Detalhe da pesquisa
1.
NOTUM from Apc-mutant cells biases clonal competition to initiate cancer.
Nature
; 594(7863): 430-435, 2021 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-34079124
2.
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.
Bioorg Med Chem Lett
; 30(3): 126751, 2020 02 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-31862412
3.
New approaches for the treatment of Alzheimer's disease.
Bioorg Med Chem Lett
; 29(2): 125-133, 2019 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30501965
4.
An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent.
Beilstein J Org Chem
; 15: 2790-2797, 2019.
Artigo
em Inglês
| MEDLINE | ID: mdl-31807213
5.
UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.
Antimicrob Agents Chemother
; 62(9)2018 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-29941635
6.
Regioselective and enantiospecific synthesis of the HSP co-inducer arimoclomol from chiral glycidyl derivatives.
Org Biomol Chem
; 15(46): 9794-9799, 2017 Nov 29.
Artigo
em Inglês
| MEDLINE | ID: mdl-29159344
7.
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Proc Natl Acad Sci U S A
; 111(35): 12853-8, 2014 Sep 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-25136132
8.
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms.
Bioorg Med Chem Lett
; 26(18): 4518-4522, 2016 09 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27485386
9.
Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".
Antimicrob Agents Chemother
; 62(11)2018 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-30355750
10.
Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity.
Eur J Med Chem
; 251: 115132, 2023 May 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-36934521
11.
Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step.
RSC Adv
; 12(41): 26497-26503, 2022 Sep 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-36275171
12.
Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity.
J Med Chem
; 65(1): 562-578, 2022 01 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-34939789
13.
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
J Med Chem
; 65(10): 7212-7230, 2022 05 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-35536179
14.
Structural Analysis and Development of Notum Fragment Screening Hits.
ACS Chem Neurosci
; 13(13): 2060-2077, 2022 07 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-35731924
15.
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Bioorg Med Chem Lett
; 21(9): 2715-20, 2011 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21195614
16.
Small-molecule inhibitors of carboxylesterase Notum.
Future Med Chem
; 13(11): 1001-1015, 2021 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-33882714
17.
Changing the HTS Paradigm: AI-Driven Iterative Screening for Hit Finding.
SLAS Discov
; 26(2): 257-262, 2021 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-32808550
18.
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.
J Med Chem
; 64(8): 4289-4311, 2021 04 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-33783220
19.
Structural Insights into Notum Covalent Inhibition.
J Med Chem
; 64(15): 11354-11363, 2021 08 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-34292747
20.
Probing the SAM Binding Site of SARS-CoV-2 Nsp14 In Vitro Using SAM Competitive Inhibitors Guides Developing Selective Bisubstrate Inhibitors.
SLAS Discov
; 26(9): 1200-1211, 2021 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-34192965