solution-water glass as activator had a compressive strength which was lower compared to geopolymer with KOH solution-water glass as act

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23

Henquin, Jean-Claude, and Myriam Nenquin. "Activators of PKA and Epac Distinctly Influence Insulin Secretion and Cytosolic Ca2+ in Female Mouse Islets Stimulated by Glucose and Tolbutamide." Endocrinology 155, no. 9 (2014): 3274–87. http://dx.doi.org/10.1210/en.2014-1247.

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Abstract Amplification of insulin secretion by cAMP is mediated by protein kinase A (PKA) and exchange protein directly activated by cAMP (Epac). Using selective activators, we determined how each effector influences the cytosolic free Ca2+ concentration ([Ca2+]c) and insulin secretion in mouse islets. Alone PKA activator amplified glucose- and tolbutamide-induced insulin secretion, with a greater impact on second than first phase. Epac activator strongly amplified both phases in response to either secretagogue. Amplification was even greater when activators were combined. Although both activa

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Carpenter, Anne E., Sevinci Memedula, Matthew J. Plutz, and Andrew S. Belmont. "Common Effects of Acidic Activators on Large-Scale Chromatin Structure and Transcription." Molecular and Cellular Biology 25, no. 3 (2005): 958–68. http://dx.doi.org/10.1128/mcb.25.3.958-968.2005.

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ABSTRACT Large-scale chromatin decondensation has been observed after the targeting of certain acidic activators to heterochromatic chromatin domains. Acidic activators are often modular, with two or more separable transcriptional activation domains. Whether these smaller regions are sufficient for all functions of the activators has not been demonstrated. We adapted an inducible heterodimerization system to allow systematic dissection of the function of acidic activators, individual subdomains within these activators, and short acidic-hydrophobic peptide motifs within these subdomains. Here,

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Triwahyuningsih, Nike. "Karakteristik Kimiawi Kompos Enceng Gondok dan Jerami Hasil Dekomposisi Dengan Aktivator Alami dan Buatan." PLANTA TROPIKA: Jurnal Agrosains (Journal of Agro Science) 1, no. 1 (2021): 29–33. http://dx.doi.org/10.18196/pt.v1i1.3109.

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A research to study the chemical properties of hyacinth- and straw-compost decomposed by natural and artificial activators was conducted at the Research Field of Faculty of Agriculture, Muhammadiyah University of Yogyakarta. Cow manure was used as natural activator, while Stardec (powdered) and EM4 (liquid) as artificial ones. The treatment was arranged in 2x3 factorial completely randomized design. The hyacinth and straw organic sources were decomposed by cow manure, Stardec and EM4 activators. Organic matters were incubated for 5-6 weeks then pH, C-organic, N-total, available P and K, CEC, a

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Sabovic, M., H. R. Lijnen, D. Keber, and D. Collen. "Effect of Retraction on the Lysis of Human Clots with Fibrin Specific and Non-Fibrin Specific Plasminogen Activators." Thrombosis and Haemostasis 62, no. 04 (1989): 1083–87. http://dx.doi.org/10.1055/s-0038-1647122.

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SummaryThe effect of the serum content of human clots on their sensitivity to lysis with plasminogen activators was studied in a system composed of 125I-fibrin labeled clots immersed in buffer or in citrated plasma. The effect was studied with plasma clots before or after mechanical compression and with whole blood clots before or after retraction, using either the fibrin specific plasminogen activators recombinant tissue-type plasminogen activator (rt-PA) or recombinant single chain urokinase-type plasminogen activator (rscu-PA), and the non-fibrin specific activators recombinant two chain ur

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Nurhilal, Otong. "Pengaruh Aktivator dan Kalsinasi terhadap Luas Permukaan Arang Aktif Eceng Gondok." Jurnal Ilmu dan Inovasi Fisika 6, no. 2 (2022): 131–36. http://dx.doi.org/10.24198/jiif.v6i2.39913.

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Water hyacinth has been used as a precursor for activated charcoal with H3PO4, KOH and ZnCl2 activators. After the activation process, the activated charcoal samples were treated without calcination and calcination at a temperature of 800 oC for one hour in an Ar gas atmosphere. Each sample of activated charcoal was characterized by N2 absorption at 77 K to determine the specific surface area, specific total pore volume and pore radius formed. From the test results, it was found that the calcination had a very significant effect on the properties of activated charcoal. Calcination of activated

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Ruslinda, Yenni, Rizki Aziz, Larasati Sekar Arum, and Novita Sari. "The Effect of Activator Addition to the Compost with Biopore Infiltration Hole (BIH) Method." Jurnal Ilmu Lingkungan 19, no. 1 (2021): 53–59. http://dx.doi.org/10.14710/jil.19.1.53-59.

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The composition of organic waste reaches 59% of the total municipal solid waste in Indonesia. One way to process organic waste is composting by utilizing microorganisms to break down waste into compost. Naturally, the composting process took a long time but can be accelerated by adding microorganisms to the activator. This study analyzes the quality and quantity of compost using the Biopore Infiltration Hole (BIH) method with activator addition. Composting was duplicated in the yard area with clay soil type and water infiltration rate of 0,3 cm/hour. The BIH was made in a 10 cm diameter, a 100

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Nizevičienė, Dalia, Nora Kybartienė, and Vacius Jusas. "Analysis of Compressive Strength of Anhydrite Binder Using Full Factorial Design." Materials 16, no. 18 (2023): 6265. http://dx.doi.org/10.3390/ma16186265.

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Flue gas desulfurization gypsum (FGD gypsum) is obtained from the desulphurization of combustion gases in fossil fuel power plants. FGD gypsum can be used to produce anhydrite binder. This research is devoted to the investigation of the influence of the calcination temperature of FGD gypsum, the activators K2SO4 and Na2SO4, and their amount on the compressive strength of anhydrite binder during hydration. The obtained results showed that as the calcination temperature increased, the compressive strength of anhydrite binder decreased at its early age (up to 3 days) and increased after 28 days.

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Guo, Sheng, De Yi Huang, Ji Feng She, and Xiang Qun Liang. "Comparison Activating Ability of Three Hydrogen Peroxide Activators." Advanced Materials Research 641-642 (January 2013): 215–18. http://dx.doi.org/10.4028/www.scientific.net/amr.641-642.215.

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The bleaching efficiency of hydrogen peroxide can be promoted by using suitable activator. In our research, two methods were applied to compare the activating ability of three activators, TAED (tetraacetylethylenediamine), acetamide and dicyandiamide. The first part was hydrogen peroxide bleaching. TAED was excellent, because the brightness improvement was the maximum; the viscosity was acceptable. Acetamide was an applied activator in peroxide bleaching，for it could get same effects as TAED if the bleaching process had enough time and enough dosage. In the last part our study was about the ki

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Sappal, Darshan, Ammar Adam, Hafiz Ahmad, et al. "Abstract 6067: Identification of selective CBP degraders with robust preclinical PK, PD, efficacy and safety across solid tumor indications." Cancer Research 84, no. 6_Supplement (2024): 6067. http://dx.doi.org/10.1158/1538-7445.am2024-6067.

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Abstract CREB binding protein (CBP) and E1A binding protein (EP300) are paralog histone acetyltransferases involved in many cellular processes via their activity as transcription factor co-activators. Dysregulation of one or both proteins has been implicated in various cancer types, and functional genomic screens have revealed a bidirectional synthetic lethal relationship between these two paralogs in tumor cells. Due to the high homology between CBP and EP300, identifying selective chemical matter that selectively disrupts the activity of CBP has proven challenging. Small molecule inhibitors

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Zimmerman, Mark, Darshan Sappal, Ammar Adam, et al. "Abstract A060: Discovery of potent and selective EP300 degraders with anti-cancer activity." Molecular Cancer Therapeutics 22, no. 12_Supplement (2023): A060. http://dx.doi.org/10.1158/1535-7163.targ-23-a060.

