Allosteric Inhibitors of Akt1 and Akt2: Discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with Potent and Balanced Activity
Overview
Authors
Affiliations
A series of [1,2,4]triazolo[3,4-f][1,6]naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory activity against Akt1 and 2 in vivo in a mouse model.
Nagarajan S, Fazlur-Rahman N ACS Omega. 2024; 9(23):24464-24476.
PMID: 38882093 PMC: 11170762. DOI: 10.1021/acsomega.4c00188.
Computational approaches for the design of modulators targeting protein-protein interactions.
Rehman A, Khurshid B, Ali Y, Rasheed S, Wadood A, Ng H Expert Opin Drug Discov. 2023; 18(3):315-333.
PMID: 36715303 PMC: 10149343. DOI: 10.1080/17460441.2023.2171396.
Synthesis and Anticancer Properties of Functionalized 1,6-Naphthyridines.
Lavanya M, Lin C, Mao J, Thirumalai D, Aabaka S, Yang X Top Curr Chem (Cham). 2021; 379(2):13.
PMID: 33624162 DOI: 10.1007/s41061-020-00314-6.
Distinct functions of AKT isoforms in breast cancer: a comprehensive review.
Hinz N, Jucker M Cell Commun Signal. 2019; 17(1):154.
PMID: 31752925 PMC: 6873690. DOI: 10.1186/s12964-019-0450-3.
Akhtar N, Jabeen I PLoS One. 2016; 11(12):e0168806.
PMID: 28036396 PMC: 5201309. DOI: 10.1371/journal.pone.0168806.