Your browser doesn't support javascript.
loading
Discovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors.
Lesniak, Robert K; Nichols, R Jeremy; Schonemann, Marcus; Zhao, Jing; Gajera, Chandresh R; Lam, Grace; Nguyen, Khanh C; Langston, J William; Smith, Mark; Montine, Thomas J.
Afiliação
  • Lesniak RK; Medicinal Chemistry Knowledge Center, Sarafan ChEM-H, Stanford University, Stanford, California 94305, United States.
  • Nichols RJ; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Schonemann M; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Zhao J; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Gajera CR; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Lam G; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Nguyen KC; Departments of Medicine and Microbiology and Immunology, Division of Gastroenterology and Hepatology, Stanford University School of Medicine, Stanford, California 94305, United States.
  • Langston JW; Departments of Medicine and Microbiology and Immunology, Division of Gastroenterology and Hepatology, Stanford University School of Medicine, Stanford, California 94305, United States.
  • Smith M; Department of Pathology, Stanford University, 300 Pasteur Drive, Stanford, California 94305, United States.
  • Montine TJ; Department of Neurology and Neuroscience, Stanford University, 300 Pasteur Drive, Stanford, California 94304, United States.
ACS Med Chem Lett ; 13(6): 981-988, 2022 Jun 09.
Article em En | MEDLINE | ID: mdl-35707141
ABSTRACT
G2019S (GS) is the most prevalent mutation in the leucine rich repeat protein kinase 2 gene (LRRK2), a genetic predisposition that is common for Parkinson's disease, as well as for some forms of cancer, and is a shared risk allele for Crohn's disease. GS-LRRK2 has a hyperactive kinase, and although numerous drug discovery programs have targeted LRRK2 kinase, few have reached clinical development. We report the discovery and preliminary development of an entirely novel structural class of potent and selective GS-LRRK2 kinase inhibitors biaryl-1H-pyrazoles.
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Estados Unidos