Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme

Tanshinones that selectively block the collagenase activity of cathepsin K provide a novel class of ectosteric antiresorptive agents for bone

(2018) Preety Panwar et al.   BRITISH JOURNAL OF PHARMACOLOGY

Liver-specific ablation of insulin-degrading enzyme causes hepatic insulin resistance and glucose intolerance, without affecting insulin clearance in mice

(2018) Pablo Villa-Pérez et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Novel Noncatalytic Substrate-Selective p38α-Specific MAPK Inhibitors with Endothelial-Stabilizing and Anti-Inflammatory Activity

(2017) Nirav G. Shah et al.   JOURNAL OF IMMUNOLOGY

Targeting Insulin-Degrading Enzyme to Treat Type 2 Diabetes Mellitus

(2016) Wei-Jen Tang   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

(2016) Matthew D Hall et al.   Methods and Applications in Fluorescence

Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate

(2016) Franck Madoux et al.   Scientific Reports

Selective Targeting of Extracellular Insulin-Degrading Enzyme by Quasi-Irreversible Thiol-Modifying Inhibitors

(2015) Samer O. Abdul-Hay et al.   ACS Chemical Biology

Neprilysin inhibition to treat heart failure: a tale of science, serendipity, and second chances

(2015) John J.V. McMurray   EUROPEAN JOURNAL OF HEART FAILURE

Structure–activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme

(2015) Julie Charton et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearancein Vivo

(2015) Timothy B. Durham et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes

(2015) Anna M. Knapinska et al.   JOURNAL OF MEDICINAL CHEMISTRY

Systematic discovery of linear binding motifs targeting an ancient protein interaction surface on MAP kinases

(2015) A. Zeke et al.   Molecular Systems Biology

Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice

(2015) Rebecca Deprez-Poulain et al.   Nature Communications

SHELXT– Integrated space-group and crystal-structure determination

(2015) George M. Sheldrick   Acta Crystallographica A-Foundation and Advances

Crystal structure refinement withSHELXL

(2015) George M. Sheldrick   Acta Crystallographica Section C-Structural Chemistry

Comparison of silver and molybdenum microfocus X-ray sources for single-crystal structure determination

(2015) Lennard Krause et al.   JOURNAL OF APPLIED CRYSTALLOGRAPHY

Insulin-Degrading Enzyme Inhibition, a Novel Therapy for Type 2 Diabetes?

(2014) Safia Costes et al.   Cell Metabolism

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis

(2014) Julie Charton et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones

(2014) Juan Pablo Maianti et al.   NATURE

Is there new hope for therapeutic matrix metalloproteinase inhibition?

(2014) Roosmarijn E. Vandenbroucke et al.   NATURE REVIEWS DRUG DISCOVERY

A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1

(2014) T. Justin Rettenmaier et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Type 2 Diabetes-Associated Gene Ide Is Required for Insulin Secretion and Suppression of  -Synuclein Levels in  -Cells

(2013) P. Steneberg et al.   DIABETES

Optimization of Peptide Hydroxamate Inhibitors of Insulin-Degrading Enzyme Reveals Marked Substrate-Selectivity

(2013) Samer O. Abdul-Hay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conformational states and recognition of amyloidogenic peptides of human insulin-degrading enzyme

(2013) Lauren A. McCord et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Substrate-Selective Inhibition of Protein Kinase PDK1 by Small Compounds that Bind to the PIF-Pocket Allosteric Docking Site

(2012) Katrien Busschots et al.   CHEMISTRY & BIOLOGY

Glucagonocentric restructuring of diabetes: a pathophysiologic and therapeutic makeover

(2012) Roger H. Unger et al.   JOURNAL OF CLINICAL INVESTIGATION

Methyl Effects on Protein–Ligand Binding

(2012) Cheryl S. Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries

(2012) Jason T. Lowe et al.   JOURNAL OF ORGANIC CHEMISTRY

Data processing and analysis with theautoPROCtoolbox

(2011) Clemens Vonrhein et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

(R)-Profens are substrate-selective inhibitors of endocannabinoid oxygenation by COX-2

(2011) Kelsey C Duggan et al.   Nature Chemical Biology

Deletion of Insulin-Degrading Enzyme Elicits Antipodal, Age-Dependent Effects on Glucose and Insulin Tolerance

(2011) Samer O. Abdul-Hay et al.   PLoS One

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Two additive mechanisms impair the differentiation of 'substrate-selective' p38 inhibitors from classical p38 inhibitors in vitro

(2010) Bart S Hendriks et al.   BMC Systems Biology

Emerging principles in protease-based drug discovery

(2010) Marcin Drag et al.   NATURE REVIEWS DRUG DISCOVERY

Guidelines for accurate EC50/IC50 estimation

(2010) J. L. Sebaugh   PHARMACEUTICAL STATISTICS

A Monomeric Variant of Insulin Degrading Enzyme (IDE) Loses Its Regulatory Properties

(2010) Eun Suk Song et al.   PLoS One

Designed Inhibitors of Insulin-Degrading Enzyme Regulate the Catabolism and Activity of Insulin

(2010) Malcolm A. Leissring et al.   PLoS One

OLEX2: a complete structure solution, refinement and analysis program

(2009) Oleg V. Dolomanov et al.   JOURNAL OF APPLIED CRYSTALLOGRAPHY

Molecular Bases for the Recognition of Short Peptide Substrates and Cysteine-Directed Modifications of Human Insulin-Degrading Enzyme†

(2008) Enrico Malito et al.   BIOCHEMISTRY

Amyloid β-degrading cryptidases: insulin degrading enzyme, presequence peptidase, and neprilysin

(2008) E. Malito et al.   CELLULAR AND MOLECULAR LIFE SCIENCES