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A CD4 mimic as an HIV entry inhibitor: pharmacokinetics.

artículo científico publicado en 2013

A future perspective on the development of chemokine receptor CXCR4 antagonists.

artículo científico

A minimally cytotoxic CD4 mimic as an HIV entry inhibitor

artículo científico publicado en 2015

A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor

artículo científico publicado en 2009

A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists

artículo científico publicado en 2002

A synthetic C34 trimer of HIV-1 gp41 shows significant increase in inhibition potency.

artículo científico publicado en 2012

An in-cell fluorogenic Tag-probe system for protein dynamics imaging enabled by cell-penetrating peptides

artículo científico publicado en 2015

Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins.

artículo científico publicado en 2015

Anti-HIV-1 peptide derivatives based on the HIV-1 Co-receptor CXCR4.

artículo científico publicado en 2013

Application of samarium diiodide (SmI2)-induced reduction of γ-acetoxy-α,β-enoates with α-specific kinetic electrophilic trapping for the synthesis of amino acid derivatives

artículo científico publicado en 2003

Application of tri- and tetrasubstituted alkene dipeptide mimetics to conformational studies of cyclic RGD peptides

article published in 2006

Azamacrocyclic metal complexes as CXCR4 antagonists

artículo científico publicado en 2011

Bioluminescence resonance energy transfer reveals ligand-induced conformational changes in CXCR4 homo- and heterodimers.

artículo científico publicado en 2005

Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells

scientific article published on 25 October 2010

CD4 mimics as HIV entry inhibitors: lead optimization studies of the aromatic substituents.

artículo científico publicado en 2013

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

artículo científico publicado en 2010

CD4 mimics targeting the mechanism of HIV entry

artículo científico publicado en 2009

CXCL12-CXCR4 engagement is required for migration of cutaneous dendritic cells

artículo científico publicado en 2007

CXCR4 engagement promotes dendritic cell survival and maturation

scientific article published on 30 July 2007

CXCR4-derived synthetic peptides inducing anti-HIV-1 antibodies.

artículo científico publicado en 2013

Cell-Permeable Stapled Peptides Based on HIV-1 Integrase Inhibitors Derived from HIV-1 Gene Products

artículo científico publicado el 15 de agosto de 2013

Certification of the critical importance of L-3-(2-naphthyl)alanine at position 3 of a specific CXCR4 inhibitor, T140, leads to an exploratory performance of its downsizing study

artículo científico publicado en 2002

Chemokine receptor expression in EBV-associated lymphoproliferation in hu/SCID mice: implications for CXCL12/CXCR4 axis in lymphoma generation.

artículo científico publicado en 2004

Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).

artículo científico publicado en 2004

Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones

artículo científico publicado en 2004

Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins.

artículo científico publicado en 2012

Corrigendum to “conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity”: [Bioorg. Med. Chem. Lett. 11 (2001) 359]

article

Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR

scientific article published on 31 May 2018

Design and synthesis of downsized metastin (45-54) analogs with maintenance of high GPR54 agonistic activity

artículo científico publicado en 2005

Development and validation of a cell-based assay system to assess human immunodeficiency virus type 1 integrase multimerization

artículo científico publicado en 2016

Development of Anti-HIV Agents Based on Chemical Biology

artículo científico publicado el 1 de enero de 2012

Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors

scientific article published on 02 May 2006

Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands

scientific article published on 11 April 2019

Development of a linear type of low molecular weight CXCR4 antagonists based on T140 analogs.

artículo científico publicado en 2006

Development of anti-HIV agents targeting dynamic supramolecular mechanism: entry and fusion inhibitors based on CXCR4/CCR5 antagonists and gp41-C34-remodeling peptides

artículo científico publicado en 2005

Development of anti-HIV peptides based on a viral capsid protein

artículo científico publicado en 2016

Development of chemokine receptor CXCR4 antagonists using bio-mimetic strategy

artículo científico publicado en 2009

Development of crosslink-type tag-probe pairs for fluorescent imaging of proteins.

artículo científico publicado en 2010

Development of low molecular weight CXCR4 antagonists by exploratory structural tuning of cyclic tetra- and pentapeptide-scaffolds towards the treatment of HIV infection, cancer metastasis and rheumatoid arthritis

artículo científico publicado en 2007

Development of peptide-targeted lipoplexes to CXCR4-expressing rat glioma cells and rat proliferating endothelial cells

artículo científico publicado en 2008

Diastereoselective Synthesis of ψ[(E)-CHCMe]- and ψ[(Z)-CHCMe]-Type Dipeptide Isosteres by Organocopper-Mediatedanti-SN2‘ Reaction

artículo científico publicado en 2002

Diastereoselective Synthesis ofψ[(E)-CMeCH]- andψ[(E)-CMeCMe]- Type Dipeptide Isosteres Based on Organocopper-Mediatedanti-SN2‘ Reaction

artículo científico publicado en 2002

Diastereoselective synthesis of new psi[(E)-CH=CMe]- and psi[(Z)-CH=CMe]-type alkene dipeptide isosteres by organocopper reagents and application to conformationally restricted cyclic RGD peptidomimetics.

artículo científico publicado en 2002

Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors

scientific article published on 04 July 2019

Direct assessment of CXCR4 mutant conformations reveals complex link between receptor structure and G(alpha)(i) activation.

artículo científico publicado en 2006

Effects of DNA binding of the zinc finger and linkers for domain fusion on the catalytic activity of sequence-specific chimeric recombinases determined by a facile fluorescent system

artículo científico publicado en 2012

Effects of replacement and addition of an amino acid contained in a cyclic peptide corresponding to a β-hairpin loop sequence of human EGF receptor

artículo científico publicado en 2017

Efficient and orthogonal transcription regulation by chemically inducible artificial transcription factors

artículo científico publicado en 2018

Elevated serum levels of stromal-derived factor-1alpha are associated with increased osteoclast activity and osteolytic bone disease in multiple myeloma patients.

artículo científico publicado en 2005

Enhanced exposure of human immunodeficiency virus type 1 primary isolate neutralization epitopes through binding of CD4 mimetic compounds

artículo científico publicado en 2010

Enhancement of the T140-based pharmacophores leads to the development of more potent and bio-stable CXCR4 antagonists

artículo científico publicado en 2003

Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines.

artículo científico publicado en 2012

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

scientific article published on 28 September 2015

Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing.

artículo científico publicado en 2008

Facile access to (Z)-alkene-containing diketopiperazine mimetics utilizing organocopper-mediated anti-SN2′ reactions

Facile synthesis of membrane-embedded peptides utilizing lipid bilayer-assisted chemical ligation

artículo científico publicado en 2004

Fluorescence-quenching screening of protein kinase C ligands with an environmentally sensitive fluorophore.

artículo científico publicado en 2011

Fluorescent-responsive synthetic C1b domains of protein kinase Cδ as reporters of specific high-affinity ligand binding

artículo científico publicado en 2010

Fluorogenically active leucine zipper peptides as tag-probe pairs for protein imaging in living cells

artículo científico publicado en 2009

Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening

artículo científico publicado en 2008

Functional evaluation of fluorescein-labeled derivatives of a peptide inhibitor of the EGF receptor dimerization

artículo científico publicado en 2016

Generation of a replication-competent simian-human immunodeficiency virus, the neutralization sensitivity of which can be enhanced in the presence of a small-molecule CD4 mimic

artículo científico publicado en 2013

Germinal center dark and light zone organization is mediated by CXCR4 and CXCR5.

artículo científico publicado en 2004

HIV protease inhibitor nelfinavir inhibits replication of SARS-associated coronavirus

artículo científico publicado en 2004

HIV-1 gp120 enhances giant depolarizing potentials via chemokine receptor CXCR4 in neonatal rat hippocampus

artículo científico publicado en 2006

HIV‐1 gp120 enhances outward potassium current via CXCR4 and cAMP‐dependent protein kinase a signaling in cultured rat microglia

artículo científico publicado el 24 de marzo de 2011

Identification of a CXCR4 antagonist, a T140 analog, as an anti-rheumatoid arthritis agent

artículo científico publicado en 2004

Identification of a new class of low molecular weight antagonists against the chemokine receptor CXCR4 having the dipicolylamine-zinc(II) complex structure.

