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List of works by Hirokazu Tamamura

A CD4 mimic as an HIV entry inhibitor: pharmacokinetics.

scientific article published on 17 October 2013

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

scientific article published on October 2008

A minimally cytotoxic CD4 mimic as an HIV entry inhibitor

scientific article published on 30 November 2015

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

scientific article

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

scientific article published on 28 March 2002

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

scientific article published on 13 January 2012

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

scientific article published on 15 May 2015

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

scientific article

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

scientific article published on 23 August 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

scientific article published on 01 August 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

scientific article published on 10 February 2011

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

scientific article

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.

scientific article published on 7 March 2013

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

scientific article published on 3 August 2010

CD4 mimics targeting the mechanism of HIV entry

scientific article

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

scientific article

CXCR4 engagement promotes dendritic cell survival and maturation

scientific article published on 30 July 2007

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

scientific article published on 21 September 2013

Cell-permeable stapled peptides based on HIV-1 integrase inhibitors derived from HIV-1 gene products

scientific article published on 15 August 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

scientific article published on May 2002

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

scientific article published on 28 September 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).

scientific article published in September 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

scientific article

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

scientific article

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

scientific article published on 18 October 2005

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

scientific article published on 26 July 2016

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.

scientific article published on 12 May 2006

Development of anti-HIV agents based on chemical biology

scientific article

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

scientific article

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

scientific article

Development of chemokine receptor CXCR4 antagonists using bio-mimetic strategy

scientific article published in January 2009

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

scientific article published in January 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

scientific article

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

scientific article published on 15 January 2008

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

scientific article published on 01 April 2002

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

scientific article published on 01 April 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.

scientific article published in August 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.

scientific article published on 29 December 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

scientific article published on 8 February 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

scientific article published on 4 April 2017

Efficient and orthogonal transcription regulation by chemically inducible artificial transcription factors

scientific article published on 02 November 2018

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

scientific article published on March 2005

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

scientific article

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

scientific article published on November 2003

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

scientific article

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.

scientific article published on 10 February 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

scientific article

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

scientific article

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

scientific article

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

scientific article published in January 2009

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

scientific article

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

scientific article published on 20 May 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

scientific article published on 11 September 2013

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

scientific article

HIV protease inhibitor nelfinavir inhibits replication of SARS-associated coronavirus

scientific article published in June 2004

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

scientific article published in March 2006

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

scientific article published on 24 March 2011

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

scientific article published in July 2004

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

scientific article published on June 2006

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

scientific article

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

scientific article published in June 2010

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

scientific article

Intense blue fluorescence in a leucine zipper assembly

scientific article published on 8 February 2011

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

scientific article published on May 1, 2003

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

scientific article published on 4 February 2014

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

scientific article published on 4 September 2003

Low-molecular-weight CXCR4 ligands with variable spacers.

scientific article

Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization

scientific article published on 2 February 2017

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

scientific article published on 12 December 2007

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

scientific article published in July 2003

Multimerized CHR-derived peptides as HIV-1 fusion inhibitors

scientific article published on 5 June 2013

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

scientific article

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

scientific article published on January 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 alpha,beta-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

scientific article published on 01 May 1997

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

scientific article

Peptide-based ligand screening and functional analysis of protein kinase C.

scientific article

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

scientific article

Peptidomimetic-based medicinal chemistry

scientific article published on June 2010

Pharmacophore-based small molecule CXCR4 ligands.

scientific article

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

scientific article published on 31 March 2008

Rapid hematopoietic progenitor mobilization by sulfated colominic acid

scientific article

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

scientific article published on April 24, 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

scientific article published in August 2002

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

scientific article published on April 2010

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

scientific article published in August 2002

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

scientific article

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

scientific article published on October 1, 2003

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

scientific article published on 2 March 2016

Screening for protein kinase C ligands using fluorescence resonance energy transfer

scientific article

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

scientific article published in March 2004

Small molecular CD4 mimics as HIV entry inhibitors

scientific article published on 29 September 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.

scientific article

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

scientific article published on 17 February 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

scientific article published on 01 May 2006

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

scientific article published on 17 August 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.

scientific article

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.

scientific article published in January 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

scientific article

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

scientific article

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

scientific article published on 20 July 2009

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

scientific article

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

scientific article

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

scientific article published on March 2002

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

scientific article published on 27 December 2017

Synthesis of hydrophilic caged DAG-lactones for chemical biology applications

scientific article published on 20 May 2020

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

scientific article published on November 2003

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

scientific article published in July 2003

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

scientific article

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

scientific article

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

scientific article published on 01 August 2003

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

scientific article published on 21 October 2019

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

scientific article published on September 2006

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

scientific article published on 04 April 2011

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

scientific article published on 19 April 2006

The successes and failures of HIV drug discovery

scientific article published on 02 September 2011

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

scientific article

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

scientific article

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

scientific article published on January 2007

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

scientific article published on 23 March 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

scientific article published on June 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.

scientific article published on 15 October 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]

scientific article published on 01 May 2010

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