NDLI: Identification of Inhibitors against Interaction between Pro-inflammatory sPLA2-IIA Protein and Integrin αvβ3

Content Provider	PubMed Central
Author	Ye, Long Dickerson, Tiffany Kaur, Handeep Takada, Yoko K. Fujita, Masaaki Liu, Ruiwu Knapp, John M. Lam, Kit S. Schore, Neil E. Kurth, Mark J. Takada, Yoshikazu
Abstract	Increased concentrations of secreted phospholipase A2 type IIA (sPLA2-IIA), have been found in the synovial fluid of patients with rheumatoid arthritis. It has been shown that sPLA2-IIA specifically binds to integrin αvβ3, and initiates a signaling pathway that leads to cell proliferation and inflammation. Therefore, the interaction between integrin and sPLA2-IIA could be a potential therapeutic target for the treatment of proliferation or inflammation-related diseases. Two one-bead-one-compound peptide libraries were co nstructed and screened, and seven target hits were identified. Herein we report the identification, synthesis, and biological testing of two pyrazolylthiazole-tethered peptide hits and their analogs. Biological assays showed that these compounds were able to suppress the sPLA2-IIA-integrin interaction and sPLA2-IIA-induced migration of monocytic cells and that the blockade of the sPLA2-IIA-integrin binding was specific to sPLA2-IIA and not to the integrin.
Related Links	http://dx.doi.org/10.1016/j.bmcl.2012.10.080
Ending Page	345
Page Count	6
Starting Page	340
File Format	PDF
ISSN	0960894X
e-ISSN	14643405
Journal	Bioorganic & medicinal chemistry letters
Issue Number	1
Volume Number	23
Language	English
Publisher Date	2013-01-01
Access Restriction	Open
Subject Keyword	Organic Chemistry Clinical Biochemistry Molecular Medicine Biochemistry Molecular Biology Drug Discovery Pharmaceutical Science Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry Molecular Biology Clinical Biochemistry Molecular Medicine Pharmaceutical Science

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