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

Thermodynamic Switch in Binding of Adhesion/Growth Regulatory Human Galectin-3 to Tumor-Associated TF Antigen (CD176) and MUC1 Glycopeptides

(2015) Maria C. Rodriguez et al.   BIOCHEMISTRY

Effects of ADAM10 upregulation on progression, migration, and prognosis of nasopharyngeal carcinoma

(2015) Bo You et al.   CANCER SCIENCE

A transmembrane C-terminal fragment of syndecan-1 is generated by the metalloproteinase ADAM17 and promotes lung epithelial tumor cell migration and lung metastasis formation

(2015) Tobias Pasqualon et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

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

The Disintegrin and Metalloprotease ADAM12 Is Associated with TGF-β-Induced Epithelial to Mesenchymal Transition

(2015) Michaël Ruff et al.   PLoS One

ADAM10 mediates trastuzumab resistance and is correlated with survival in HER2 positive breast cancer

(2015) Katharina Feldinger et al.   Oncotarget

Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β

(2014) Franck Madoux et al.   BIOPOLYMERS

Leukocytes require ADAM10 but not ADAM17 for their migration and inflammatory recruitment into the alveolar space

(2014) J. Pruessmeyer et al.   BLOOD

POVME 2.0: An Enhanced Tool for Determining Pocket Shape and Volume Characteristics

(2014) Jacob D. Durrant et al.   Journal of Chemical Theory and Computation

Characterization of Selective Exosite-Binding Inhibitors of Matrix Metalloproteinase 13 That Prevent Articular Cartilage Degradation in Vitro

(2014) Timothy P. Spicer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Substrate-selective COX-2 inhibition as a novel strategy for therapeutic endocannabinoid augmentation

(2014) Daniel J. Hermanson et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Multiple Exosites Distributed across the Three Domains of Streptokinase Co-Operate to Generate High Catalytic Rates in the Streptokinase–Plasmin Activator Complex

(2013) Rachna Aneja et al.   BIOCHEMISTRY

Activity of ADAM17 (a Disintegrin and Metalloprotease 17) Is Regulated by Its Noncatalytic Domains and Secondary Structure of its Substrates

(2013) Roma Stawikowska et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Designing Allosteric Regulators of Thrombin. Exosite 2 Features Multiple Subsites That Can Be Targeted by Sulfated Small Molecules for Inducing Inhibition

(2013) Preetpal Singh Sidhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

ADAM17 is overexpressed in non-small cell lung cancer and its expression correlates with poor patient survival

(2013) Shuang-Shuang Ni et al.   TUMOR BIOLOGY

Identifi cation of protease exosite-interacting peptides that enhance substrate cleavage kinetics

(2012) Abeer M. Jabaiah et al.   BIOLOGICAL CHEMISTRY

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

The Role of the Anti-Amyloidogenic Secretase ADAM10 in Shedding the APP-like Proteins

(2012) Kristina Endres et al.   Current Alzheimer Research

Novel methods and strategies in the discovery of TACE inhibitors

(2012) Prashant R Murumkar et al.   Expert Opinion on Drug Discovery

Discovery of Novel Inhibitors of a Disintegrin and Metalloprotease 17 (ADAM17) Using Glycosylated and Non-glycosylated Substrates

(2012) Dmitriy Minond et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterizing the Diversity and Biological Relevance of the MLPCN Assay Manifold and Screening Set

(2011) Jintao Zhang et al.   Journal of Chemical Information and Modeling

Cross-domain inhibition of TACE ectodomain

(2011) C. J. Tape et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct role of the intracellular C-terminus for subcellular expression, shedding and function of the murine transmembrane chemokine CX3CL1

(2010) Michael G. Andrzejewski et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

ADAM17 is regulated by a rapid and reversible mechanism that controls access to its catalytic site

(2010) S. M. Le Gall et al.   JOURNAL OF CELL SCIENCE

Structural basis for high-affinity HER2 receptor binding by an engineered protein

(2010) C. Eigenbrot et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

HER2 Phosphorylation Is Maintained by a PKB Negative Feedback Loop in Response to Anti-HER2 Herceptin in Breast Cancer

(2010) Merel Gijsen et al.   PLOS BIOLOGY

CXCL16 Is Expressed in Podocytes and Acts as a Scavenger Receptor for Oxidized Low-Density Lipoprotein

(2009) Paul Gutwein et al.   AMERICAN JOURNAL OF PATHOLOGY

The discovery of novel tartrate-based TNF-α converting enzyme (TACE) inhibitors

(2009) Kristin E. Rosner et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Disintegrin and Metalloproteinase 17 (ADAM17) Mediates Inflammation-induced Shedding of Syndecan-1 and -4 by Lung Epithelial Cells

(2009) Jessica Pruessmeyer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Variants of the Antibody Herceptin That Interact with HER2 and VEGF at the Antigen Binding Site

(2009) J. Bostrom et al.   SCIENCE

Specific targeting of metzincin family members with small-molecule inhibitors: Progress toward a multifarious challenge

(2008) Dimitris Georgiadis et al.   BIOORGANIC & MEDICINAL CHEMISTRY

High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate

(2008) Janelle L. Lauer-Fields et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthetic active site-directed inhibitors of metzincins: Achievement and perspectives

(2008) A YIOTAKIS et al.   MOLECULAR ASPECTS OF MEDICINE

Drug Insight: tumor necrosis factor-converting enzyme as a pharmaceutical target for rheumatoid arthritis

(2008) Marcia L Moss et al.   Nature clinical practice. Rheumatology