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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.
Artículo
en Inglés
| MEDLINE | ID: mdl-31796582
2.
Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.
Bioconjug Chem;
30(5): 1356-1370, 2019 05 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-30966735
3.
Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.
Bioorg Med Chem Lett;
23(17): 4953-9, 2013 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23867164
4.
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Bioorg Med Chem Lett;
22(13): 4296-302, 2012 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-22672799
5.
A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel.
Neuron;
109(2): 273-284.e4, 2021 01 20.
Artículo
en Inglés
| MEDLINE | ID: mdl-33152265
6.
Immune-stimulating antibody conjugates elicit robust myeloid activation and durable antitumor immunity.
Nat Cancer;
2(1): 18-33, 2021 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-35121890
7.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-33749283
8.
Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310.
J Med Chem;
64(6): 2953-2966, 2021 03 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-33682420
9.
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.
J Med Chem;
62(8): 4091-4109, 2019 04 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-30943032
10.
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity.
J Med Chem;
62(2): 908-927, 2019 01 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-30499663
11.
Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain.
Cell Rep;
24(12): 3133-3145, 2018 09 18.
Artículo
en Inglés
| MEDLINE | ID: mdl-30231997
12.
Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.
J Med Chem;
61(3): 989-1000, 2018 02 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-29227683
13.
Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.
J Med Chem;
61(8): 3641-3659, 2018 04 26.
Artículo
en Inglés
| MEDLINE | ID: mdl-29590749
14.
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
J Med Chem;
61(11): 4810-4831, 2018 06 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-29737846
15.
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.
ACS Med Chem Lett;
8(9): 936-940, 2017 Sep 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-28947940
16.
Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.
J Med Chem;
60(23): 9490-9507, 2017 12 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-29112410
17.
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
ACS Med Chem Lett;
7(3): 277-82, 2016 Mar 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-26985315
18.
Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
Science;
350(6267): aac5464, 2015 Dec 18.
Artículo
en Inglés
| MEDLINE | ID: mdl-26680203
19.
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.
J Med Chem;
55(17): 7686-95, 2012 Sep 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-22877085
20.
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
J Med Chem;
55(18): 8110-27, 2012 Sep 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-22934575