artículo científico publicado en 2006

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

artículo científico publicado en 2005

Induction of myogenic differentiation by SDF-1 via CXCR4 and CXCR7 receptors.

artículo científico publicado en 2010

Inhibitory effect of newly developed CXC-chemokine receptor 4 antagonists on the infection with feline immunodeficiency virus

artículo científico publicado en 2009

Intense blue fluorescence in a leucine zipper assembly

artículo científico publicado en 2011

Involvement of CD44 in induction of matrix metalloproteinases by a COOH‐terminal heparin‐binding fragment of fibronectin in human articular cartilage in culture

artículo científico publicado el 1 de mayo de 2003

Isostere-based design of 8-azacoumarin-type photolabile protecting groups: a hydrophilicity-increasing strategy for coumarin-4-ylmethyls

artículo científico publicado en 2014

Lipid bilayer simulations of CXCR4 with inverse agonists and weak partial agonists

artículo científico publicado en 2003

Low-molecular-weight CXCR4 ligands with variable spacers.

artículo científico publicado en 2012

Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization

artículo científico publicado en 2017

Modulation of network-driven, GABA-mediated giant depolarizing potentials by SDF-1alpha in the developing hippocampus

artículo científico publicado en 2007

Molecular-size reduction of a potent CXCR4-chemokine antagonist using orthogonal combination of conformation- and sequence-based libraries

artículo científico publicado en 2003

Multimerized CHR-derived peptides as HIV-1 fusion inhibitors

artículo científico publicado el 5 de junio de 2013

Multimerized HIV-gp41-derived peptides as fusion inhibitors and vaccines

artículo científico publicado en 2015

Mutations conferring resistance to human immunodeficiency virus type 1 fusion inhibitors are restricted by gp41 and Rev-responsive element functions

artículo científico publicado en 2005

New access to α-substituted (Z)-fluoroalkene dipeptide isosteres utilizing organocopper reagents under ‘reduction–oxidative alkylation (R–OA)’ conditions

article published in 2001

Palladium(0)-Catalyzed Isomerization Reactions of Aziridines Bearing an α,β-Unsaturated Ester Group: A Thermodynamic Preference for Chiral Alkyl (2E)-4,5-cis-4,5-Epimino-N-(alkyl- or arylsulfonyl) 2-Enoates over the Other Three Stereoisomers

artículo científico publicado el 2 de mayo de 1997

Peptide HIV-1 integrase inhibitors from HIV-1 gene products.

artículo científico publicado en 2010

Peptide‐based ligand screening and functional analysis of protein kinase C

artículo científico publicado el 1 de noviembre de 2013

Peptidic HIV integrase inhibitors derived from HIV gene products: structure-activity relationship studies.

artículo científico publicado en 2010

Peptidomimetic-based medicinal chemistry

artículo científico publicado en 2010

Pharmacophore-based small molecule CXCR4 ligands.

artículo científico publicado en 2012

Photolabile protection for one-pot sequential native chemical ligation

scientific article published on 01 November 2005

Potent synergistic anti-human immunodeficiency virus (HIV) effects using combinations of the CCR5 inhibitor aplaviroc with other anti-HIV drugs

artículo científico publicado en 2008

Rapid hematopoietic progenitor mobilization by sulfated colominic acid

artículo científico publicado en 2007

Reduction of Peptide Character of HIV Protease Inhibitors That Exhibit Nanomolar Potency against Multidrug Resistant HIV-1 Strains

artículo científico publicado el 24 de abril de 2003

Regio- and stereoselective ring-opening of chiral 1,3-oxazolidin-2-one derivatives by organocopper reagents provides novel access to di-, tri- and tetra-substituted alkene dipeptide isosteresElectronic supplementary information (ESI) available: synth

Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-S(N)2' reactions

artículo científico publicado en 2002

Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies.

artículo científico publicado en 2010

Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells

artículo científico publicado en 2002

Retrograde migration of pectoral girdle muscle precursors depends on CXCR4/SDF-1 signaling

artículo científico publicado en 2014

Role of CXCR4 and SDF-1 in Mammary Tumor Metastasis in the Cat

artículo científico publicado el 1 de octubre de 2003

SDF-1 controls the muscle and blood vessel formation of the somite

artículo científico publicado en 2016

Screening for protein kinase C ligands using fluorescence resonance energy transfer

artículo científico publicado en 2014

SmI2-mediated reduction of gamma,gamma-difluoro-alpha,beta-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipeptide isosteres

artículo científico publicado en 2004

Small molecular CD4 mimics as HIV entry inhibitors

artículo científico publicado el 29 de septiembre de 2011

Small peptide inhibitors of the CXCR4 chemokine receptor (CD184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells.

