Detalhe da pesquisa
1.
A selective small-molecule STAT5 PROTAC degrader capable of achieving tumor regression in vivo.
Nat Chem Biol
; 19(6): 703-711, 2023 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-36732620
2.
Inhibitors of Mycobacterium tuberculosis DosRST signaling and persistence.
Nat Chem Biol
; 13(2): 218-225, 2017 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-27992879
3.
Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Bioorg Med Chem Lett
; 28(9): 1507-1515, 2018 05 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29627263
4.
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.
Bioorg Med Chem Lett
; 28(10): 1972-1980, 2018 06 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29650289
5.
Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo.
J Virol
; 88(19): 11199-214, 2014 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-25031353
6.
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
Bioorg Med Chem Lett
; 23(13): 3826-32, 2013 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-23707258
7.
Discovery of a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia.
J Med Chem
; 66(4): 2717-2743, 2023 02 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-36735833
8.
Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
J Med Chem
; 66(13): 8822-8843, 2023 07 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-37382562
9.
Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer.
J Med Chem
; 66(18): 13280-13303, 2023 Sep 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-37683104
10.
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
Bioorg Med Chem Lett
; 21(20): 6094-9, 2011 Oct 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21903392
11.
Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
J Med Chem
; 64(18): 13487-13509, 2021 09 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-34473519
12.
Discovery of M-1121 as an Orally Active Covalent Inhibitor of Menin-MLL Interaction Capable of Achieving Complete and Long-Lasting Tumor Regression.
J Med Chem
; 64(14): 10333-10349, 2021 07 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-34196551
13.
Research into selective biomarkers of erythrocyte exposure to organophosphorus compounds.
Anal Biochem
; 392(2): 155-61, 2009 Sep 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19497294
14.
Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J Med Chem
; 59(8): 3793-807, 2016 04 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-27050625
15.
LigScore: a novel scoring function for predicting binding affinities.
J Mol Graph Model
; 23(5): 395-407, 2005 Apr.
Artigo
em Inglês
| MEDLINE | ID: mdl-15781182
16.
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
J Med Chem
; 56(11): 4758-63, 2013 Jun 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-23679862
17.
MScreen: an integrated compound management and high-throughput screening data storage and analysis system.
J Biomol Screen
; 17(8): 1080-7, 2012 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-22706349
18.
Small molecule screening identifies regulators of the transcription factor ΔFosB.
ACS Chem Neurosci
; 3(7): 546-56, 2012 Jul 18.
Artigo
em Inglês
| MEDLINE | ID: mdl-22860224
19.
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
J Med Chem
; 55(8): 3814-26, 2012 Apr 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-22452568
20.
Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity.
Biochem Pharmacol
; 82(4): 341-9, 2011 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21621524