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Abstract E1A binding protein (EP300) and CREB binding protein (CBP) are paralog histone acetyltransferases involved in many cellular processes via their activity as transcriptional co-activators. Dysregulation of one or both proteins has been implicated in various cancers, and functional genomic screens have demonstrated a bidirectional synthetic lethal relationship between the two genes in tumor cells. Due to the high homology between EP300 and CBP, identifying chemical matter that selectively targets EP300 or CBP has proven challenging. Here, we describe a potent, highly selective heterobifu

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Kirchhofer, Daniel, Mark Peek, Michael T. Lipari, Karen Billeci, Bin Fan, and Paul Moran. "Hepsin activates pro-hepatocyte growth factor and is inhibited by hepatocyte growth factor activator inhibitor-1B (HAI-1B) and HAI-2." FEBS Letters 579, no. 9 (2005): 1945–50. http://dx.doi.org/10.1016/j.febslet.2005.01.085.

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Klose, Karl E., Veronica Novik та John J. Mekalanos. "Identification of Multiple ς54-Dependent Transcriptional Activators inVibrio cholerae". Journal of Bacteriology 180, № 19 (1998): 5256–59. http://dx.doi.org/10.1128/jb.180.19.5256-5259.1998.

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ABSTRACT In the pathogenic bacterium Vibrio cholerae, the alternate sigma factor ς54 is required for expression of multiple sets of genes, including an unidentified gene(s) necessary for enhanced colonization within the host. To identify ς54-dependent transcriptional activators involved in colonization, PCR was performed with V. choleraechromosomal DNA and degenerate primers, revealing six novel and distinct coding sequences with homology to ς54-dependent activators. One sequence had high homology to the luxO gene of V. harveyi, which in that organism is involved in quorum sensing. Phenotypes

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Lemesre, Louise, Rachida Idir, and Martin Cyr. "Strength Development and Environmental Impact of Waste-Glass-Based Cements Activated with Portland Cement, NaOH, Na-Silicate or Na-Carbonates at Ambient Temperature." Materials 17, no. 20 (2024): 5097. http://dx.doi.org/10.3390/ma17205097.

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This paper presents an experimental approach to the study of the compressive strength, isothermal calorimetry and life cycle assessment (LCA) of alkali-activated pastes based on soda–lime–silica glass, established to investigate the effect of the nature and proportion of the activator. Four different activators are compared: Portland cement, sodium silicate, sodium carbonate (at four percentages by weight: 5, 10, 15 and 25 wt% relative to glass) and sodium hydroxide (3.5 wt%). Portland cement and sodium carbonate were added in dry form (powder), while sodium hydroxide (pellets) and silicate we

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Zheng, Yang, Zhi-Yuan Zhang, Yisong Liu, et al. "Preparation of Low Carbon Silicomanganese Slag-Based Alkali-Activated Materials Using Alkali-Activated Silica Waste." Buildings 14, no. 12 (2024): 3835. http://dx.doi.org/10.3390/buildings14123835.

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The utilization of silicomanganese slag (SiMnS) as a precursor for alkali-activated materials (AAMs) is considered as an efficient approach for sustainable and eco-friendly large-scale resource utilization. However, sodium silicate solutions account for more than 50% of the production costs and carbon emissions of AAMs. In this study, AAM activators were prepared by silica-containing waste (acid leaching residue of boron mud, BM-AR) and NaOH as raw materials, and were successfully substituted for commercial sodium silicate-NaOH activators. Results indicated that the NaOH dosage had a great eff

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John, Victoria H., Tim J. Dale, Emma C. Hollands, et al. "Novel 384-Well Population Patch Clamp Electrophysiology Assays for Ca2+-Activated K+ Channels." Journal of Biomolecular Screening 12, no. 1 (2006): 50–60. http://dx.doi.org/10.1177/1087057106294920.

