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

Facile synthesis of 7-alkyl-1,2,3,4-tetrahydro-1,8-naphthyridines as arginine mimetics using a Horner–Wadsworth–Emmons-based approach

(2020) Rhys A Lippa et al.   Beilstein Journal of Organic Chemistry

Selective Targeting of Integrin αvβ8 by a Highly Active Cyclic Peptide

(2019) Florian Reichart et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an Orally Bioavailable Pan αv Integrin Inhibitor for Idiopathic Pulmonary Fibrosis

(2019) Niall A. Anderson et al.   JOURNAL OF MEDICINAL CHEMISTRY

From a Helix to a Small Cycle: Metadynamics-Inspired αvβ6 Integrin Selective Ligands

(2018) Francesco Saverio Di Leva et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

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

(2018) Richard J. D. Hatley et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis

(2018) Panayiotis A. Procopiou et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins

(2017) Tobias G. Kapp et al.   Scientific Reports

Integrin-based therapeutics: biological basis, clinical use and new drugs

(2016) Klaus Ley et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis and determination of absolute configuration of a non-peptidic αvβ6 integrin antagonist for the treatment of idiopathic pulmonary fibrosis

(2016) Niall A. Anderson et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Dissociation Constants (pKa) of Tertiary and Cyclic Amines: Structural and Temperature Dependences

(2014) Aravind V. Rayer et al.   JOURNAL OF CHEMICAL AND ENGINEERING DATA

Structural determinants of integrin β-subunit specificity for latent TGF-β

(2014) Xianchi Dong et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Structure Activity Relationships of αv Integrin Antagonists for Pulmonary Fibrosis by Variation in Aryl Substituents

(2014) James Adams et al.   ACS Medicinal Chemistry Letters

Effective Treatment of Mouse Sepsis With an Inhibitory Antibody Targeting Integrin αvβ5*

(2013) George Su et al.   CRITICAL CARE MEDICINE

Target validation using chemical probes

(2013) Mark E Bunnage et al.   Nature Chemical Biology

Absence of Integrin αvβ3 Enhances Vascular Leak in Mice by Inhibiting Endothelial Cortical Actin Formation

(2011) George Su et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

A General Strategy for the Perfluoroalkylation of Arenes and Arylbromides by Using Arylboronate Esters and [(phen)CuRF]

(2011) Nichole D. Litvinas et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Integrin  v 5-Mediated TGF-  Activation by Airway Smooth Muscle Cells in Asthma

(2011) A. L. Tatler et al.   JOURNAL OF IMMUNOLOGY

Conformational Control of Integrin-Subtype Selectivity in isoDGR Peptide Motifs: A Biological Switch

(2010) Andreas O. Frank et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION