PMID

Data

Article Title

Organization

Influence of chain length on the activity of tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4).

University of Bergen

Synthesis and evaluation of 2,5 and 2,6 pyridine-based CXCR4 inhibitors.

Georgia State University

Structure-Activity Relationship and Signaling of New Chimeric CXCR4 Agonists.

Universit£

Exploring the N-Terminal Region of C-X-C Motif Chemokine 12 (CXCL12): Identification of Plasma-Stable Cyclic Peptides As Novel, Potent C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonists.

Second University of Naples

Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.

Shandong University

Discovery of non-peptide small molecular CXCR4 antagonists as anti-HIV agents: Recent advances and future opportunities.

Shandong University

Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands.

Tokyo Medical and Dental University

Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.

National Health Research Institutes

Discovery of novel N-aryl piperazine CXCR4 antagonists.

Emory Institute For Drug Development

Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.

Emory University

Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4).

Uit The Arctic University of Norway

Development of novel CXC chemokine receptor 7 (CXCR7) ligands: selectivity switch from CXCR4 antagonists with a cyclic pentapeptide scaffold.

Kyoto University

Toward fluorescent probes for G-protein-coupled receptors (GPCRs).

Shandong University

Discovery of tetrahydroisoquinoline-based CXCR4 antagonists.

Emory University

Improved guanide compounds which bind the CXCR4 co-receptor and inhibit HIV-1 infection.

Montana State University

Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes.

Kyoto University

Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.

Universite£

Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo.

TBA

Rational design of conformationally constrained cyclopentapeptide antagonists for C-x-C chemokine receptor 4 (CXCR4).

University of Troms£

Chemokine receptor antagonists.

National Heart and Lung Institute

Noncyclam tetraamines inhibit CXC chemokine receptor type 4 and target glioma-initiating cells.

Universitat Ramon Llull

Potent CXCR4 antagonists containing amidine type Peptide bond isosteres.

TBA

Structure-activity relationship study of a CXC chemokine receptor type 4 antagonist, FC131, using a series of alkene dipeptide isosteres.

Kyoto University

Agonists for the Chemokine Receptor CXCR4.

TBA

Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.

Ono Pharmaceutical

Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.

Anormed

Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.

Kyoto University

Molecular modeling study of cyclic pentapeptide CXCR4 antagonists: new insight into CXCR4-FC131 interactions.

Pharmadesign

Design, synthesis, and functionalization of dimeric peptides targeting chemokine receptor CXCR4.

Technische Universit£T M£Nchen

Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.

Ono Pharmaceutical

Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.

Emory University

Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Genzyme

The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100.

National Institute of Infectious Diseases

Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.

Genzyme

CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist.

Tokyo Medical and Dental University

Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.

Glaxosmithkline

Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.

Glaxosmithkline

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Genzyme

Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.

Glaxosmithkline

Spiropiperidine CCR5 antagonists.

Roche Palo Alto

Identification of a new class of small molecule C5a receptor antagonists.

Wyeth Research

64Cu-AMD3100--a novel imaging agent for targeting chemokine receptor CXCR4.

National Institute of Biomedical Imaging and Bioengineering

Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.

Novartis Institutes For Biomedical Research

Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.

Roche Palo Alto

Identification of novel non-peptide CXCR4 antagonists by ligand-based design approach.

Kyoto University

Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.

Université

Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.

University of Copenhagen

Discovery of small molecule CXCR4 antagonists.

Emory University

Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone functionalities.

Kyoto University

A fragment integrational approach to GPCR inhibition: Identification of a high affinity small molecule CXCR4 antagonist.

Tsinghua University

Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds.

Kyoto University

Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131.

Kyoto University

Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.

Emory University

Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.

University of Michigan

Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.

Soochow University

Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.

Virginia Commonwealth University

Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.

University of Florida

Structural optimization of aminopyrimidine-based CXCR4 antagonists.

Soochow University

Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239.

Idorsia Pharmaceuticals

Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.

Virginia Commonwealth University

Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety.

Kyoto University

Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.

Merck Research Laboratories

Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.

Merck Research Laboratories

Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel ?-Arrestin Antagonist Activity.

Pfizer

Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma.

Sanford Burnham Prebys Medical Discovery Institute

Design, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4.

Upstate Medical University

High affinity CXCR4 inhibitors generated by linking low affinity peptides.

University of California San Diego

Tetrahydroisoquinoline CXCR4 Antagonists Adopt a Hybrid Binding Mode within the Peptide Subpocket of the CXCR4 Receptor.

Emory University

Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.

Griffin Discoveries

Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands.

Tokyo Medical and Dental University (Tmdu)

The discovery and optimization of a series of 2-aminobenzoxazole derivatives as ChemR23 inhibitors.

Kyowa Kirin

Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.

Glaxosmithkline

HIV-1 X4 activities of polycationic "viologen" based dendrimers by interaction with the chemokine receptor CXCR4: study of structure-activity relationship.

University of Osnabr£Ck

The chemical diversity and structure-based evolution of non-peptide CXCR4 antagonists with diverse therapeutic potential.

Central South University

Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists.

Soochow University

Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties.

Emory University

Insight into structural requirements for selective and/or dual CXCR3 and CXCR4 allosteric modulators.

University of Ljubljana

Discovery of

Emory University

Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.

Emory University

Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists.

Emory University

An update on small molecules targeting CXCR4 as starting points for the development of anti-cancer therapeutics.

University of Calabria

Discovery of Tetrahydroisoquinoline-Containing CXCR4 Antagonists with Improved in Vitro ADMET Properties.

Emory University

Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

Pfizer

Structure-Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3).

Kyoto University

Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.

Gsk Pharmaceuticals R & D

Structure-Activity Relationships and Biological Characterization of a Novel, Potent, and Serum Stable C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonist.

University of Campania

Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.

National Health Research Institutes

Ligand-Based NMR Study of C-X-C Chemokine Receptor Type 4 (CXCR4)-Ligand Interactions on Living Cancer Cells.

Universit£