Sgc-cbp30 mechanism
Web23 Apr 2024 · The first inhibitor developed for CBP/p300, SGC-CBP30, exhibited potent activity for BRDs in these two HATs ( KD: 21 and 38 nM, respectively), retaining however significant BET affinity, which... WebThe SGC recently reported their parallel efforts to create a se-lective CBP BRD inhibitor, which culminated in the discovery of SGC-CBP30 (40-fold selective by ITC) (Hay et al., 2014). Crystal structures of SGC-CBP30 with BRD4 and CBP are almost iden-tical to those with BDOIA383, and the R1173 cation-p interac-
Sgc-cbp30 mechanism
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Web11 Feb 2024 · This strategy also appeared to be more broadly applicable as SGC-CBP30 could re-sensitize two resistant HMCLs with low but detectable CRBN expression to … WebSGC-CBP30 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC 50 = 0.021 and 0.038 μM, respectively). SGC-CBP30 has …
WebDownload scientific diagram Comparison of CBP30 binding to the p300 and CBP bromodomains. (A) Binding of CBP30 to p300. The inhibitor and most important interacting side chains are shown in ball ... Web22 Dec 2024 · We evaluated p300 in vivousing tamoxifen-inducible, cholangiocyte-selective, p300 knockout (KO) coupled with bile duct ligation (BDL) and MdrKO mice treated with …
Web4 Jul 2024 · SGC-CBP30 increased the expression of MHC class I polypeptide-related sequence A (MICA; a ligand of natural killer (NK) cells that is expressed in multiple myeloma) and promoted NK-mediated ... Web11 Apr 2024 · P300 and CREB-binding protein (CBP) are two paralogs with strong histone acetylsinotransferase (HAT) activity. Under hypoxic conditions, p300 and CBP can interact with HIF-1α or HIF-2α as coactivators to regulate gene expression by their histone acetylation activity over a few HIF target promoters [ 6 ].
Web5 Jan 2016 · SGC-CBP30 and I-CBP112 are chemically distinct tool compounds with selective affinity for the bromodomains of CBP/EP300 over other bromodomains in this protein family. Independent of CBP/EP300, the bromodomains with the highest affinity for these molecules is the BET bromodomain family ( Hay et al., 2014 ).
Web8 Apr 2024 · Fig. 1: A chromatin-focused chemical screen identifies CBP/EP300 bromodomain inhibitors as enhancers of reprogramming. a, Design of the chemical screen. dH1f cells were transduced with lentiviral... htl maturaWebThe cAMP-responsive element-binding protein (CREB), a transacting factor of the CRE, is also activated by NS3 or ZIKV. Furthermore,a specific inhibitor of CREB, i.e. SGC-CBP30, reduced ZIKV-induced CCN1 up-regulation and ZIKV replication. htl mödling campus mWebEpigenetic mechanisms have been shown to be crucial mediators of fibrotic gene expression in a wide range of fibrotic disorders , including cardiac fibrosis , liver ... (0.5 µM) and SGC-CBP30 (2.5 µM) inhibition of the H3K27ac mark at promotor proximal regions of ACTA2 (E) and COL1A1 (F) in patient-derived myofibroblasts. Data are ... htl rankweil maturaball 2022WebSGC-CBP30 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC 50 = 0.021 and 0.038 μM, respectively). SGC-CBP30 has little activity against other bromodomains at concentrations up to 1 mM. htl salzburg maturaball 2022Web2 Feb 2024 · In the present study, we demonstrated that inhibition of CBP bromodomain at 8 h following the onset of sepsis by the selective and potent inhibitor SGC-CBP30 significantly increased the survival rate of mice with severe sepsis, at least in part, through a mechanism that involves expression, active release, and the pro-inflammatory activity of HMGB1. htl rankweil maturaballWebSGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first … htl ungargasse anmeldungWeb10 Aug 2015 · CBP30 is a selective and potent inhibitor of CBP/p300. ( A) Chemical structure of CBP30. ( B) Temperature shift data covering 45 human bromodomains. Screened … htluk.co.uk