853063-25-9Relevant academic research and scientific papers
Novel μ opioid antagonists derived from the μ opioid agonists endomorphin and [Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2)
Shi, Saijian,Xu, Jian,Feng, LingLing,Fan, Xin,Chen, Zhen,Qin, Yajuan,Chung, Nga N.,Li, Tingyou,Schiller, Peter W.
, p. 1305 - 1314 (2020/08/05)
Hybrid analogues of the μ opioid agonists endomorphin and [Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2, Dmt?=?2′,6′-dimethyltyrosine) containing cis-4-amino-Pro, trans-4-amino-Pro, cis-4-aminoethyl-Pro or cis-4-guanidinylethyl-Pro in the 2 p
Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds
Tamamura, Hirokazu,Araki, Takanobu,Ueda, Satoshi,Wang, Zixuan,Oishi, Shinya,Esaka, Ai,Trent, John O.,Nakashima, Hideki,Yamamoto, Naoki,Peiper, Stephen C.,Otaka, Akira,Fujii, Nobutaka
, p. 3280 - 3289 (2007/10/03)
A highly potent CXCR4 antagonist, compound 2, was previously found by using two orthogonal cyclic pentapeptide libraries involving conformation-based and sequence-based libraries based on the pharmacophore of a 14-mer peptidic antagonist, 1. Herein, cyclic tetrapeptides derived from replacements of the dipeptide unit (Nal-Gly) with a γ-amino acid and pseudopeptides cyclized by disulfide and olefin bridges were synthesized to find novel scaffold structures different from that of cyclic pentapeptides. These compounds contain a reduced number of peptide bonds compared to compound 2. Furthermore, several analogues with chemical modification of the side chain of Arg4 in 2 were also prepared. From these, several new leads possessing high to moderate CXCR4-antagonistic activity were characterized.
