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Page 1
A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists.
Zhang WB, Navenot JM, Haribabu B, Tamamura H, Hiramatu K, Omagari A, Pei G, Manfredi JP, Fujii N, Broach JR, Peiper SC. Zhang WB, et al. Among authors: omagari a. J Biol Chem. 2002 Jul 5;277(27):24515-21. doi: 10.1074/jbc.M200889200. Epub 2002 Mar 28. J Biol Chem. 2002. PMID: 11923301 Free article.
Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity.
Tamamura H, Sugioka M, Odagaki Y, Omagari A, Kan Y, Oishi S, Nakashima H, Yamamoto N, Peiper SC, Hamanaka N, Otaka A, Fujii N. Tamamura H, et al. Among authors: omagari a. Bioorg Med Chem Lett. 2001 Feb 12;11(3):359-62. doi: 10.1016/s0960-894x(00)00664-8. Bioorg Med Chem Lett. 2001. PMID: 11212110
Certification of the critical importance of L-3-(2-naphthyl)alanine at position 3 of a specific CXCR4 inhibitor, T140, leads to an exploratory performance of its downsizing study.
Tamamura H, Omagari A, Hiramatsu K, Oishi S, Habashita H, Kanamoto T, Gotoh K, Yamamoto N, Nakashima H, Otaka A, Fujii N. Tamamura H, et al. Among authors: omagari a. Bioorg Med Chem. 2002 May;10(5):1417-26. doi: 10.1016/s0968-0896(01)00419-9. Bioorg Med Chem. 2002. PMID: 11886804
Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety.
Tamamura H, Hiramatsu K, Miyamoto K, Omagari A, Oishi S, Nakashima H, Yamamoto N, Kuroda Y, Nakagawa T, Otaka A, Fujii N. Tamamura H, et al. Among authors: omagari a. Bioorg Med Chem Lett. 2002 Mar 25;12(6):923-8. doi: 10.1016/s0960-894x(02)00041-0. Bioorg Med Chem Lett. 2002. PMID: 11958995
Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.
Tamamura H, Omagari A, Hiramatsu K, Gotoh K, Kanamoto T, Xu Y, Kodama E, Matsuoka M, Hattori T, Yamamoto N, Nakashima H, Otaka A, Fujii N. Tamamura H, et al. Among authors: omagari a. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. doi: 10.1016/s0960-894x(01)00323-7. Bioorg Med Chem Lett. 2001. PMID: 11459656