Polythiazole linkers as functional rigid connectors: a new RGD cyclopeptide with enhanced integrin selectivity

Pharmacophoric Modifications Lead to Superpotent αvβ3 Integrin Ligands with Suppressed α5β1 Activity

(2014) Stefanie Neubauer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benefits of NOPO As Chelator in Gallium-68 Peptides, Exemplified by Preclinical Characterization of 68Ga-NOPO–c(RGDfK)

(2014) Jakub Šimeček et al.   MOLECULAR PHARMACEUTICS

Selective Imaging of the Angiogenic Relevant Integrins α5β1 and αvβ3

(2013) Stefanie Neubauer et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Newi,i + 3 Peptide Stapling System for α-Helix Stabilization

(2013) So Youn Shim et al.   Chemical Biology & Drug Design

Biselectivity of isoDGR Peptides for Fibronectin Binding Integrin Subtypes α5β1 and αvβ6: Conformational Control through Flanking Amino Acids

(2013) Alexander Bochen et al.   JOURNAL OF MEDICINAL CHEMISTRY

2012 FDA drug approvals

(2013) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Synthesis of heteroglycoclusters by using orthogonal chemoselective ligations

(2012) Baptiste Thomas et al.   Beilstein Journal of Organic Chemistry

A comparative study of backbone versus side chain peptide cyclization: Application for HIV-1 integrase inhibitors

(2012) Zvi Hayouka et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Cyclic RGD Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds as New Potent Integrin Ligands

(2012) Mattia Marchini et al.   CHEMISTRY-A EUROPEAN JOURNAL

Therapeutic peptides

(2012) Fernando Albericio et al.   Future Medicinal Chemistry

125I-Radiolabeled Morpholine-Containing Arginine–Glycine–Aspartate (RGD) Ligand of αvβ3 Integrin As a Molecular Imaging Probe for Angiogenesis

(2012) Francesca Bianchini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cyclic Aza-peptide Integrin Ligand Synthesis and Biological Activity

(2012) Jochen Spiegel et al.   JOURNAL OF ORGANIC CHEMISTRY

Targeted Delivery of Insoluble Cargo (Paclitaxel) by PEGylated Chitosan Nanoparticles Grafted with Arg-Gly-Asp (RGD)

(2012) Pi-Ping Lv et al.   MOLECULAR PHARMACEUTICS

2011 FDA drug approvals

(2012) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Increasing αvβ3 Selectivity of the Anti-Angiogenic Drug Cilengitide by N-Methylation

(2011) Carlos Mas-Moruno et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation

(2011) Carlos Mas-Moruno et al.   Anti-Cancer Agents in Medicinal Chemistry

Oxorhenium-Mediated Assembly of Noncyclic Selective Integrin Antagonists: A Combinatorial Approach

(2011) Marie Aufort et al.   CHEMBIOCHEM

Peptides and Proteins as a Continuing Exciting Source of Inspiration for Peptidomimetics

(2011) Rob M. J. Liskamp et al.   CHEMBIOCHEM

2010 FDA drug approvals

(2011) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Cu(I)- and Ru(II)-Mediated “Click” Cyclization of Tripeptides Toward Vancomycin-Inspired Mimics

(2011) Jinqiang Zhang et al.   ORGANIC LETTERS

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

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

Synthesis of cRGD-peptide conjugated near-infrared CdTe/ZnSe core–shell quantum dots for in vivo cancer targeting and imaging

(2010) Ken-Tye Yong et al.   CHEMICAL COMMUNICATIONS

Orthogonally Protected Thiazole and Isoxazole Diamino Acids: An Efficient Synthetic Route

(2010) Jeffrey D. Butler et al.   CHEMISTRY-A EUROPEAN JOURNAL

Targeting αvβ3 Integrin: Design and Applications of Mono- and Multifunctional RGD-Based Peptides and Semipeptides

(2010) L. Auzzas et al.   CURRENT MEDICINAL CHEMISTRY

2009 FDA drug approvals

(2010) Bethan Hughes   NATURE REVIEWS DRUG DISCOVERY

N-terminus 4-chloromethyl thiazole peptide as a macrocyclization tool in the synthesis of cyclic peptides: application to the synthesis of conformationally constrained RGD-containing integrin ligands

(2010) Adel Nefzi et al.   TETRAHEDRON LETTERS

Ligands for Mapping αvβ3-Integrin Expression in Vivo

(2009) Margret Schottelius et al.   ACCOUNTS OF CHEMICAL RESEARCH

The Transmembrane Structure of Integrin αIIbβ3: Significance for Signal Transduction

(2009) Martin Hoefling et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cyclic RGD-Peptidomimetics Containing Bifunctional Diketopiperazine Scaffolds as New Potent Integrin Ligands

(2009) Ana Sofia M. da Ressurreição et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis of chemically modified bioactive peptides: recent advances, challenges and developments for medicinal chemistry

(2009) Soledad Royo Gracia et al.   Future Medicinal Chemistry

Muscarine, imidazole, oxazole and thiazole alkaloids

(2009) Zhong Jin   NATURAL PRODUCT REPORTS

Inhibition of HIV-1 Fusion by Hydrogen-Bond-Surrogate-Based α Helices

(2008) Deyun Wang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Synthesis and Conformational Analysis of a Cyclic Peptide Obtained viaitoi+4 Intramolecular Side-Chain to Side-Chain Azide−Alkyne 1,3-Dipolar Cycloaddition

(2008) Sonia Cantel et al.   JOURNAL OF ORGANIC CHEMISTRY

Morphing peptide backbones into heterocycles

(2008) C. T. Walsh et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA