Detalhe da pesquisa
1.
Identification of highly selective SIK1/2 inhibitors that modulate innate immune activation and suppress intestinal inflammation.
Proc Natl Acad Sci U S A
; 121(1): e2307086120, 2024 Jan 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-38147543
2.
Potent Phenylpyridine and Oxodihydrofuran Inhibitors of Cyclooxygenase-2: Optimization toward a Long Residence Time with Balanced Internal Energetics.
Biochemistry
; 60(31): 2407-2418, 2021 08 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-34293856
3.
Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor.
J Pharmacol Exp Ther
; 372(3): 339-353, 2020 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-31818916
4.
Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1.
Bioorg Med Chem Lett
; 28(6): 1043-1049, 2018 04 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29486970
5.
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
Bioorg Med Chem Lett
; 26(1): 197-202, 2016 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26597534
6.
Small molecule-mediated allosteric activation of the base excision repair enzyme 8-oxoguanine DNA glycosylase and its impact on mitochondrial function.
Sci Rep
; 12(1): 14685, 2022 08 29.
Artigo
em Inglês
| MEDLINE | ID: mdl-36038587
7.
Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency.
Biochemistry
; 50(32): 6867-78, 2011 Aug 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-21728345
8.
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
J Med Chem
; 64(15): 11570-11596, 2021 08 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-34279934
9.
Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1.
Bioorg Med Chem Lett
; 20(16): 4878-81, 2010 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20637614
10.
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
J Med Chem
; 50(24): 5912-25, 2007 Nov 29.
Artigo
em Inglês
| MEDLINE | ID: mdl-17985862
11.
Modulation of cyclin-dependent kinase 4 by binding of magnesium (II) and manganese (II).
Biophys Chem
; 95(1): 79-90, 2002 Jan 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-11880175
12.
Biochemical characterization and in vitro activity of AZ513, a noncovalent, reversible, and noncompetitive inhibitor of fatty acid amide hydrolase.
Eur J Pharmacol
; 667(1-3): 74-9, 2011 Sep 30.
Artigo
em Inglês
| MEDLINE | ID: mdl-21645511
13.
Neurokinin-3 receptor-specific antagonists talnetant and osanetant show distinct mode of action in cellular Ca2+ mobilization but display similar binding kinetics and identical mechanism of binding in ligand cross-competition.
Mol Pharmacol
; 71(3): 902-11, 2007 Mar.
Artigo
em Inglês
| MEDLINE | ID: mdl-17172464
14.
The mechanism of gamma-secretase: multiple inhibitor binding sites for transition state analogs and small molecule inhibitors.
J Biol Chem
; 278(31): 28968-75, 2003 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-12719412
15.
Mechanism of gamma-secretase cleavage activation: is gamma-secretase regulated through autoinhibition involving the presenilin-1 exon 9 loop?
Biochemistry
; 43(20): 6208-18, 2004 May 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-15147205
16.
Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepines.
J Biol Chem
; 277(35): 31499-505, 2002 Aug 30.
Artigo
em Inglês
| MEDLINE | ID: mdl-12072428