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Planar array electrophysiology techniques were applied to assays for modulators of recombinant hIK and hSK3 Ca2+-activated K+ channels. In CHO-hIK—expressing cells, under asymmetric K+ gradients, small-molecule channel activators evoked time- and voltage-independent currents characteristic of those previously described by classical patch clamp electrophysiology methods. In single-hole (cell) experiments, the large cell-to-cell heterogeneity in channel expression rendered it difficult to generate activator concentration-response curves. However, in population patch clamp mode, in which signals

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Moon, Hyun Kyung, Jong-Eun Won, Jae Jun Ryu, and Ji Suk Shim. "The Effect of the Initiator/Activator/Accelerator Ratio on the Degree of Conversion, Film Thickness, Flow, and Cytotoxicity of Dual-Cured Self-Adhesive Resin Cements." Materials 17, no. 14 (2024): 3572. http://dx.doi.org/10.3390/ma17143572.

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Although self-adhesive resin cements are convenient and less technique-sensitive materials for dental clinicians, they exhibit a lower degree of conversion due to acidic components in their composition. Supplementation of the initiator, accelerator, and activator in self-adhesive resin cements has been suggested to compensate for the lower degree of conversion. This study aimed to evaluate the effects of different combinations of self-curing initiators, self-curing activators, and accelerators on the degree of conversion (DC) of self-adhesive resin cements. A dual-cured self-adhesive resin was

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Kahlouche, R., A. Badaoui, and M. Criado. "Fresh, hardened and durability properties of sodium carbonate-activated Algerian slag exposed to sulfate and acid attacks." Materiales de Construcción 73, no. 351 (2023): e321. http://dx.doi.org/10.3989/mc.2023.309922.

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This paper investigates the use of Na2CO3 as an alkaline activator on the durability of the alkali-activated slag (AAS) mortar toward sulfates and acids. The behavior of this binder in these aggressive environments is compared to those of slags activated with Na2SiO3 and NaOH. In addition, the setting times, workabilities, mechanical properties and drying shrinkage were evaluated. The AAS had superior workabilities, faster setting times and higher shrinkage rates than the Portland cement (PC). Increases in the activator dosages had positive effects on the mechanical strengths of the materials.

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Pratiwi, Ellyza Yohana Putri, Suhartini, and Ahmad Kamal Sudrajat. "THE EFFECT OF DIFFERENT BIO ACTIVATORS ON QUALITY COMPOST OF AGRICULTURAL WASTE." Indonesian Journal of Bioscience (IJOBI) 1, no. 1 (2023): 37–44. http://dx.doi.org/10.21831/ijobi.v1i1.105.

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This study aims to determine the effect of using various bio activators on quality compost from agricultural waste and the best bio activators to obtain good quality compost from agricultural waste. This type of research is experimental with a Completely Randomized Design (CRD). The object of this research is compost from agricultural waste added with various bio activators: Tape Yeast, Tempe Yeast, Stardec, EM-4, and M-21 Decomposer. Each treatment consisted of 3 (three) replications. This study lasted for 75 days. The quality of compost is observed by physical parameters (temperature, humidi

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Said, M. I., E. Abustam, St Rohani, and R. N. Adiatma. "Properties and cost analysis of bio-urine liquid fertilizer (BLF) from Balinese cattle on the use of bio-activators and different fermentation times." Journal of the Indonesian Tropical Animal Agriculture 45, no. 1 (2020): 47–57. http://dx.doi.org/10.14710/jitaa.45.1.47-57.

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The study was aimed to evaluate the effect of bio-activator and different fermentation time in the process of producing bio-urine liquid fertilizer (BLF) from Balinese cattle. Two types of bio-activators are used, namely (1) animal bio-activator (ABA) and (2) plant bio-activator (PBA). The time of fermentation process applied is (1) 7, (2) 14 and (3) 21 days. The research was prepared based on a Completely Randomized Design (CRD) of the factorial pattern. The data of the research were analyzed using ANOVA. The result showed that the difference of bio-activator and time of fermentation process

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Kitching, A. Richard, Stephen R. Holdsworth, Victoria A. Ploplis, et al. "Plasminogen and Plasminogen Activators Protect against Renal Injury in Crescentic Glomerulonephritis." Journal of Experimental Medicine 185, no. 5 (1997): 963–68. http://dx.doi.org/10.1084/jem.185.5.963.

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The plasminogen/plasmin system has the potential to affect the outcome of inflammatory diseases by regulating accumulation of fibrin and other matrix proteins. In human and experimental crescentic glomerulonephritis (GN), fibrin is an important mediator of glomerular injury and renal impairment. Glomerular deposition of matrix proteins is a feature of progressive disease. To study the role of plasminogen and plasminogen activators in the development of inflammatory glomerular injury, GN was induced in mice in which the genes for these proteins had been disrupted by homologous recombination. De

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Okic-Djordjevic, Ivana, Tamara Kukolj, Hristina Obradovic, et al. "Interleukin-17 modulates uPA and MMP2 expression in human periodontal ligament mesenchymal stem cells: Involvement of the ERK1/2 MAPK pathway." Archives of Biological Sciences 74, no. 1 (2022): 15–24. http://dx.doi.org/10.2298/abs210929048o.

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Periodontal disease is a chronic infection of periodontal tissue characterized by extracellular matrix (ECM) degradation due to increased expression of plasminogen activators and matrix metalloproteinases (MMPs) and various proinflammatory cytokines, including interleukin (IL)-17. Successful regeneration of damaged periodontal tissues depends on the proper functionality of periodontal ligament mesenchymal stem cells (PDLMSCs), especially the production of extracellular matrix proteases. We investigated the influence of IL-17 on ECM remodeling through modulation of urokinasetype plasminogen act

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Bae, Nahee, Hye-Jee Park, Hanbi Park, Minyoung Kim, Eunsoo Do, and Sang-Wook Han. "Elucidating Functions of FleQ in Xanthomonas oryzae pv. oryzae by Comparative Proteomic and Phenotypic Analyses." International Journal of Molecular Sciences 19, no. 10 (2018): 3038. http://dx.doi.org/10.3390/ijms19103038.

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To acclimate to different environments, gene expression has to be controlled using diverse transcriptional activators. FleQ activates σ54-dependent transcription initiation and regulates flagellar biosynthesis and other mechanisms in several bacteria. Xanthomonas oryzae pv. oryzae (Xoo), which is a causal agent of bacterial leaf blight on rice, lacking FleQ loses swimming motility and virulence is not altered. However, other biological mechanisms related with FleQ in Xoo are unknown. In this study, we generated the FleQ-overexpressing strain, Xoo(FleQ), and knockout mutant, XooΔfleQ. To predic

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Fitriani, Fitriani. "PEMURNIAN MINYAK GORENG BEKAS MENGGUNAKAN ADSORBEN BIJI ALPUKAT TERAKTIVASI." Jurnal Pendidikan Matematika dan IPA 9, no. 2 (2018): 65. http://dx.doi.org/10.26418/jpmipa.v9i2.26770.

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Abstract This research had been conducted in the use of avocado seed powder (Persea americana Mill) as an adsorbent to reduce peroxide and free fatty acids of the used cooking oil. The aim of this research was to determine the best activator of avocado seed powder as an adsorbent to reduce peroxide and free fatty acids of the used cooking oil. This research used the variation of activators, consist of hydrochloric acid (HCl), citric acid (C6H8O7), sodium chloride (NaCl) and sodium hydrogen phosphate (Na2HPO4) solutions. The result showed that the best activator of avocado seed powder by HCl wh

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Zimmerman, Mark, Ammar Adam, Hafiz Ahmad, et al. "Abstract 6064: Discovery of potent and selective EP300 degraders with anti-cancer activity." Cancer Research 84, no. 6_Supplement (2024): 6064. http://dx.doi.org/10.1158/1538-7445.am2024-6064.

