Peptidomimetics: An Overview of Recent Medicinal Chemistry Efforts toward the Discovery of Novel Small Molecule Inhibitors.

Autor: Li Petri G; Drug Discovery Unit, Ri.MED Foundation, Palermo 90133, Italy., Di Martino S; Drug Discovery Unit, Ri.MED Foundation, Palermo 90133, Italy., De Rosa M; Drug Discovery Unit, Ri.MED Foundation, Palermo 90133, Italy.
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2022 Jun 09; Vol. 65 (11), pp. 7438-7475. Date of Electronic Publication: 2022 May 23.
DOI: 10.1021/acs.jmedchem.2c00123
Abstrakt: The use of peptides as therapeutics has often been associated with several drawbacks such as poor absorption, low stability to proteolytic digestion, and fast clearance. Peptidomimetics are developed by modifications of native peptides with the aim of obtaining molecules that are more suitable for clinical development and, for this reason, are widely used as tools in medicinal chemistry programs. The effort to disclose innovative peptidomimetic therapies is recurrent and constantly evolving as demonstrated by the new lead compounds in clinical trials. Synthetic strategies for the development of peptidomimetics have also been implemented with time. This perspective highlights some of the most recent efforts for the design and synthesis of peptidomimetic agents together with their biological evaluation toward a panel of targets.
Databáze: MEDLINE