ACS Medicinal Chemistry Letters
Page 6 of 7
The authors would like to acknowledge Dr. Shaoxiang Wu of
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Wilson, L. J.; Liotta, D. C., Emergence of Small-Molecule
Emory NMR facility, and Dr. Fred Strobel for mass spectrometry.
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CXCR4 Antagonists as Novel Immune and Hematopoietic System
Regulatory Agents. Drug Dev. Res. 2011, 72 (7), 598-602.
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ABBREVIATIONS
CXCR4, CXC chemokine receptor type 4; GPCR, G proteinꢀ
coupled receptor; CXCL12, CXC chemokine ligand type 12;
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Jenkinson, S.; Thomson, M.; McCoy, D.; Edelstein, M.;
Danehower, S.; Lawrence, W.; Wheelan, P.; Spaltenstein, A.;
Gudmundsson, K., Blockade of X4-Tropic HIV-1 Cellular Entry by
THQ,
5,6,7,8ꢀtetrahydroquinoline;
THIQ,
1,2,3,4ꢀ
GSK812397,
a
Potent Noncompetitive CXCR4 Receptor
tetrahydroisoquinoline; HLM, human liver microsomes; RLM, rat
liver microsomes; MLM, mouse liver microsomes; TFA, triꢀ
fluoroacetic acid; DCE, 1,2ꢀdichloroethane; mAChR, muscarinic
acetylcholine receptor; STABꢀH, sodium triacetoxyborohydride;
PAMPA, parallel artificial membrane permeability assay.
Antagonist. Antimicrob. Agents Chemother. 2010, 54 (2), 817-
824.
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Thoma, G.; Streiff, M. B.; Kovarik, J.; Glickman, F.;
Wagner, T.; Beerli, C.; Zerwes, H.-G., Orally Bioavailable
Isothioureas Block Function of the Chemokine Receptor CXCR4 in
Vitro and in Vivo. J. Med. Chem. 2008, 51 (24), 7915-7920.
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