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Synthesis and Analysis of Pyridine Derivatives as Small Molecule Antagonists of CXCR4

Virani, Saniya
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Abstract

Chemokines, largest family of cytokines, regulate cell trafficking through interaction of GPCR. Chemokines are classified into categories depending on the pattern of cysteine residue. Chemokine receptor type 4 (CXCR4) is a cell surface receptor important when cells migrate during inflammation and has been linked to various disease pathways such as cancer metastasis, inflammation disease, HIV-1 proliferation, and auto-immune disorders. CXCR4 along with its cognate ligand CXCL12 have been projected to regulate metastases sites in invasion of breast cancer cells. Several pyridine analogues have been synthesized as potential CXCR4 antagonists via reductive amination. These compounds are analyzed through proton and carbon NMR, high- resolution mass spectrometry, and melting point. After synthesis, the analogues undergo several assays at Emory University in Shim lab. The assays include Binding affinity assay, Matrigel invasion assay, and Carrageenan paw edema test.

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2018-08-07
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Small molecules, CXCR4, CXCL12, Inhibitors, Cancer metastasis, Inflammation, Reductive amination, Binding affinity assay, Matrigel invasion assay, Carrageenan paw edema test.
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