artículo científico publicado en 2005

Small-Molecule CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors

artículo científico publicado en 2016

Specific probes for chemokine receptors

scientific article published on 01 January 2006

Stereoselective Synthesis of 3,6-Disubstituted-3,6-dihydropyridin-2-ones as Potential Diketopiperazine Mimetics Using Organocopper-Mediatedanti-SN2‘ Reactions and Their Use in the Preparation of Low-Molecule CXCR4 Antagonists

artículo científico publicado en 2006

Stereoselective formation of trisubstituted (Z)-chloroalkenes adjacent to a tertiary carbon stereogenic center by organocuprate-mediated reduction/alkylation

artículo científico publicado en 2012

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.

artículo científico publicado en 2005

Stereoselective synthesis of a set of two functionalized (E)-alkene dipeptide isosteres of L-amino acid-L-Glu and L-amino acid-D-Glu

Stereoselective synthesis of peptidomimetics based on acid-catalyzed ring-opening of beta-aziridinyl-alpha,beta-enoates.

artículo científico publicado en 2009

Stromal cell-derived factor 1-mediated CXCR4 signaling in rat and human cortical neural progenitor cells

scientific journal article

Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

artículo científico publicado en 2005

Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore

artículo científico publicado en 2008

Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids

artículo científico publicado en 2009

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

artículo científico publicado en 2007

Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands.

artículo científico publicado en 2017

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

artículo científico publicado en 2002

Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application

artículo científico publicado en 2017

Synthesis of hydrophilic caged DAG-lactones for chemical biology applications

artículo científico publicado en 2020

Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives

artículo científico publicado en 2003

Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies

artículo científico publicado en 2003

Synthesis of protein kinase Cdelta C1b domain by native chemical ligation methodology and characterization of its folding and ligand binding.

artículo científico publicado en 2009

Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C.

artículo científico publicado en 2011

T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer

artículo científico publicado en 2003

TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases

artículo científico publicado en 2019

The chemokine receptor CXCR4 as a therapeutic target for several diseases.

artículo científico publicado en 2006

The increase in surface CXCR4 expression on lung extravascular neutrophils and its effects on neutrophils during endotoxin-induced lung injury.

artículo científico publicado en 2011

The involvement of stromal derived factor 1alpha in homing and progression of multiple myeloma in the 5TMM model.

artículo científico publicado en 2006

The successes and failures of HIV drug discovery

artículo científico publicado el 2 de septiembre de 2011

The therapeutic potential of CXCR4 antagonists in the treatment of HIV infection, cancer metastasis and rheumatoid arthritis

artículo científico publicado en 2005

The therapeutic potential of CXCR4 antagonists in the treatment of HIV.

artículo científico publicado en 2003

Therapeutic potential of the chemokine receptor CXCR4 antagonists as multifunctional agents.

artículo científico publicado el 1 de enero de 2007

Topochemical exploration of potent compounds using retro-enantiomer libraries of cyclic pentapeptides

artículo científico publicado en 2004

Trivalent ligands for CXCR4 bearing polyproline linkers show specific recognition for cells with increased CXCR4 expression

scientific article published on 17 July 2015

Two orthogonal approaches to overcome multi-drug resistant HIV-1s: development of protease inhibitors and entry inhibitors based on CXCR4 antagonists

artículo científico publicado en 2004

Unequivocal Synthesis of (Z)-Alkene or (E)-Fluoroalkene Dipeptide Isosteres via DKP Mimetics to Probe Structural Requirements of Peptide Transporter

Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-Type Photolabile Protecting Group.

artículo científico publicado en 2015

Versatile use of acid-catalyzed ring-opening of β-aziridinyl-α,β-enoates to stereoselective synthesis of peptidomimetics

[Development of site-specific DNA methylase for epigenetic regulation of gene expression]

artículo científico publicado en 2010