Detalhe da pesquisa
1.
Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.
Cell
; 178(4): 949-963.e18, 2019 08 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-31353221
2.
Targeted degradation via direct 26S proteasome recruitment.
Nat Chem Biol
; 19(1): 55-63, 2023 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-36577875
3.
USP7 small-molecule inhibitors interfere with ubiquitin binding.
Nature
; 550(7677): 534-538, 2017 10 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-29045385
4.
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer.
Bioorg Med Chem Lett
; 50: 128335, 2021 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-34425201
5.
Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).
Bioorg Med Chem Lett
; 30(4): 126907, 2020 02 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31902710
6.
Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.
Bioorg Med Chem Lett
; 29(4): 674-680, 2019 02 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30522953
7.
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Bioorg Med Chem Lett
; 29(16): 2090-2093, 2019 08 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31311734
8.
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Bioorg Med Chem Lett
; 29(7): 905-911, 2019 04 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-30732944
9.
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
J Med Chem
; 65(21): 14721-14739, 2022 11 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-36279149
10.
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.
J Med Chem
; 64(5): 2534-2575, 2021 03 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-33596065
11.
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
J Med Chem
; 64(16): 11841-11856, 2021 08 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-34251202
12.
Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.
J Med Chem
; 64(5): 2576-2607, 2021 03 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-33596073
13.
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.
ACS Med Chem Lett
; 11(6): 1342-1347, 2020 Jun 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-32551022
14.
Antibody Conjugation of a Chimeric BET Degrader Enables inâ vivo Activity.
ChemMedChem
; 15(1): 17-25, 2020 01 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-31674143
15.
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.
J Med Chem
; 60(24): 10056-10070, 2017 12 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-29166018
16.
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
J Med Chem
; 59(23): 10549-10563, 2016 12 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-27682507
17.
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
J Med Chem
; 57(3): 921-36, 2014 Feb 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-24354345
18.
A simple high-content cell cycle assay reveals frequent discrepancies between cell number and ATP and MTS proliferation assays.
PLoS One
; 8(5): e63583, 2013.
Artigo
em Inglês
| MEDLINE | ID: mdl-23691072
19.
Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.
ACS Med Chem Lett
; 4(1): 85-90, 2013 Jan 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-24900567
20.
Ser1292 autophosphorylation is an indicator of LRRK2 kinase activity and contributes to the cellular effects of PD mutations.
Sci Transl Med
; 4(164): 164ra161, 2012 Dec 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-23241745