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A novel class of ion displacement ligands as antagonists of the αIIbß3 receptor that limit conformational reorganization of the receptor.
Jiang, Jian-kang; McCoy, Joshua G; Shen, Min; LeClair, Christopher A; Huang, Wenwei; Negri, Ana; Li, Jihong; Blue, Robert; Harrington, Amanda Weil; Naini, Sarasija; David, George; Choi, Won-Seok; Volpi, Elisabetta; Fernandez, Joseph; Babayeva, Mariana; Nedelman, Mark A; Filizola, Marta; Coller, Barry S; Thomas, Craig J.
Afiliação
  • Jiang JK; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
  • McCoy JG; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
  • Shen M; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
  • LeClair CA; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
  • Huang W; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
  • Negri A; Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY, United States.
  • Li J; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Blue R; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Harrington AW; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Naini S; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • David G; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Choi WS; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Volpi E; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Fernandez J; Proteomics Resource Center, Rockefeller University, New York, NY, United States.
  • Babayeva M; Touro College of Pharmacy, New York, NY, United States.
  • Nedelman MA; Ekam Imaging, Boston, MA, United States.
  • Filizola M; Department of Structural and Chemical Biology, Icahn School of Medicine at Mount Sinai, New York, NY, United States.
  • Coller BS; Allen and Frances Adler Laboratory of Blood and Vascular Biology, Rockefeller University, New York, NY, United States.
  • Thomas CJ; NIH Chemical Genomics Center, Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address: craigt@mail.nih.gov.
Bioorg Med Chem Lett ; 24(4): 1148-53, 2014 Feb 15.
Article em En | MEDLINE | ID: mdl-24461295
ABSTRACT
A collection of αIIbß3 integrin receptor antagonists possessing a unique MIDAS metal ion displacement mechanism of action is presented. Insight into these agents' structure-activity relationships, binding modality, and pharmacokinetic and pharmacodynamic profiles highlight the potential of these small molecule ion displacement ligands as attractive candidates for clinical development.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Sanguíneas / Complexo Glicoproteico GPIIb-IIIa de Plaquetas Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Proteínas Sanguíneas / Complexo Glicoproteico GPIIb-IIIa de Plaquetas Limite: Humans Idioma: En Ano de publicação: 2014 Tipo de documento: Article