Recent developments and strategies for the discovery of TACE inhibitors

ADAM17: An Emerging Therapeutic Target for Lung Cancer

(2019) Saad et al.   Cancers

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis

(2018) Jean-Guy Boiteau et al.   BIOORGANIC & MEDICINAL CHEMISTRY

ADAM17 inhibition enhances platinum efficiency in ovarian cancer

(2018) Nina Hedemann et al.   Oncotarget

Specific inhibition of ADAM17/TACE promotes neurogenesis in the injured motor cortex

(2018) Noelia Geribaldi-Doldán et al.   Cell Death & Disease

Targeting ADAM17 inhibits human colorectal adenocarcinoma progression and tumor-initiating cell frequency

(2017) Joseph Dosch et al.   Oncotarget

Inhibition of ADAM17/TACE activity by zinc-chelating rye secalin-derived tripeptides and analogues

(2017) M. Chinonye Udechukwu et al.   RSC Advances

Molecular design and structural optimization of potent peptide hydroxamate inhibitors to selectively target human ADAM metallopeptidase domain 17

(2016) Zhengting Wang et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

An alignment-independent 3D-QSAR study on series of hydroxamic acid-based tumor necrosis factor-α converting enzyme inhibitors

(2016) Ali Akbar Alizadeh et al.   JOURNAL OF CHEMOMETRICS

Molecular basis for the mechanism of action of an anti-TACE antibody

(2016) Li Peng et al.   mAbs

Regulation of A disintegrin and metalloproteinase (ADAM) family sheddases ADAM10 and ADAM17: The emerging role of tetraspanins and rhomboids

(2016) Alexandra L. Matthews et al.   PLATELETS

Harnessing the natural inhibitory domain to control TNFα Converting Enzyme (TACE) activity in vivo

(2016) Eitan Wong et al.   Scientific Reports

Selective Inhibition of ADAM17 Efficiently Mediates Glycoprotein Ibα Retention During Ex Vivo Generation of Human Induced Pluripotent Stem Cell-Derived Platelets

(2016) Shinji Hirata et al.   Stem Cells Translational Medicine

Anti-arthritis effect of a novel quinazoline derivative through inhibiting production of TNF-α mediated by TNF-α converting enzyme in murine collagen-induced arthritis model

(2015) Yuzhi Pu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A metal-based tumour necrosis factor-alpha converting enzyme inhibitor

(2015) Chung-Hang Leung et al.   CHEMICAL COMMUNICATIONS

The Functional Maturation of A Disintegrin and Metalloproteinase (ADAM) 9, 10, and 17 Requires Processing at a Newly Identified Proprotein Convertase (PC) Cleavage Site

(2015) Eitan Wong et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure-based rational design of peptide hydroxamic acid inhibitors to target tumor necrosis factor-αconverting enzyme as potential therapeutics for hepatitis

(2015) Dan Wu et al.   JOURNAL OF DRUG TARGETING

Media effects in modulating the conformational equilibrium of a model compound for tumor necrosis factor converting enzyme inhibition

(2015) Martina Banchelli et al.   JOURNAL OF MOLECULAR STRUCTURE

The Antiatherogenic Effect of Fish Oil in Male Mice Is Associated with a Diminished Release of Endothelial ADAM17 and ADAM10 Substrates

(2015) Nancy Speck et al.   JOURNAL OF NUTRITION

Pharmacophore modeling for the identification of small-molecule inhibitors of TACE

(2015) Li-Juan Liu et al.   METHODS

A Monoclonal Antibody to ADAM17 Inhibits Tumor Growth by Inhibiting EGFR and Non-EGFR-Mediated Pathways

(2015) J. Rios-Doria et al.   MOLECULAR CANCER THERAPEUTICS

Design of selective TACE inhibitors using molecular docking studies: Synthesis and preliminary evaluation of anti-inflammatory and TACE inhibitory activity

(2015) A.P. Sarkate et al.   SAR AND QSAR IN ENVIRONMENTAL RESEARCH

Embelin inhibits TNF-α converting enzyme and cancer cell metastasis: molecular dynamics and experimental evidence

(2014) Jaspreet Kaur Dhanjal et al.   BMC CANCER

Involvement of TACE in colon inflammation: A novel mechanism of regulation via SIRT-1 activation

(2014) Manoranjan Sharma et al.   CYTOKINE

Synthesis of [3H], [13C3,15N], and [14C]SCH 900567: an inhibitor of TNF-α(tumor necrosis factor alpha) converting enzyme (TACE)

(2014) Sumei Ren et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Virtual screening-based identification of lead molecules as selective TACE inhibitors

(2014) Prashant R. Murumkar et al.   MEDICINAL CHEMISTRY RESEARCH

The P2/P2′ sites affect the substrate cleavage of TNF-α converting enzyme (TACE)

(2014) Sen Liu et al.   MOLECULAR IMMUNOLOGY

Development of a ‘mouse and human cross-reactive’ affinity-matured exosite inhibitory human antibody specific to TACE (ADAM17) for cancer immunotherapy

(2014) Hang Fai Kwok et al.   PROTEIN ENGINEERING DESIGN & SELECTION

Selective Arylsulfonamide Inhibitors of ADAM-17: Hit Optimization and Activity in Ovarian Cancer Cell Models

(2013) Elisa Nuti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Three-dimensional quantitative structure–activity relationship CoMFA/CoMSIA on pyrrolidine-based tartrate diamides as TACE inhibitors

(2013) Prashant R. Murumkar et al.   MEDICINAL CHEMISTRY RESEARCH

The conformational landscape of tartrate-based inhibitors of the TACE enzyme as revealed by Hamiltonian Replica Exchange simulation

(2013) Carlo Guardiani et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Chemical–physical analysis of a tartrate model compound for TACE inhibition

(2013) Martina Banchelli et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Discovery of Selective Small Molecular TACE Inhibitors for the Treatment of Rheumatoid Arthritis

(2012) N. -G. Li et al.   CURRENT MEDICINAL CHEMISTRY

Novel methods and strategies in the discovery of TACE inhibitors

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

2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors

(2011) Chaoyang Dai et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacophore Modelling: A Forty Year Old Approach and its Modern Synergies

(2011) F. Caporuscio et al.   CURRENT MEDICINAL CHEMISTRY

Toward in silico structure-based ADMET prediction in drug discovery

(2011) Gautier Moroy et al.   DRUG DISCOVERY TODAY

Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE

(2011) Prabal Sengupta et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Embelin reduces cutaneous TNF-α level and ameliorates skin edema in acute and chronic model of skin inflammation in mice

(2011) G. Kalyan Kumar et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Definition of peptide inhibitors from a synthetic peptide library by targeting gelatinase B/matrix metalloproteinase-9 (MMP-9) and TNF-α converting enzyme (TACE/ADAM-17)

(2011) Zheng Qiu et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

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

Determination of structural requirements of influenza neuraminidase type A inhibitors and binding interaction analysis with the active site of A/H1N1 by 3D-QSAR CoMFA and CoMSIA modeling

(2011) Prashant R. Murumkar et al.   MedChemComm

Discovery and SAR of hydantoin TACE inhibitors

(2010) Wensheng Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Biaryl substituted hydantoin compounds as TACE inhibitors

(2010) Wensheng Yu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure and activity relationships of tartrate-based TACE inhibitors

(2010) Dansu Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development of predictive pharmacophore model for in silico screening, and 3D QSAR CoMFA and CoMSIA studies for lead optimization, for designing of potent tumor necrosis factor alpha converting enzyme inhibitors

(2010) Prashant Revan Murumkar et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Potent Arylsulfonamide Inhibitors of Tumor Necrosis Factor-α Converting Enzyme Able to Reduce Activated Leukocyte Cell Adhesion Molecule Shedding in Cancer Cell Models

(2010) Elisa Nuti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Active Metalloproteases of the A Disintegrin And Metalloprotease (ADAM) Family: Biological Function and Structure

(2010) Theo Klein et al.   JOURNAL OF PROTEOME RESEARCH

Studies on novel 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones as potential TACE inhibitors: Design, synthesis, molecular modeling, and preliminary biological evaluation

(2009) Shirshendu DasGupta et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

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

Novel TACE inhibitors in drug discovery: a review of patented compounds

(2009) Prashant R Murumkar et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Molecular modeling and biological effects of peptidomimetic inhibitors of TACE activity

(2009) Wen-fang Feng et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

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

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

Current perspective of TACE inhibitors: A review

(2008) Shirshendu DasGupta et al.   BIOORGANIC & MEDICINAL CHEMISTRY

3D-Quantitative Structure–Activity Relationship Studies on Benzothiadiazepine Hydroxamates as Inhibitors of Tumor Necrosis Factor-α Converting Enzyme

(2008) Prashant R. Murumkar et al.   Chemical Biology & Drug Design

Development of Predictive 3D-QSAR CoMFA and CoMSIA Models for β-aminohydroxamic Acid-Derived Tumor Necrosis Factor-α Converting Enzyme Inhibitors

(2008) Prashant R. Murumkar et al.   Chemical Biology & Drug Design

Progress in the Development of Matrix Metalloproteinase Inhibitors

(2008) GuoGang Tu et al.   CURRENT MEDICINAL CHEMISTRY

Prodrugs: design and clinical applications

(2008) Jarkko Rautio et al.   NATURE REVIEWS DRUG DISCOVERY

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

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

An expeditious one-pot synthesis of 1,6-dideoxy-N-alkylated nojirimycin derivatives and their inhibitory effects on the secretion of IFN-γ and IL-4

(2007) Jian Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones

(2007) Upul K. Bandarage et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS