Charles M. Rice
2020年获得诺贝尔生理学或医学奖
- Nat Commun, 2020, 11(1):1677
- bioRxiv, 2020, 2020.10.09.334128
- bioRxiv, 2020, 2020.01.20.910927
- Viruses, 2019, 11(11)E1039
- Cell Rep, 2018, 25(4):833-840.e3
- Cell, 2018, 172(3):423-438.e25
- Gastroenterology, 2017, 153(2):566-578.e5
- Gastroenterology, 2016, 150(1):82-85.e4
- Antimicrob, 2016, 60(6):3786-93
- Nature, 2015, 524(7566):471-5
- Antimicrob, 2015, 59(6):3482-92
- J Virol, 2014, 88(20):12098-111
- Antimicrob, 2014, 58(9):5386-94
- J Virol, 2013, 87(13):7593-607
- Nature, 2013, 501(7466):237-41
- Nature, 2013, 99(1):6-11
- Antimicrob, 2012, 56(10):5365-73
William G. Kaelin Jr
2019年获得诺贝尔生理学或医学奖
Peter J. Ratcliffe
2019年获得诺贝尔生理学或医学奖
Gregg L. Semenza
2019年获得诺贝尔生理学或医学奖
Aziz Sancar
2015年获得诺贝尔化学奖
G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with IC50 of 10.2 nM.
TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.
KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
Mizagliflozin is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.
Guadecitabine (SGI-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.
CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
INT-777 (S-EMCA) is a novel potent and selective TGR5 agonist with EC50 values of 0.18 μM, 3.9 μM and 1.45 μM for WT TGR5, TGR5(N76A) and TGR5(Y89F) respectively.
BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).