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Abstract E1A binding protein (EP300) and CREB binding protein (CBP) are paralog histone acetyltransferases involved in many cellular processes via their activity as transcriptional co-activators. Dysregulation of one or both proteins has been implicated in various cancers, and functional genomic screens have demonstrated a bidirectional synthetic lethal relationship between the two genes in tumor cells. Due to the high homology between EP300 and CBP, identifying chemical matter that selectively targets EP300 or CBP has proven challenging. Here, we describe a potent, highly selective heterobifu

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47

Sasaki, K., S. Moriyama, Y. Tanaka, H. Sumi, N. Toki, and KC Robbins. "The transport of 125I-labeled human high molecular weight urokinase across the intestinal tract in a dog model with stimulation of synthesis and/or release of plasminogen activators." Blood 66, no. 1 (1985): 69–75. http://dx.doi.org/10.1182/blood.v66.1.69.69.

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Abstract In an attempt to elucidate the mechanism of fibrinolytic enhancement by orally administered urokinase, studies on the intestinal transport of urokinase were carried out, using 125I-labeled human high mol wt urokinase, administered intraduodenally in the experimental dog model with a saphenous vein thrombus. Using the plasma sample obtained from blood 45 minutes after intraduodenal administration of the urokinase, protein fractions were isolated by a sequential two-step affinity chromatography method, first with [N alpha-(epsilon-aminocaproyl)-DL- homoarginine hexylester]-Sepharose fol

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48

Sasaki, K., S. Moriyama, Y. Tanaka, H. Sumi, N. Toki, and KC Robbins. "The transport of 125I-labeled human high molecular weight urokinase across the intestinal tract in a dog model with stimulation of synthesis and/or release of plasminogen activators." Blood 66, no. 1 (1985): 69–75. http://dx.doi.org/10.1182/blood.v66.1.69.bloodjournal66169.

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In an attempt to elucidate the mechanism of fibrinolytic enhancement by orally administered urokinase, studies on the intestinal transport of urokinase were carried out, using 125I-labeled human high mol wt urokinase, administered intraduodenally in the experimental dog model with a saphenous vein thrombus. Using the plasma sample obtained from blood 45 minutes after intraduodenal administration of the urokinase, protein fractions were isolated by a sequential two-step affinity chromatography method, first with [N alpha-(epsilon-aminocaproyl)-DL- homoarginine hexylester]-Sepharose followed by

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Lluı́s, Frederic, Josep Roma, Mònica Suelves, et al. "Urokinase-dependent plasminogen activation is required for efficient skeletal muscle regeneration in vivo." Blood 97, no. 6 (2001): 1703–11. http://dx.doi.org/10.1182/blood.v97.6.1703.

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Plasminogen activators urokinase-type plasminogen activator (uPA) and tissue-type plasminogen activator (tPA) are extracellular proteases involved in various tissue remodeling processes. A requirement for uPA activity in skeletal myogenesis was recently demonstrated in vitro. The role of plasminogen activators in skeletal muscle regeneration in vivo in wild-type, uPA-deficient, and tPA-deficient mice is investigated here. Wild-type and tPA−/− mice completely repaired experimentally damaged skeletal muscle. In contrast, uPA−/− mice had a severe regeneration defect, with decreased recruitment of

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van Hinsbergh, VW, RM Bertina, A. van Wijngaarden, NH van Tilburg, JJ Emeis, and F. Haverkate. "Activated protein C decreases plasminogen activator-inhibitor activity in endothelial cell-conditioned medium." Blood 65, no. 2 (1985): 444–51. http://dx.doi.org/10.1182/blood.v65.2.444.bloodjournal652444.

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Confluent cultures of endothelial cells from human umbilical cord were used to study the effect of activated human protein C (APC) on the production of plasminogen activators, plasminogen activator-inhibitor, and factor VIII-related antigen. Addition of APC to the cells in a serum-free medium did not affect the production of tissue-type plasminogen activator (t-PA) or factor VIII-related antigen; under all measured conditions, no urokinase activity was found. However, less plasminogen activator-inhibitor activity accumulated in the conditioned medium in the presence of APC. This decrease was d

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