Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase

Mpakali, Anastasia; Barla, Ioanna; Lu, Liying; Ramesh, Karthik M.; Thomaidis, Nikolaos; Stern, Lawrence J.; Giastas, Petros; Stratikos, Efstratios

doi:10.1016/j.jmb.2024.168449

Title: Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase

Journal Article · 01 March 2024 · Journal of Molecular Biology

DOI: https://doi.org/10.1016/j.jmb.2024.168449 · OSTI ID:2283269

Mpakali, Anastasia;

; Lu, Liying;

;

; Stern, Lawrence J.;

;

View Accepted Manuscript (Publisher)

Cite

Export

Save

Sponsoring Organization:: USDOE

OSTI ID:: 2283269

Journal Information:: Journal of Molecular Biology, Journal Name: Journal of Molecular Biology Vol. 436 Journal Issue: 6; ISSN 0022-2836

Publisher:: ElsevierCopyright Statement

Country of Publication:: United Kingdom

Language:: English

References (50)

Phenylalanine-544 Plays a Key Role in Substrate and Inhibitor Binding by Providing a Hydrophobic Packing Point at the Active Site of Insulin-Regulated Aminopeptidase Albiston, Anthony L.; Pham, Vi; Ye, Siying Molecular Pharmacology, Vol. 78, Issue 4 https://doi.org/10.1124/mol.110.065458	journal	July 2010
Insulin-regulated aminopeptidase immunoreactivity is abundantly present in human hypothalamus and posterior pituitary gland, with reduced expression in paraventricular and suprachiasmatic neurons in chronic schizophrenia Bernstein, Hans-Gert; Müller, Susan; Dobrowolny, Hendrik European Archives of Psychiatry and Clinical Neuroscience, Vol. 267, Issue 5 https://doi.org/10.1007/s00406-016-0757-7	journal	December 2016
Serum IRAP, a Novel Direct Biomarker of Prediabetes and Type 2 Diabetes? Trocmé, Candice; Gonnet, Nicolas; Di Tommaso, Margaux Frontiers in Molecular Biosciences, Vol. 7 https://doi.org/10.3389/fmolb.2020.596141	journal	February 2021
Crystal Structure of Insulin-Regulated Aminopeptidase with Bound Substrate Analogue Provides Insight on Antigenic Epitope Precursor Recognition and Processing Mpakali, Anastasia; Saridakis, Emmanuel; Harlos, Karl The Journal of Immunology, Vol. 195, Issue 6 https://doi.org/10.4049/jimmunol.1501103	journal	August 2015
3,4-Diaminobenzoic Acid Derivatives as Inhibitors of the Oxytocinase Subfamily of M1 Aminopeptidases with Immune-Regulating Properties Papakyriakou, Athanasios; Zervoudi, Efthalia; Tsoukalidou, Sofia Journal of Medicinal Chemistry, Vol. 58, Issue 3 https://doi.org/10.1021/jm501867s	journal	January 2015
Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Aryl Sulfonamides Vanga, Sudarsana Reddy; Sävmarker, Jonas; Ng, Leelee ACS Omega, Vol. 3, Issue 4 https://doi.org/10.1021/acsomega.8b00595	journal	April 2018
Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Benzopyran-Based Inhibitors Vanga, Sudarsana Reddy; Åqvist, Johan; Hallberg, Anders Frontiers in Molecular Biosciences, Vol. 8 https://doi.org/10.3389/fmolb.2021.625274	journal	April 2021
Tools for supporting solution scattering during the COVID-19 pandemic Yang, Lin; Lazo, Edwin; Byrnes, James Journal of Synchrotron Radiation, Vol. 28, Issue 4 https://doi.org/10.1107/S160057752100521X	journal	June 2021
Crystal structure of human insulin-regulated aminopeptidase with specificity for cyclic peptides: Structure of Insulin-Regulated Aminopeptidase Hermans, Stefan J.; Ascher, David B.; Hancock, Nancy C. Protein Science, Vol. 24, Issue 2 https://doi.org/10.1002/pro.2604	journal	December 2014
Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures Diwakarla, Shanti; Nylander, Erik; Grönbladh, Alfhild ACS Chemical Neuroscience, Vol. 7, Issue 10 https://doi.org/10.1021/acschemneuro.6b00146	journal	August 2016
