1215685-45-2Relevant academic research and scientific papers
Synthesis and biological evaluation of selective CXCR4 antagonists containing alkene dipeptide isosteres
Narumi, Tetsuo,Hayashi, Ryoko,Tomita, Kenji,Kobayashi, Kazuya,Tanahara, Noriko,Ohno, Hiroaki,Naito, Takeshi,Kodama, Eiichi,Matsuoka, Masao,Oishi, Shinya,Fujii, Nobutaka
, p. 616 - 621 (2010)
A set of cyclic peptide analogues of a selective CXCR4 antagonist FC131 [cyclo(-d-Tyr-Arg-Arg-Nal-Gly-)] were synthesized and bioevaluated. Using (E)-alkene and (Z)-fluoroalkene dipeptide isosteres for Arg-Arg and Arg-Nal substructures, indispensable or the partial contribution of the two peptide bonds to the CXCR4 antagonism and anti-HIV activity was demonstrated. FC131 and the analogues were shown to selectively inhibit SDF-1 binding to CXCR4, whereas no inhibition of binding of SDF-1 to CXCR7 was observed.
