Detalhe da pesquisa
1.
TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism.
Proc Natl Acad Sci U S A
; 116(51): 26008-26019, 2019 12 17.
Artigo
Inglês
| MEDLINE | ID: mdl-31796582
2.
Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs.
Toxicol Pathol
; 48(3): 465-480, 2020 04.
Artigo
Inglês
| MEDLINE | ID: mdl-32124659
3.
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Bioorg Med Chem Lett
; 28(1): 15-23, 2018 01 01.
Artigo
Inglês
| MEDLINE | ID: mdl-29169673
4.
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition.
J Biol Chem
; 291(25): 13014-27, 2016 Jun 17.
Artigo
Inglês
| MEDLINE | ID: mdl-27056325
5.
Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Bioorg Med Chem Lett
; 27(18): 4370-4376, 2017 09 15.
Artigo
Inglês
| MEDLINE | ID: mdl-28830649
6.
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Bioorg Med Chem Lett
; 27(15): 3534-3541, 2017 08 01.
Artigo
Inglês
| MEDLINE | ID: mdl-28606761
7.
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.
Bioorg Med Chem Lett
; 25(21): 4728-4732, 2015 Nov 01.
Artigo
Inglês
| MEDLINE | ID: mdl-26338362
8.
A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors.
J Immunol
; 191(5): 2205-16, 2013 Sep 01.
Artigo
Inglês
| MEDLINE | ID: mdl-23894201
9.
Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.
Bioorg Med Chem Lett
; 24(11): 2448-52, 2014 Jun 01.
Artigo
Inglês
| MEDLINE | ID: mdl-24767842
10.
Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.
Bioorg Med Chem Lett
; 24(18): 4546-4552, 2014 Sep 15.
Artigo
Inglês
| MEDLINE | ID: mdl-25139565
11.
Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.
Bioorg Med Chem Lett
; 23(11): 3149-53, 2013 Jun 01.
Artigo
Inglês
| MEDLINE | ID: mdl-23623490
12.
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
ACS Med Chem Lett
; 14(9): 1179-1187, 2023 Sep 14.
Artigo
Inglês
| MEDLINE | ID: mdl-37736184
13.
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
J Med Chem
; 65(16): 11177-11186, 2022 08 25.
Artigo
Inglês
| MEDLINE | ID: mdl-35930799
14.
A new regulatory switch in a JAK protein kinase.
Proteins
; 79(2): 393-401, 2011 Feb.
Artigo
Inglês
| MEDLINE | ID: mdl-21117080
15.
A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists.
ACS Med Chem Lett
; 12(8): 1230-1237, 2021 Aug 12.
Artigo
Inglês
| MEDLINE | ID: mdl-34413952
16.
Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.
J Med Chem
; 64(7): 3843-3869, 2021 04 08.
Artigo
Inglês
| MEDLINE | ID: mdl-33749283
17.
Regulation of Tumor-Associated Myeloid Cell Activity by CBP/EP300 Bromodomain Modulation of H3K27 Acetylation.
Cell Rep
; 27(1): 269-281.e4, 2019 04 02.
Artigo
Inglês
| MEDLINE | ID: mdl-30943407
18.
CBP/p300 Drives the Differentiation of Regulatory T Cells through Transcriptional and Non-Transcriptional Mechanisms.
Cancer Res
; 79(15): 3916-3927, 2019 08 01.
Artigo
Inglês
| MEDLINE | ID: mdl-31182547
19.
Enhancer Activity Requires CBP/P300 Bromodomain-Dependent Histone H3K27 Acetylation.
Cell Rep
; 24(7): 1722-1729, 2018 08 14.
Artigo
Inglês
| MEDLINE | ID: mdl-30110629
20.
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
J Med Chem
; 61(20): 9301-9315, 2018 10 25.
Artigo
Inglês
| MEDLINE | ID: mdl-30289257