Discovery of the first potent and selective αvβ5 integrin inhibitor based on an amide-containing core

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2020.112719 ◽

2020 ◽

Vol 208 ◽

pp. 112719

Author(s):

Rhys A. Lippa ◽

John Barrett ◽

Sandeep Pal ◽

James E. Rowedder ◽

John A. Murphy ◽

...

Keyword(s):

Integrin Inhibitor

Download Full-text

Beta 3-specific non-peptidic integrin inhibitor EMD409915 blocks PDGF-BB stimulated migration in HSC via inhibition of p38 signalling pathway

Zeitschrift für Gastroenterologie ◽

10.1055/s-2004-816040 ◽

2004 ◽

Vol 42 (01) ◽

Author(s):

E Patsenker ◽

Y Popov ◽

M Wiesner ◽

S Goodman ◽

D Schuppan

Keyword(s):

Signalling Pathway ◽

Integrin Inhibitor

Download Full-text

A phase I, dose escalation, pharmacodynamic, pharmacokinetic, and food-effect study of α2 integrin inhibitor E7820 in patients with advanced solid tumors

Investigational New Drugs ◽

10.1007/s10637-016-0344-9 ◽

2016 ◽

Vol 34 (3) ◽

pp. 329-337 ◽

Author(s):

B. Milojkovic Kerklaan ◽

S. Slater ◽

M. Flynn ◽

A. Greystoke ◽

P. O. Witteveen ◽

...

Keyword(s):

Phase I ◽

Solid Tumors ◽

Dose Escalation ◽

Food Effect ◽

Effect Study ◽

Advanced Solid Tumors ◽

Integrin Inhibitor

Download Full-text

Effects of natalizumab, an α4 integrin inhibitor, on fertility in male and female guinea pigs

Birth Defects Research Part B Developmental and Reproductive Toxicology ◽

10.1002/bdrb.20191 ◽

2009 ◽

Vol 86 (2) ◽

pp. 108-116 ◽

Author(s):

Nancy G. Wehner ◽

Michael Skov ◽

George Shopp ◽

Meredith S. Rocca ◽

Janet Clarke

Keyword(s):

Guinea Pigs ◽

Male And Female ◽

Integrin Inhibitor

Download Full-text

Thermodynamic Understanding of an Aza-Michael Reaction Enables Five-Step Synthesis of the Potent Integrin Inhibitor MK-0429

The Journal of Organic Chemistry ◽

10.1021/acs.joc.1c02375 ◽

2021 ◽

Author(s):

Anya Gupta ◽

Matthew L. Condakes

Keyword(s):

Michael Reaction ◽

Integrin Inhibitor

Download Full-text

A positron emission tomography imaging study to confirm target engagement in the lungs of patients with idiopathic pulmonary fibrosis following a single dose of a novel inhaled αvβ6 integrin inhibitor

Respiratory Research ◽

10.1186/s12931-020-01339-7 ◽

2020 ◽

Vol 21 (1) ◽

Author(s):

Toby M. Maher ◽

Juliet K. Simpson ◽

Joanna C. Porter ◽

Frederick J. Wilson ◽

Robert Chan ◽

...

Keyword(s):

Positron Emission Tomography ◽

Single Dose ◽

Idiopathic Pulmonary Fibrosis ◽

Positron Emission Tomography Imaging ◽

Imaging Study ◽

Emission Tomography ◽

Target Engagement ◽

Tomography Imaging ◽

Positron Emission ◽

Integrin Inhibitor

Download Full-text

Randomized phase II study of three doses of the integrin inhibitor cilengitide versus docetaxel as second-line treatment for patients with advanced non-small-cell lung cancer

Investigational New Drugs ◽

10.1007/s10637-012-9842-6 ◽

2012 ◽

Vol 31 (1) ◽

pp. 175-182 ◽

Author(s):

Christian Manegold ◽

Johan Vansteenkiste ◽

Felipe Cardenal ◽

Wolfgang Schuette ◽

Penella J. Woll ◽

...

Keyword(s):

Lung Cancer ◽

Small Cell Lung Cancer ◽

Phase Ii ◽

Phase Ii Study ◽

Line Treatment ◽

Second Line ◽

Small Cell Lung ◽

Randomized Phase Ii ◽

Integrin Inhibitor

Download Full-text

Tyrosine modified analogues of the α4β7 integrin inhibitor biotin-R8ERY prepared via Click Chemistry: Synthesis and biological evaluation

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2012.02.035 ◽

2012 ◽

Vol 20 (8) ◽

pp. 2638-2644 ◽

Author(s):

Stefanie Papst ◽

Anaïs Noisier ◽

Margaret A. Brimble ◽

Yi Yang ◽

Geoffrey W. Krissansen

Keyword(s):

Click Chemistry ◽

Biological Evaluation ◽

Synthesis And Biological Evaluation ◽

Integrin Inhibitor

Download Full-text

An αv-RGD Integrin Inhibitor Toolbox: Drug Discovery Insight, Challenges and Opportunities

Angewandte Chemie International Edition ◽

10.1002/anie.201707948 ◽

2018 ◽

Vol 57 (13) ◽

pp. 3298-3321 ◽

Author(s):

Richard J. D. Hatley ◽

Simon J. F. Macdonald ◽

Robert J. Slack ◽

Joelle Le ◽

Steven B. Ludbrook ◽

...

Keyword(s):

Drug Discovery ◽

Challenges And Opportunities ◽

Integrin Inhibitor

Download Full-text

IS20I, a Specific ??v??3 Integrin Inhibitor, Reduces Glioma Growth in Vivo

Neurosurgery ◽

10.1097/00006123-200301000-00023 ◽

2003 ◽

Vol 52 (1) ◽

pp. 177-186 ◽

Author(s):

Lorenzo Bello ◽

Valeria Lucini ◽

Carlo Giussani ◽

Giorgio Carrabba ◽

Mauro Pluderi ◽

...

Keyword(s):

Glioma Growth ◽

Integrin Inhibitor

Download Full-text

Reduction in types I and III collagen gene expression by an alphavbeta1 integrin inhibitor correlates with a decrease in PRO-C1 and PRO-C3 levels in precision-cut liver tissue slices from cirrhotic non-alcoholic steatohepatitis patients

Journal of Hepatology ◽

10.1016/s0168-8278(20)31511-7 ◽

2020 ◽

Vol 73 ◽

pp. S517-S518

Author(s):

Johanna Schaub ◽

Steve Ho ◽

Vikram Rao ◽

Megan Marlow ◽

Eric Lefebvre ◽

...

Keyword(s):

Gene Expression ◽

Liver Tissue ◽

Collagen Gene ◽

Tissue Slices ◽

Alcoholic Steatohepatitis ◽

Collagen Gene Expression ◽

Integrin Inhibitor

Download Full-text