List of works - J. Fernando Díaz

A Method for the Stereoselective Construction of the Hemiaminal Center in Zampanolides

scientific article published on 12 October 2020

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.

scientific article

A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs

scientific article

A structure-based design of new C2- and C13-substituted taxanes: tubulin binding affinities and extended quantitative structure-activity relationships using comparative binding energy (COMBINE) analysis.

scientific article

Aggregated Compound Biological Signatures Facilitate Phenotypic Drug Discovery and Target Elucidation

scientific article

Antivascular and antitumor properties of the tubulin-binding chalcone TUB091

scientific article

Apo-Hsp90 coexists in two open conformational states in solution.

scientific article

Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.

scientific article published on 12 May 2007

Changes in Microtubule Protofilament Number Induced by Taxol Binding to an Easily Accessible Site

scientific article published in Journal of Biological Chemistry

Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.

scientific article published on 10 February 2018

Control of the Structural Stability of the Tubulin Dimer by One High Affinity Bound Magnesium Ion at Nucleotide N-site

scientific article published in Journal of Biological Chemistry

Corrigendum: Mechanism of Action of the Cytotoxic Macrolides Amphidinolide X and J

scholarly article published in ChemBioChem

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands ⬇️

scientific article published on 20 March 2019

Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites.

scientific article published on 7 January 2007

Cyclostreptin derivatives specifically target cellular tubulin and further map the paclitaxel site.

scientific article published on 30 December 2011

Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin.

scientific article published on 12 July 2015

Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin

scientific article published on 12 December 2014

Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules

scientific article published on 22 February 2011

Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain.

scientific article

Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop

scientific article published on 21 March 2019

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport.

scientific article

Endowing indole-based tubulin inhibitors with an anchor for derivatization: highly potent 3-substituted indolephenstatins and indoleisocombretastatins.

scientific article published on 20 March 2013

Equilibrium and kinetic study of the conformational transition toward the active state of p21Ha-ras, induced by the binding of BeF3- to the GDP-bound state, in the absence of GTPase-activating proteins

scientific article published on 01 September 1997

Fluorescent taxoid probes for microtubule research.

scientific article published on January 2010

Free Energy Profile and Kinetics Studies of Paclitaxel Internalization from the Outer to the Inner Wall of Microtubules.

scientific article published on 16 November 2012

Gallic acid sensitizes paclitaxel-resistant human ovarian carcinoma cells through an increase in reactive oxygen species and subsequent downregulation of ERK activation.

scientific article published on 18 April 2018

High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells

scientific article published on 12 August 2015

High-affinity ligands of the colchicine domain in tubulin based on a structure-guided design.

scientific article published on 9 March 2018

Identification of pyrrolopyrimidine derivative PP-13 as a novel microtubule-destabilizing agent with promising anticancer properties

scientific article published on 31 August 2017

Insights into Molecular Plasticity of Choline Binding Proteins (Pneumococcal Surface Proteins) by SAXS

article by Rubén M. Buey et al published January 2007 in Journal of Molecular Biology

Insights into nucleotide recognition by cell division protein FtsZ from a mant-GTP competition assay and molecular dynamics.

scientific article

Insights into the Interaction of Discodermolide and Docetaxel with Tubulin. Mapping the Binding Sites of Microtubule-Stabilizing Agents by Using an Integrated NMR and Computational Approach ⬇️

scientific article published on May 13, 2011

Interaction of a cyclostreptin analogue with the microtubule taxoid site: the covalent reaction rapidly follows binding.

scientific article

Low resolution structure of microtubules in solution. Synchrotron X-ray scattering and electron microscopy of taxol-induced microtubules assembled from purified tubulin in comparison with glycerol and MAP-induced microtubules

scientific article published on July 5, 1992

Macromolecular accessibility of fluorescent taxoids bound at a paclitaxel binding site in the microtubule surface.

scientific article published on 18 November 2004

Mechanism of action of the cytotoxic macrolides amphidinolide X and J.

scientific article published on 15 April 2011

Modification of C-seco taxoids through ring tethering and substituent replacement leading to effective agents against tumor drug resistance mediated by βIII-Tubulin and P-glycoprotein (P-gp) overexpressions.

scientific article published on 3 June 2017

Modulation of Microtubule Interprotofilament Interactions by Modified Taxanes ⬇️

scientific article published on December 20, 2011

Molecular Recognition of Epothilones by Microtubules and Tubulin Dimers Revealed by Biochemical and NMR Approaches

scientific article published on 25 February 2014

Molecular mechanism of action of microtubule-stabilizing anticancer agents

scientific article

Molecular mechanisms of pressure induced conformational changes in BPTI

scientific article published on 01 August 1996

Molecular recognition of taxol by microtubules. Kinetics and thermodynamics of binding of fluorescent taxol derivatives to an exposed site

scientific article published on 01 August 2000

NMR determination of the bioactive conformation of peloruside A bound to microtubules.

scientific article

New interfacial microtubule inhibitors of marine origin, PM050489/PM060184, with potent antitumor activity and a distinct mechanism.

scientific article

Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach

scientific article published on 9 May 2014

Optimization of taxane binding to microtubules: binding affinity dissection and incremental construction of a high-affinity analog of paclitaxel.

scientific article

Overcoming tumor drug resistance with high-affinity taxanes: a SAR study of C2-modified 7-acyl-10-deacetyl cephalomannines.

scientific article published on May 2007

PM060184, a new tubulin binding agent with potent antitumor activity including P-glycoprotein over-expressing tumors

scientific article

Pironetin Binds Covalently to αCys316 and Perturbs a Major Loop and Helix of α-Tubulin to Inhibit Microtubule Formation

scientific article

Possible binding site for paclitaxel at microtubule pores.

scientific article

Protein Shape and Assembly Studied with X-Ray Solution Scattering: Fundaments and Practice

Quinolin-6-Yloxyacetamides Are Microtubule Destabilizing Agents That Bind to the Colchicine Site of Tubulin.

scientific article published on 22 June 2017

Restoration of Microtubule Interaction and Cytotoxicity in D-seco Taxanes upon Incorporation of 20-Hydroxymethyl-4-allyloxy Groups

scientific article published on 09 December 2015

Self-Organization of FtsZ Polymers in Solution Reveals Spacer Role of the Disordered C-Terminal Tail.

scientific article

Solution structure of GDP-tubulin double rings to 3 nm resolution and comparison with microtubules

scientific article published on 01 April 1994

Structural Basis of Microtubule Stabilization by Discodermolide.

scientific article published on 16 February 2017

Structural and Biochemical Characterization of the Interaction of Tubulin with Potent Natural Analogues of Podophyllotoxin

scientific article published on 12 August 2016

Structural model for differential cap maturation at growing microtubule ends

scientific article published on 10 March 2020

Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents

scientific article published on 03 November 2018

Synthesis and Anti-Proliferative Activity of Sulfanyltriazolylnaphthalenols and Sulfanyltriazolylnaphthalene-1,4-diones.

scientific article published on 12 July 2016

Synthesis and biological evaluation as microtubule-active agents of several tetrahydrofuran and spiroacetal derivatives.

scientific article published on January 2013

Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation.

scientific article

Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents

scientific article

Synthesis and biological evaluation of truncated α-tubulin-binding pironetin analogues lacking alkyl pendants in the side chain or the dihydropyrone ring.

scientific article published on September 2013

Synthesis of N-acyl Derivatives of Aminocombretastatin A-4 and Study of their Interaction with Tubulin and downregulation of c-Myc

scientific article published on 19 November 2020

Synthesis of Thicolchicine-Based Conjugates: Investigation towards Bivalent Tubulin/Microtubules Binders

scientific article published on 01 January 2019

Synthesis, Biological Profiling and Determination of the Tubulin-Bound Conformation of 12-Aza-Epothilones (Azathilones).

scientific article published on 3 August 2016

Synthesis, Characterization, and Application in HeLa Cells of an NIR Light Responsive Doxorubicin Delivery System Based on NaYF4:Yb,Tm@SiO2-PEG Nanoparticles.

scientific article

Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate ⬇️

scientific article published on 05 March 2019

Synthesis, biological evaluations, and tubulin binding poses of C-2alpha sulfur linked taxol analogues

scientific article published on 14 March 2007

TRAPPII regulates exocytic Golgi exit by mediating nucleotide exchange on the Ypt31 ortholog RabERAB11.

scientific article

Taxanes with high potency inducing tubulin assembly overcome tumoural cell resistances.

scientific article

The Binding Sites of Microtubule-Stabilizing Agents ⬇️

scientific article published on March 21, 2013

The Interaction of Microtubules with Stabilizers Characterized at Biochemical and Structural Levels ⬇️

scientific article published on 01 January 2009

The Mechanism of the Interactions of Pironetin Analog/Combretastatin A-4 Hybrids with Tubulin.

