Discovery and Optimization of a Series of Benzofuran Selective ERAP1 Inhibitors: Biochemical and In Silico Studies
Author:
Affiliation:
1. Sanofi, 67080 Strasbourg, France
2. Sanofi, D-65926 Frankfurt am Main, Germany
3. Domain Therapeutics, 67400 Illkirch, France
4. Biosynex, 67400 Illkirch, France
5. Evotec, 31036 Toulouse cedex, France
Publisher
American Chemical Society (ACS)
Subject
Organic Chemistry,Drug Discovery,Biochemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.1c00235
Reference20 articles.
1. Genetic associations and functional characterization of M1 aminopeptidases and immune-mediated diseases
2. The ER aminopeptidase ERAP1 enhances or limits antigen presentation by trimming epitopes to 8–9 residues
3. Functionally distinctERAP1allotype combinations distinguish individuals with Ankylosing Spondylitis
4. Induction of Protective Antitumor Immunity through Attenuation of ERAAP Function
5. The roles of ERAP1 and ERAP2 in autoimmunity and cancer immunity: New insights and perspective
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1. ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights;Journal of Medicinal Chemistry;2024-07-16
2. Distinct modulation of cellular immunopeptidome by the allosteric regulatory site of ER aminopeptidase 1;European Journal of Immunology;2023-05-15
3. Distinct modulation of cellular immunopeptidome by the allosteric regulatory site of ER aminopeptidase 1;2023-02-16
4. Phosphinic Peptides as Tool Compounds for the Study of Pharmacologically Relevant Zn-Metalloproteases;ACS Pharmacology & Translational Science;2022-11-28
5. ERAP1 Controls the Interaction of the Inhibitory Receptor KIR3DL1 With HLA-B51:01 by Affecting Natural Killer Cell Function;Frontiers in Immunology;2021-11-30
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