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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation 期刊论文
, 2020, 卷号: 368, 期号: 6489
作者:  Gilan O.;  Rioja I.;  Knezevic K.;  Bell M.J.;  Yeung M.M.;  Harker N.R.;  Lam E.Y.N.;  Chung C.;  Bamborough P.;  Petretich M.;  Urh M.;  Atkinson S.J.;  Bassil A.K.;  Roberts E.J.;  Vassiliadis D.;  Burr M.L.;  Preston A.G.S.;  Wellaway C.;  Werner T.;  Gray J.R.;  Michon A.-M.;  Gobbetti T.;  Kumar V.;  Soden P.E.;  Haynes A.;  Vappiani J.;  Tough D.F.;  Taylor S.;  Dawson S.-J.;  Bantscheff M.;  Lindon M.;  Drewes G.;  Demont E.H.;  Daniels D.L.;  Grandi P.;  Prinjha R.K.;  Dawson M.A.
收藏  |  浏览/下载：48/0  |  提交时间：2020/07/28
7 (3,5 dimethyl 4 isoxazolyl) 1,3 dihydro 8 methoxy 1 [1 (2 pyridinyl)ethyl] 2h imidazo[4,5 c]quinolin 2 one  apremilast  bromodomain and extraterminal domain protein 1  bromodomain and extraterminal domain protein 2  bromodomain inhibitor  gsk 046  gsk 620  gsk 778  transcription factor  unclassified drug  cancer  drug  gene expression  immune response  inhibitor  physiological response  acute myeloid leukemia  animal experiment  animal model  animal tissue  antibody response  antineoplastic activity  antiproliferative activity  apoptosis  Article  binding affinity  controlled study  crystal structure  drug design  drug efficacy  drug protein binding  drug selectivity  drug specificity  drug structure  drug targeting  gene expression  high throughput screening  human  human cell  IC50  immunomodulation  in vivo study  inflammation  K-562 cell line  malignant neoplasm  MDA-MB-453 cell line  MOLM-13 cell line  mouse  nonhuman  priority journal  psoriasis  
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved a-ketoamide inhibitors 期刊论文
, 2020, 卷号: 368, 期号: 6489
作者:  Zhang L.;  Lin D.;  Sun X.;  Curth U.;  Drosten C.;  Sauerhering L.;  Becker S.;  Rox K.;  Hilgenfeld R.
收藏  |  浏览/下载：42/0  |  提交时间：2020/07/28
alanine  alpha ketoamide inhibitor  antivirus agent  isoleucine  leucine  proteinase  Severe acute respiratory syndrome coronavirus 2 main protease  threonine  unclassified drug  crystal structure  drug  enzyme  enzyme activity  inhibitor  reaction kinetics  amino acid sequence  animal cell  animal experiment  animal tissue  antiviral activity  Article  catalysis  catalytic efficiency  controlled study  crystal structure  dimerization  dissociation constant  drug clearance  drug design  drug distribution  drug half life  drug potency  drug protein binding  drug solubility  drug structure  EC50  enzyme inhibition  human  human cell  hydrogen bond  hydrophobicity  IC50  maximum concentration  mean residence time  metabolic stability  mouse  nonhuman  priority journal  protein structure  RNA replication  SARS coronavirus  Severe acute respiratory syndrome coronavirus 2  viral tropism  virus inhibition  Coronavirus  SARS coronavirus