Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains
about
Modulation of Protein-Protein Interactions for the Development of Novel TherapeuticsAcetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase InhibitorsTargeting bromodomains: epigenetic readers of lysine acetylationDiscovery and optimization of small-molecule ligands for the CBP/p300 bromodomainsTargeting BET bromodomains for cancer treatmentSegmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase ADrug Discovery Targeting Bromodomain-Containing Protein 4.Privileged diazepine compounds and their emergence as bromodomain inhibitors.Inhibition of BRD4 attenuates tumor cell self-renewal and suppresses stem cell signaling in MYC driven medulloblastoma.Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversificationSmall-molecule inhibitors of protein-protein interactions: progressing toward the reality.Epigenetic drugs against cancer: an evolving landscape.Inducible in vivo silencing of Brd4 identifies potential toxicities of sustained BET protein inhibitionMolecularly targeted therapies in non-small-cell lung cancer annual update 2014Bromodomain inhibitors regulate the C9ORF72 locus in ALSTargeting protein-protein interactions in hematologic malignancies: still a challenge or a great opportunity for future therapies?Impressive Response to Dose-Dense Chemotherapy in a Patient with NUT Midline Carcinoma.The Bromodomain protein BRD4 controls HOTAIR, a long noncoding RNA essential for glioblastoma proliferation.BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell.Small molecules, big targets: drug discovery faces the protein-protein interaction challenge.Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk.BET inhibition as a new strategy for the treatment of gastric cancer.Potent and selective bivalent inhibitors of BET bromodomains.CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancerBET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in miceStructure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.ERK5 kinase activity is dispensable for cellular immune response and proliferation.Comparative drug screening in NUT midline carcinoma.Phenotypic screening and fragment-based approaches to the discovery of small-molecule bromodomain ligands.Bromodomains and their pharmacological inhibitors.Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11.MLL leukemia and future treatment strategies.Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb FamilyInhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence.Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014).Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.Progress in the Development of non-BET Bromodomain Chemical Probes.BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.Transcriptional Elongation of HSV Immediate Early Genes by the Super Elongation Complex Drives Lytic Infection and Reactivation from Latency.Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
P2860
Q26775356-4A0F174D-6EF9-41C1-B181-A4FC688F6499Q27681896-517D7030-4AF2-4FC2-BED9-E160FAF0DB4BQ28238635-50D3AE30-375D-4B77-BF22-5239D7897B99Q28242369-3B0340CD-267D-4841-90AE-4F50AA15AD29Q28263519-75E6AE59-2F94-440E-A30C-70B588BCEA52Q28551713-D50DC968-6ED8-4F54-98F3-729F10CD577AQ30352390-253AF1D5-C900-4592-A12B-39FFB4C28176Q33671341-DF72713F-1E95-4280-AE5B-17486E21A4AAQ33756997-8B6043DD-9776-4050-8D69-B6B64BD12E3DQ34207033-D62439E6-D5E5-40B8-BB18-1EF1A4E624FBQ34263719-DDCF7B32-0F28-4733-9CE0-8641B86C1410Q34431964-2D8F740A-6751-4C3C-92E3-98A24DA92930Q34522818-187514CE-1EC0-4551-B5BE-CF5240A1ECAFQ35136424-AD50295D-AD7E-41F0-860C-2B1D14CB8055Q35670978-E503E39C-B1EA-4788-AF50-552FC1073E64Q35687836-0A9D7DE9-C960-47E3-BEEC-80D86E7DEA3EQ35821531-9E2CC309-2534-4DA5-A88A-2A7122618D63Q35846001-6851BB44-2812-4FA6-BEF4-C346AF88521FQ35967957-C2DA6D40-915C-4598-AA21-0260359C5914Q35981250-9100595E-DF45-4B59-88BB-BCAB6913C466Q36012341-08EECE7E-E2EA-46E3-B573-1052FF14560BQ36040347-9AD11BA6-BFB0-4253-A098-03FE05ACC92FQ36172945-E53790FA-2B86-4326-BBFB-83CB7E5CB1EDQ36515055-F6A108B7-F2B7-4FB0-B845-E9BC1B86E45BQ36575895-B92684DE-BC3F-4ED5-A045-644FA7576621Q36586506-AA4D0175-0D5A-4EAE-9D7E-99242CFB6C42Q37369392-11419DCD-DBC8-4526-94FD-857B201CB534Q37632187-231FB2DF-ECF5-4EC1-BF48-1CD3229C7816Q38182138-6A1A0BB3-F5FC-4B6D-8175-5E2052122D86Q38185355-59CA4D3B-6242-4480-96D7-CD2BF300154FQ38233723-AE6ACAC4-5DAE-481C-B8B1-9794E9A1EFBBQ38367735-ED50F17E-7EB0-4E60-86B4-2E8C647B27A4Q38434032-E395407A-C83D-45BC-8865-06D3FFFA4F51Q38542092-9B9A17D6-80BD-4EA8-988E-119D6326CA10Q38547122-76B49CF4-3957-48D0-996B-0AAC13660661Q38668661-8A615505-C420-47DB-8F00-206BF15B87B2Q38691377-829DF980-0D66-4280-BD46-274E3DBFBD6FQ38702568-789A1118-045F-4A45-B642-9A5212AA231AQ38707836-203F0AA8-4F71-4147-A85A-08E784D2D708Q38710711-43BA67A2-D126-4F1A-A755-0F87CD842294
P2860
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains
description
2013 nî lūn-bûn
@nan
2013 թուականի Հոկտեմբերին հրատարակուած գիտական յօդուած
@hyw
2013 թվականի հոտեմբերին հրատարակված գիտական հոդված
@hy
2013年の論文
@ja
2013年学术文章
@wuu
2013年学术文章
@zh-cn
2013年学术文章
@zh-hans
2013年学术文章
@zh-my
2013年学术文章
@zh-sg
2013年學術文章
@yue
name
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@ast
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@en
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@nl
type
label
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@ast
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@en
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@nl
prefLabel
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@ast
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@en
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@nl
P2093
P3181
P356
P1476
Discovery of epigenetic regula ...... ibitor of the BET bromodomains
@en
P2093
Alain Daugan
Andrea C Haynes
Antonia Lewis
Catherine A Clément
Chun-wa Chung
Edwige Nicodème
Iain J Uings
Jacqueline E Mordaunt
Jason Witherington
Jean-Marie Brusq
P304
P3181
P356
10.1021/JM401088K
P407
P577
2013-10-10T00:00:00Z