id author title date pages extension mime words sentences flesch summary cache txt cord-256324-w3bejmy5 Hamada, Yoshio New directions for protease inhibitors directed drug discovery 2016-07-22 .txt text/plain 5066 292 55 23 Most b-secretase inhibitors possess a transition state analogue at the P 1 position and are designed based on the amino acid sequence of Swedish mutant APP, which has a double mutation around the b-site (at the K670N and M671L residues). Many inhibitors with an aromatic ring at the P 1 position were subsequently reported; for example, a research group at Merck Sharp and Dohme (MSD) reported the potent inhibitors 50 63, 64 Although 18 was designed based on peptidomimetic inhibitors by using the SBDD approach, it is notable because it forms a unique cyclic structure at the P 1 position where the hydroxyl and amino groups on the cyclic sulfone ring of 18 appear to interact with two Asp residues at the active site of b-secretase as well as acting as a transition state analogue. ./cache/cord-256324-w3bejmy5.txt ./txt/cord-256324-w3bejmy5.txt