Ligand-Induced Conformational Change of Insulin-Regulated Aminopeptidase: Insights on Catalytic Mechanism and Active Site Plasticity Mpakali, Anastasia; Saridakis, Emmanuel; Harlos, Karl Journal of Medicinal Chemistry, Vol. 60, Issue 7 https://doi.org/10.1021/acs.jmedchem.6b01890	journal	April 2017
Insulin-Regulated Aminopeptidase Inhibition Ameliorates Metabolism in Obese Zucker Rats Krskova, Katarina; Balazova, Lucia; Dobrocsyova, Viktoria Frontiers in Molecular Biosciences, Vol. 7 https://doi.org/10.3389/fmolb.2020.586225	journal	December 2020
Insulin-Regulated Aminopeptidase Deficiency Provides Protection against Ischemic Stroke in Mice Pham, Vi; Albiston, Anthony L.; Downes, Catherine E. Journal of Neurotrauma, Vol. 29, Issue 6 https://doi.org/10.1089/neu.2011.1824	journal	April 2012
Disulfide Cyclized Tripeptide Analogues of Angiotensin IV as Potent and Selective Inhibitors of Insulin-Regulated Aminopeptidase (IRAP) Andersson, Hanna; Demaegdt, Heidi; Vauquelin, Georges Journal of Medicinal Chemistry, Vol. 53, Issue 22 https://doi.org/10.1021/jm100793t	journal	November 2010
Probing the S1 specificity pocket of the aminopeptidases that generate antigenic peptides Zervoudi, Efthalia; Papakyriakou, Athanasios; Georgiadou, Dimitra Biochemical Journal, Vol. 435, Issue 2 https://doi.org/10.1042/BJ20102049	journal	March 2011
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation Liddle, John; Hutchinson, Jonathan P.; Kitchen, Semra Journal of Medicinal Chemistry, Vol. 63, Issue 6 https://doi.org/10.1021/acs.jmedchem.9b02123	journal	February 2020
Insulin-regulated aminopeptidase inhibitors do not alter glucose handling in normal and diabetic rats Albiston, Anthony L.; Cacador, Mauricio; Sinnayah, Puspha Journal of Molecular Endocrinology, Vol. 58, Issue 4 https://doi.org/10.1530/JME-17-0033	journal	May 2017
Synthesis, Structure–Activity Relationships and Brain Uptake of a Novel Series of Benzopyran Inhibitors of Insulin-Regulated Aminopeptidase Mountford, Simon J.; Albiston, Anthony L.; Charman, William N. Journal of Medicinal Chemistry, Vol. 57, Issue 4 https://doi.org/10.1021/jm401540f	journal	February 2014
Is There an Interplay Between the Functional Domains of IRAP? Vear, Anika; Gaspari, Tracey; Thompson, Philip Frontiers in Cell and Developmental Biology, Vol. 8 https://doi.org/10.3389/fcell.2020.585237	journal	September 2020
Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides Borhade, Sanjay R.; Rosenström, Ulrika; Sävmarker, Jonas ChemistryOpen, Vol. 3, Issue 6 https://doi.org/10.1002/open.201402027	journal	November 2014
Phenylsulfamoyl Benzoic Acid Inhibitor of ERAP2 with a Novel Mode of Inhibition Arya, Richa; Maben, Zachary; Rane, Digamber ACS Chemical Biology, Vol. 17, Issue 7 https://doi.org/10.1021/acschembio.2c00093	journal	June 2022
The Apolipoprotein E2(Arg145Cys) Mutation Causes Autosomal Dominant Type III Hyperlipoproteinemia With Incomplete Penetrance de Villiers, Willem J. S.; van der Westhuyzen, Deneys R.; Coetzee, Gerhard A. Arteriosclerosis, Thrombosis, and Vascular Biology, Vol. 17, Issue 5 https://doi.org/10.1161/01.ATV.17.5.865	journal	May 1997
IRAP inhibition using HFI419 prevents moderate to severe acetylcholine mediated vasoconstriction in a rabbit model El-Hawli, Aisha; Qaradakhi, Tawar; Hayes, Alan Biomedicine & Pharmacotherapy, Vol. 86 https://doi.org/10.1016/j.biopha.2016.11.142	journal	February 2017
Identification of human placental leucine aminopeptidase as oxytocinase Tsujimoto, Masafumi; Mizutani, Shigehiko; Adachi, Hideki Archives of Biochemistry and Biophysics, Vol. 292, Issue 2 https://doi.org/10.1016/0003-9861(92)90007-J	journal	February 1992
Discovery of Selective Inhibitor Leads by Targeting an Allosteric Site in Insulin-Regulated Aminopeptidase Temponeras, Ioannis; Chiniadis, Lykourgos; Papakyriakou, Athanasios Pharmaceuticals, Vol. 14, Issue 6 https://doi.org/10.3390/ph14060584	journal	June 2021
