138109-37-2Relevant academic research and scientific papers
Poly-α,β-aspartyl-Arg-Gly-Asp-Phe: A novel polymeric nanomedicine
Chen, Shuangling,Wang, Yuji,Li, Shan,Wang, Yaonan,Zhao, Ming,Zhu, Haimei,Wu, Jianhui,Peng, Shiqi
supporting information, p. 182 - 186 (2015/02/18)
Thrombosis is a pathological condition and has been one of the most prominent causes of morbidity and mortality. Poly-α,β-aspartic acid is a biodegradable polymer, and RGD-tetrapeptides target thrombus. These led to the design of poly-α,β-aspartyl-Arg-Gly
Design of a new class of orally active fibrinogen receptor antagonists
Klein, Scott I.,Molino, Bruce F.,Czekaj, Mark,Gardner, Charles J.,Chu, Valeria,Brown, Karen,Sabatino, Ralph D.,Bostwick, Jeffrey S.,Kasiewski, Charles,Bentley, Ross,Windisch, Vincent,Perrone, Mark,Dunwiddie, Christopher T.,Leadley, Robert J.
, p. 2492 - 2502 (2007/10/03)
The integrin receptor recognition sequence Arg-Gly-Asp was successfully used as a template from which to develop a series of potent, selective, orally active, peptide-based fibrinogen receptor antagonists with a long duration of action. Simple modifications centered on the Arg and Gly residues quickly led to a modified peptide (1) with significantly enhanced ability to inhibit in vitro platelet aggregation. Substitution of the guanidino group in 1 by piperidine provided 3, which showed not only a further increase in potency but also a modest degree of oral efficacy. Finally, exploration of the nature of the C-terminal amino acid, with respect to its side-chain functionality and the carboxy terminus, yielded a group of molecules that showed excellent in vitro potency for inhibiting platelet aggregation, excellent integrin selectivity, a high level of oral efficacy, and an extended duration of action.
