Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 57, Issue 22, Pages 9693-9699Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm501194p
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Funding
- National Institutes of Health [GM097381, AI058072, CA173056]
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CXCL12 binds to CXCR4, promoting both chemotaxis of lymphocytes and metastasis of cancer cells. We previously identified small molecule ligands that bind CXCL12 and block CXCR4-mediated chemotaxis. We now report a 1.9 angstrom resolution X-ray structure of CXCL12 bound by such a molecule at a site normally bound by sY21 of CXCR4. The complex structure reveals binding hot spots for future inhibitor design and suggests a new approach to targeting CXCL12CXCR4 signaling in drug discovery.
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