IRAP Inhibitors: M1-Aminopeptidase Family Inspiration Barlow, Nicholas; Thompson, Philip E. Frontiers in Pharmacology, Vol. 11 https://doi.org/10.3389/fphar.2020.585930	journal	September 2020
Conformational dynamics linked to domain closure and substrate binding explain the ERAP1 allosteric regulation mechanism Maben, Zachary; Arya, Richa; Georgiadis, Dimitris Nature Communications, Vol. 12, Issue 1 https://doi.org/10.1038/s41467-021-25564-w	journal	September 2021
Insulin‐regulated aminopeptidase inhibitor‐mediated increases in dendritic spine density are facilitated by glucose uptake Seyer, Benjamin; Diwakarla, Shanti; Burns, Peta Journal of Neurochemistry, Vol. 153, Issue 4 https://doi.org/10.1111/jnc.14880	journal	October 2019
Solution scattering at the Life Science X-ray Scattering (LiX) beamline Yang, Lin; Antonelli, Stephen; Chodankar, Shirish Journal of Synchrotron Radiation, Vol. 27, Issue 3 https://doi.org/10.1107/S1600577520002362	journal	March 2020
The insulin-regulated aminopeptidase a companion and regulator of GLUT4 Keller, Susanna R. Frontiers in Bioscience, Vol. 8, Issue 6 https://doi.org/10.2741/1078	journal	January 2003
Development of cognitive enhancers based on inhibition of insulin-regulated aminopeptidase Chai, Siew Yeen; Yeatman, Holly R.; Parker, Michael W. BMC Neuroscience, Vol. 9, Issue S2 https://doi.org/10.1186/1471-2202-9-S2-S14	journal	December 2008
Non-Competitive Inhibition by Active Site Binders: Non-Competitive Inhibition by Active Site Binders Blat, Yuval Chemical Biology & Drug Design, Vol. 75, Issue 6 https://doi.org/10.1111/j.1747-0285.2010.00972.x	journal	March 2010
Optimization and Structure–Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases That Generate Antigenic Peptides Kokkala, Paraskevi; Mpakali, Anastasia; Mauvais, Francois-Xavier Journal of Medicinal Chemistry, Vol. 59, Issue 19 https://doi.org/10.1021/acs.jmedchem.6b01031	journal	September 2016
IRAP Identifies an Endosomal Compartment Required for MHC Class I Cross-Presentation Saveanu, Loredana; Carroll, Oliver; Weimershaus, Mirjana Science, Vol. 325, Issue 5937 https://doi.org/10.1126/science.1172845	journal	July 2009
Inhibition of insulin-regulated aminopeptidase confers neuroprotection in a conscious model of ischemic stroke Telianidis, Jonathon; Hunter, Andrew; Widdop, Robert Scientific Reports, Vol. 13, Issue 1 https://doi.org/10.1038/s41598-023-46072-5	journal	November 2023
Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor Mpakali, Anastasia; Saridakis, Emmanuel; Giastas, Petros ACS Medicinal Chemistry Letters, Vol. 11, Issue 7 https://doi.org/10.1021/acsmedchemlett.0c00172	journal	June 2020
Crystal structures of the endoplasmic reticulum aminopeptidase-1 (ERAP1) reveal the molecular basis for N-terminal peptide trimming Kochan, G.; Krojer, T.; Harvey, D. Proceedings of the National Academy of Sciences, Vol. 108, Issue 19 https://doi.org/10.1073/pnas.1101262108	journal	April 2011
Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on α-Hydroxy-β-amino Acid Derivatives of Bestatin Vourloumis, Dionisios; Mavridis, Ioannis; Athanasoulis, Alexandros Journal of Medicinal Chemistry, Vol. 65, Issue 14 https://doi.org/10.1021/acs.jmedchem.2c00904	journal	July 2022
Mixed and non-competitive enzyme inhibition: underlying mechanisms and mechanistic irrelevance of the formal two-site model Pesaresi, Alessandro Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 38, Issue 1 https://doi.org/10.1080/14756366.2023.2245168	journal	August 2023
A systematic re-examination of processing of MHCI-bound antigenic peptide precursors by endoplasmic reticulum aminopeptidase 1 Mavridis, George; Arya, Richa; Domnick, Alexander Journal of Biological Chemistry, Vol. 295, Issue 21 https://doi.org/10.1074/jbc.RA120.012976	journal	May 2020
