ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights

V Fougiaxis, B He, T Khan, R Vatinel… - Journal of Medicinal …, 2024 - ACS Publications
Endoplasmic reticulum aminopeptidases ERAP1 and 2 are intracellular aminopeptidases
that trim antigenic precursors and generate antigens presented by major histocompatibility …

Organophosphorus chemistry based on elemental phosphorus: Advances and horizons

NK Gusarova, BA Trofimov - Russian Chemical Reviews, 2020 - iopscience.iop.org
The results of studies on the application of elemental phosphorus for the synthesis of
important organophosphorus compounds are surveyed and summarized. Currently, this …

Acetylene group, friend or foe in medicinal chemistry

TT Talele - Journal of Medicinal Chemistry, 2020 - ACS Publications
The use of an acetylene (ethynyl) group in medicinal chemistry coincides with the launch of
the Journal of Medicinal Chemistry in 1959. Since then, the acetylene group has been …

A novel microporous hydrogen-bonded organic framework with electron-rich alkynyl groups for highly efficient C 2 H 6/C 2 H 4 separation

YB Wang, TF Zhang, YX Lin, JX Wang… - Journal of Materials …, 2024 - pubs.rsc.org
Microporous hydrogen-bonded organic frameworks (HOFs) have been considered
promising materials for ethane/ethylene (C2H6/C2H4) separation owing to their native …

Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase

A Mpakali, I Barla, L Lu, KM Ramesh… - Journal of Molecular …, 2024 - Elsevier
Abstract Inhibition of Insulin-Regulated Aminopeptidase is being actively explored for the
treatment of several human diseases and several classes of inhibitors have been developed …

Intracellular antigen processing by ERAP2: Molecular mechanism and roles in health and disease

JAL de Castro, E Stratikos - Human Immunology, 2019 - Elsevier
Abstract Endoplasmic Reticulum Aminopeptidase 2 (ERAP2) is an intracellular enzyme
localized in the ER that has been shown to play roles in the generation of peptides that …

Mechanism for antigenic peptide selection by endoplasmic reticulum aminopeptidase 1

P Giastas, A Mpakali, A Papakyriakou… - Proceedings of the …, 2019 - National Acad Sciences
Endoplasmic reticulum aminopeptidase 1 (ERAP1) is an intracellular enzyme that optimizes
the peptide cargo of major histocompatibility class I (MHC-I) molecules and regulates …

Carnosic Acid: A Novel Selective Inhibitor of ERAP1 by Direct Binding and Its Modulation of Antigen Processing and Presentation

J Wu, Z Li, X Liu, D Feng, R Liang, X Su… - Journal of Agricultural …, 2024 - ACS Publications
ERAP1 is an emerging target for a large subclass of severe autoimmune diseases known as
“MHC-I-opathy”, together with tumor immunity. Nevertheless, effective inhibitors targeting …

Editing the immunopeptidome of melanoma cells using a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1)

D Koumantou, E Barnea, A Martin-Esteban… - Cancer Immunology …, 2019 - Springer
The efficacy of cancer immunotherapy, including treatment with immune-checkpoint
inhibitors, often is limited by ineffective presentation of antigenic peptides that elicit T-cell …

Discovery of selective inhibitors of endoplasmic reticulum aminopeptidase 1

Z Maben, R Arya, D Rane, WF An… - Journal of medicinal …, 2019 - ACS Publications
ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important
role in the immune system by trimming peptides for loading onto major histocompatibility …