scientific article published on 17 June 2015

The binding mode of side chain- and C3-modified epothilones to tubulin.

scientific article

The diamagnetic susceptibility of the tubulin dimer

scientific article published on 18 February 2014

The impact of cyclopropane configuration on the biological activity of cyclopropyl-epothilones.

scientific article

The interactions of cell division protein FtsZ with guanine nucleotides.

scientific article published on 31 October 2007

The microtubule stabilizing agent laulimalide does not bind in the taxoid site, kills cells resistant to paclitaxel and epothilones, and may not require its epoxide moiety for activity.

scientific article

The nucleotide switch of tubulin and microtubule assembly: a polymerization-driven structural change

scientific article published on 01 May 2006

Total Synthesis of Amphidinolide K, a Macrolide That Stabilizes F-Actin

scientific article published on 23 June 2015

Triazolopyrimidines Are Microtubule-Stabilizing Agents that Bind the Vinca Inhibitor Site of Tubulin

scientific article

Tubulin binding, protein-bound conformation in solution, and antimitotic cellular profiling of noscapine and its derivatives.

scientific article published on 27 February 2012

Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

scientific article published on 06 August 2020

Zampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration

scientific article

Zampanolide, a Potent New Microtubule-Stabilizing Agent, Covalently Reacts with the Taxane Luminal Site in Tubulin α,β-Heterodimers and Microtubules ⬇️

scientific article published on June 22, 2012

enterotoxins tilimycin and tilivalline have distinct host DNA-damaging and microtubule-stabilizing activities

scientific article published on 11 February 2019

List of works by J. Fernando Díaz

A Method for the Stereoselective Construction of the Hemiaminal Center in Zampanolides

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.

A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs

A structure-based design of new C2- and C13-substituted taxanes: tubulin binding affinities and extended quantitative structure-activity relationships using comparative binding energy (COMBINE) analysis.

Aggregated Compound Biological Signatures Facilitate Phenotypic Drug Discovery and Target Elucidation

Antivascular and antitumor properties of the tubulin-binding chalcone TUB091

Apo-Hsp90 coexists in two open conformational states in solution.

Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.

Changes in Microtubule Protofilament Number Induced by Taxol Binding to an Easily Accessible Site

Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.

Control of the Structural Stability of the Tubulin Dimer by One High Affinity Bound Magnesium Ion at Nucleotide N-site

Corrigendum: Mechanism of Action of the Cytotoxic Macrolides Amphidinolide X and J

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands ⬇️

Cyclostreptin binds covalently to microtubule pores and lumenal taxoid binding sites.

Cyclostreptin derivatives specifically target cellular tubulin and further map the paclitaxel site.

Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin.

Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin

Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules

Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain.

Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop

Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport.

Endowing indole-based tubulin inhibitors with an anchor for derivatization: highly potent 3-substituted indolephenstatins and indoleisocombretastatins.

Equilibrium and kinetic study of the conformational transition toward the active state of p21Ha-ras, induced by the binding of BeF3- to the GDP-bound state, in the absence of GTPase-activating proteins

Fluorescent taxoid probes for microtubule research.

Free Energy Profile and Kinetics Studies of Paclitaxel Internalization from the Outer to the Inner Wall of Microtubules.

Gallic acid sensitizes paclitaxel-resistant human ovarian carcinoma cells through an increase in reactive oxygen species and subsequent downregulation of ERK activation.

High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells

High-affinity ligands of the colchicine domain in tubulin based on a structure-guided design.

Identification of pyrrolopyrimidine derivative PP-13 as a novel microtubule-destabilizing agent with promising anticancer properties

Insights into Molecular Plasticity of Choline Binding Proteins (Pneumococcal Surface Proteins) by SAXS

Insights into nucleotide recognition by cell division protein FtsZ from a mant-GTP competition assay and molecular dynamics.

Insights into the Interaction of Discodermolide and Docetaxel with Tubulin. Mapping the Binding Sites of Microtubule-Stabilizing Agents by Using an Integrated NMR and Computational Approach ⬇️

Interaction of a cyclostreptin analogue with the microtubule taxoid site: the covalent reaction rapidly follows binding.

Low resolution structure of microtubules in solution. Synchrotron X-ray scattering and electron microscopy of taxol-induced microtubules assembled from purified tubulin in comparison with glycerol and MAP-induced microtubules

Macromolecular accessibility of fluorescent taxoids bound at a paclitaxel binding site in the microtubule surface.