Mechanism for antigenic peptide selection by endoplasmic reticulum aminopeptidase 1 Giastas, Petros; Mpakali, Anastasia; Papakyriakou, Athanasios Proceedings of the National Academy of Sciences, Vol. 116, Issue 52 https://doi.org/10.1073/pnas.1912070116	journal	December 2019
Electroosmotic Perfusion–Microdialysis Probe Created by Direct Laser Writing for Quantitative Assessment of Leucine Enkephalin Hydrolysis by Insulin-Regulated Aminopeptidase in Vivo Wilson, Rachael E.; Jaquins-Gerstl, Andrea; Chen, Jun Analytical Chemistry, Vol. 92, Issue 21 https://doi.org/10.1021/acs.analchem.0c02799	journal	September 2020
The Role of Conformational Dynamics in Antigen Trimming by Intracellular Aminopeptidases Papakyriakou, Athanasios; Stratikos, Efstratios Frontiers in Immunology, Vol. 8 https://doi.org/10.3389/fimmu.2017.00946	journal	August 2017
Critical Role of Interdomain Interactions in the Conformational Change and Catalytic Mechanism of Endoplasmic Reticulum Aminopeptidase 1 Stamogiannos, Athanasios; Maben, Zachary; Papakyriakou, Athanasios Biochemistry, Vol. 56, Issue 10 https://doi.org/10.1021/acs.biochem.6b01170	journal	March 2017
Identification and characterization of a new cognitive enhancer based on inhibition of insulin‐regulated aminopeptidase Albiston, Anthony L.; Morton, Craig J.; Ng, Hooi Ling The FASEB Journal, Vol. 22, Issue 12 https://doi.org/10.1096/fj.08-112227	journal	August 2008
Regulation of Insulin-Regulated Membrane Aminopeptidase Activity by Its C-Terminal Domain Ascher, David B.; Cromer, Brett A.; Morton, Craig J. Biochemistry, Vol. 50, Issue 13 https://doi.org/10.1021/bi101893w	journal	March 2011
Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers Andersson, Hanna; Hallberg, Mathias International Journal of Hypertension, Vol. 2012 https://doi.org/10.1155/2012/789671	journal	January 2012
Identification and development of specific inhibitors for insulin-regulated aminopeptidase as a new class of cognitive enhancers: Novel IRAP inhibitors Albiston, Anthony L.; Diwakarla, Shanti; Fernando, Ruani N. British Journal of Pharmacology, Vol. 164, Issue 1 https://doi.org/10.1111/j.1476-5381.2011.01402.x	journal	August 2011
IRAP-dependent endosomal T cell receptor signalling is essential for T cell responses Evnouchidou, Irini; Chappert, Pascal; Benadda, Samira Nature Communications, Vol. 11, Issue 1 https://doi.org/10.1038/s41467-020-16471-7	journal	June 2020
Discovery of potent and selective inhibitors of human aminopeptidases ERAP1 and ERAP2 by screening libraries of phosphorus-containing amino acid and dipeptide analogues Węglarz-Tomczak, Ewelina; Vassiliou, Stamatia; Mucha, Artur Bioorganic & Medicinal Chemistry Letters, Vol. 26, Issue 16 https://doi.org/10.1016/j.bmcl.2016.06.062	journal	August 2016

Similar Records

Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor

Journal Article · 2021 · ACS Medicinal Chemistry Letters · OSTI ID:1690159

Mpakali, A; Saridakis, E.; Giastas, P.; +5 more

Lysosomal enzyme binding to the cation-independent mannose 6-phosphate receptor is regulated allosterically by insulin-like growth factor 2

Journal Article · 2024 · Scientific Reports · OSTI ID:2481711

Bohnsack, Richard N.; Misra, Sandeep K.; Liu, Jianfang; +6 more

The gene expression of two endoplasmic reticulum aminopeptidase 1 isoforms is regulated by distinct posttranscriptional mechanisms

Journal Article · 2018 · Biochemical and Biophysical Research Communications · OSTI ID:23134254

Aoki, Kazuma; Furuya, Akemi; Matsumoto, Ken; +1 more

Title: Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase

Citation Formats

References (50)

Similar Records

Related Subjects