TY - JOUR
T1 - The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin
AU - Andersen, Jacob Lauwring
AU - Lindberg, Samsa
AU - Langgård, Morten
AU - Maltas, Philip J
AU - Rønn, Lars Christian Biilmann
AU - Bundgaard, Christoffer
AU - Strandbygaard, Dorthe
AU - Thirup, Søren
AU - Watson, Stephen Paul
N1 - Copyright © 2017 Elsevier Ltd. All rights reserved.
PY - 2017/6/1
Y1 - 2017/6/1
N2 - Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.
AB - Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.
KW - Journal Article
U2 - 10.1016/j.bmcl.2017.02.028
DO - 10.1016/j.bmcl.2017.02.028
M3 - Journal article
C2 - 28462834
SN - 0960-894X
VL - 27
SP - 2629
EP - 2633
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
IS - 11
ER -