Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.

V, Camberlein; C, Fléau; P, Sierocki; L, Li; R, Gealageas; D, Bosc; V, Guillaume; S, Warenghem; F, Leroux; M, Rosell; K, Cheng; L, Medve; M, Prigent; M, Decanter; C, Piveteau; A, Biela; M, Eveque; J, Dumont; A, Mpakali; P, Giastas; A, Herledan; C, Couturier; J, Haupenthal; L, Lesire; AKH, Hirsch; B, Deprez; E, Stratikos; M, Bouvier; R, Deprez-Poulain

doi:10.1002/anie.202203560

Public

Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.

Shared by NobleBlocks on Aug 19, 2022 • 12:00 AM UTC

Authors:

Camberlein V

Fléau C

Sierocki P

Abstract

Endoplasmic reticulum aminopeptidase 2 (ERAP2) is a key enzyme involved in the trimming of antigenic peptides presented by Major Histocompatibility Complex class I. It is a target of growing interest for the treatment of autoimmune diseases and in cancer immunotherapy. However, the discovery of pote...

Subject

Medicinal chemistry

Metalloenzymes

Erap2

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