1215685-53-2Relevant 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
supporting information; experimental part, p. 616 - 621 (2010/05/11)
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.