Mechanism of action of the cytotoxic macrolides amphidinolide X and J.

Modification of C-seco taxoids through ring tethering and substituent replacement leading to effective agents against tumor drug resistance mediated by βIII-Tubulin and P-glycoprotein (P-gp) overexpressions.

Modulation of Microtubule Interprotofilament Interactions by Modified Taxanes ⬇️

Molecular Recognition of Epothilones by Microtubules and Tubulin Dimers Revealed by Biochemical and NMR Approaches

Molecular mechanism of action of microtubule-stabilizing anticancer agents

Molecular mechanisms of pressure induced conformational changes in BPTI

Molecular recognition of taxol by microtubules. Kinetics and thermodynamics of binding of fluorescent taxol derivatives to an exposed site

NMR determination of the bioactive conformation of peloruside A bound to microtubules.

New interfacial microtubule inhibitors of marine origin, PM050489/PM060184, with potent antitumor activity and a distinct mechanism.

Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach

Optimization of taxane binding to microtubules: binding affinity dissection and incremental construction of a high-affinity analog of paclitaxel.

Overcoming tumor drug resistance with high-affinity taxanes: a SAR study of C2-modified 7-acyl-10-deacetyl cephalomannines.

PM060184, a new tubulin binding agent with potent antitumor activity including P-glycoprotein over-expressing tumors

Pironetin Binds Covalently to αCys316 and Perturbs a Major Loop and Helix of α-Tubulin to Inhibit Microtubule Formation

Possible binding site for paclitaxel at microtubule pores.

Protein Shape and Assembly Studied with X-Ray Solution Scattering: Fundaments and Practice

Quinolin-6-Yloxyacetamides Are Microtubule Destabilizing Agents That Bind to the Colchicine Site of Tubulin.

Restoration of Microtubule Interaction and Cytotoxicity in D-seco Taxanes upon Incorporation of 20-Hydroxymethyl-4-allyloxy Groups

Self-Organization of FtsZ Polymers in Solution Reveals Spacer Role of the Disordered C-Terminal Tail.

Solution structure of GDP-tubulin double rings to 3 nm resolution and comparison with microtubules

Structural Basis of Microtubule Stabilization by Discodermolide.

Structural and Biochemical Characterization of the Interaction of Tubulin with Potent Natural Analogues of Podophyllotoxin

Structural model for differential cap maturation at growing microtubule ends

Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents

Synthesis and Anti-Proliferative Activity of Sulfanyltriazolylnaphthalenols and Sulfanyltriazolylnaphthalene-1,4-diones.

Synthesis and biological evaluation as microtubule-active agents of several tetrahydrofuran and spiroacetal derivatives.

Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation.

Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents

Synthesis and biological evaluation of truncated α-tubulin-binding pironetin analogues lacking alkyl pendants in the side chain or the dihydropyrone ring.

Synthesis of N-acyl Derivatives of Aminocombretastatin A-4 and Study of their Interaction with Tubulin and downregulation of c-Myc

Synthesis of Thicolchicine-Based Conjugates: Investigation towards Bivalent Tubulin/Microtubules Binders

Synthesis, Biological Profiling and Determination of the Tubulin-Bound Conformation of 12-Aza-Epothilones (Azathilones).

Synthesis, Characterization, and Application in HeLa Cells of an NIR Light Responsive Doxorubicin Delivery System Based on NaYF4:Yb,Tm@SiO2-PEG Nanoparticles.

Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate ⬇️

Synthesis, biological evaluations, and tubulin binding poses of C-2alpha sulfur linked taxol analogues

TRAPPII regulates exocytic Golgi exit by mediating nucleotide exchange on the Ypt31 ortholog RabERAB11.

Taxanes with high potency inducing tubulin assembly overcome tumoural cell resistances.

The Binding Sites of Microtubule-Stabilizing Agents ⬇️

The Interaction of Microtubules with Stabilizers Characterized at Biochemical and Structural Levels ⬇️

The Mechanism of the Interactions of Pironetin Analog/Combretastatin A-4 Hybrids with Tubulin.

The binding mode of side chain- and C3-modified epothilones to tubulin.

The diamagnetic susceptibility of the tubulin dimer

The impact of cyclopropane configuration on the biological activity of cyclopropyl-epothilones.

The interactions of cell division protein FtsZ with guanine nucleotides.