J. Díaz

发表

Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site

S. Matthew, D. Lucena‐Agell, A. Prota, 2021, Proceedings of the National Academy of Sciences.

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

I. Barasoain, C. Galmarini, M. Peñalva, 2013, ACS chemical biology.

Structural model for differential cap maturation at growing microtubule ends

M. Steinmetz, H. Iwamoto, D. Lucena‐Agell, 2020, eLife.

Interaction of epothilone analogs with the paclitaxel binding site: relationship between binding affinity, microtubule stabilization, and cytotoxicity.

A. Ritzén, K. Nicolaou, P. Giannakakou, 2004, Chemistry & biology.

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

M. Redondo-Horcajo, I. Barasoain, F. Cañada, 2016, Journal of natural products.

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

M. Steinmetz, K. Altmann, A. Prota, 2014, Proceedings of the National Academy of Sciences.

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

M. Redondo-Horcajo, I. Barasoain, M. Carda, 2013, Organic & biomolecular chemistry.

Synthesis and Biological Evaluation of α‐Tubulin‐Binding Pironetin Analogues with Enhanced Lipophilicity

I. Barasoain, M. Carda, E. Falomir, 2013 .

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

M. Redondo-Horcajo, I. Barasoain, M. Carda, 2013, Current medicinal chemistry.

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

I. Barasoain, J. Díaz, M. Carda, 2011, European journal of medicinal chemistry.

Synthesis and biological activities of high affinity taxane-based fluorescent probes.

I. Barasoain, W. Fang, R. Matesanz, 2009, Bioorganic & medicinal chemistry letters.

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

I. Barasoain, E. Calvo, R. Buey, 2007, Nature chemical biology.

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

K. Altmann, M. Moore, S. Ambati, 2015, Cancer letters.

Characterization of the hinges of the effector loop in the reaction pathway of the activation of ras‐proteins. Kinetics of binding of beryllium trifluoride to V29G and I36G mutants of Ha‐ras‐p21

Y. Engelborghs, J. Díaz, Steven Kuppens, 1999, Protein science : a publication of the Protein Society.

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

M. Steinmetz, F. Gago, I. Barasoain, 2018, Scientific Reports.

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.

F. Gago, A. Morreale, J. Klett, 2013, Organic & biomolecular chemistry.

Solution structure of Taxotere-induced microtubules to 3-nm resolution. The change in protofilament number is linked to the binding of the taxol side chain.

J. M. de Pereda, J. F. Díaz, V. Peyrot, 1994, The Journal of biological chemistry.

Lattice defects induced by microtubule-stabilizing agents exert a long-range effect on microtubule growth by promoting catastrophes

A. Akhmanova, E. Katrukha, C. Moores, 2021, Proceedings of the National Academy of Sciences.

Microtubule lattice defects promote catastrophes

A. Akhmanova, E. Katrukha, C. Moores, 2021 .

Peloruside A Does Not Bind to the Taxoid Site on β-Tubulin and Retains Its Activity in Multidrug-Resistant Cell Lines

P. Teesdale-Spittle, J. Miller, R. Buey, 2004, Cancer Research.

Retains Its Activity in Multidrug-Resistant Cell Lines-Tubulin β Peloruside A Does Not Bind to the Taxoid Site on

P. Teesdale-Spittle, J. Miller, R. Buey, 2004 .

Advances in Brief Peloruside A Does Not Bind to the Taxoid Site on-Tubulin and Retains Its Activity in Multidrug-Resistant Cell Lines

P. Teesdale-Spittle, J. Miller, R. Buey, 2004 .

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

I. Barasoain, B. Bouchet, C. Galmarini, 2014, Biochemical pharmacology.

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

K. Altmann, M. Redondo-Horcajo, I. Barasoain, 2019, International journal of molecular sciences.

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

A. Jantsch, K. Altmann, J. Gertsch, 2016, Molecules.

The Impact of Cyclopropane Configuration on the Biological Activity of Cyclopropyl‐Epothilones

K. Altmann, M. Redondo-Horcajo, I. Barasoain, 2014, ChemMedChem.

Fluorescent taxoid probes for microtubule research.

I. Barasoain, J. Andreu, J. Díaz, 2010, Methods in cell biology.

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.

D. Lucena‐Agell, I. Barasoain, Yong Tang, 2017, European journal of medicinal chemistry.

Structural Determinants of the Dictyostatin Chemotype for Tubulin Binding Affinity and Antitumor Activity Against Taxane- and Epothilone-Resistant Cancer Cells

M. Steinmetz, A. Nogales, F. Gago, 2016, ACS omega.

Thermodynamics of ligand-induced assembly of tubulin.

M. Menéndez, J. Andreu, J. Díaz, 1993, Biochemistry.

New tubulin binding site targeted by novel cyclodepsipeptide chemotype, gatorbulin-1 1

S. Matthew, D. Lucena‐Agell, A. Prota, 2020 .

Chemical modulation of microtubule structure through the laulimalide/peloruside site.

M. Steinmetz, K. Altmann, F. Gago, 2022, Structure.

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

M. Redondo-Horcajo, I. Barasoain, J. Yli-Kauhaluoma, 2014, European journal of medicinal chemistry.

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

David R. Williams, D. Lucena‐Agell, I. Barasoain, 2015, The Journal of organic chemistry.

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

S. Noppen, S. Liekens, M. Camarasa, 2014, Journal of medicinal chemistry.

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

I. Barasoain, R. Buey, I. Paterson, 2005, Bioorganic & medicinal chemistry letters.

The interaction of microtubules with stabilizers characterized at biochemical and structural levels.

J. Andreu, J. Jiménez‐Barbero, J. Díaz, 2009, Topics in current chemistry.

Título artículo / Títol article: Design and Synthesis of Pironetin Analogue/Colchicine Hybrids and Study of Their Cytotoxic Activity and Mechanisms of Interaction with Tubulin

M. Redondo-Horcajo, I. Barasoain, M. Carda, 2014 .

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

D. Fabbro, M. Zvelebil, Roger L. Williams, 2017, Nature Communications.

The total synthesis and biological properties of the cytotoxic macrolide FD-891 and its non-natural (Z)-C12 isomer.

I. Barasoain, J. Díaz, J. F. Díaz, 2007, Chemistry.

Mechanism of Action of the Cytotoxic Macrolides Amphidinolide X and J

I. Barasoain, M. Barbazanges, C. Meyer, 2011, Chembiochem : a European journal of chemical biology.

Chemical synthesis and biological evaluation of novel epothilone B and trans-12,13-cyclopropyl epothilone B analogues

A. Ritzén, K. Nicolaou, K. Altmann, 2002 .

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

M. Steinmetz, K. Altmann, A. Prota, 2019, International journal of molecular sciences.

Cyclostreptin (FR182877), an antitumor tubulin-polymerizing agent deficient in enhancing tubulin assembly despite its high affinity for the taxoid site.

A. Marcus, R. Gussio, P. Giannakakou, 2005, Biochemistry.

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

F. Mollinedo, J. Andreu, M. Medarde, 2013, Journal of medicinal chemistry.

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

G. Rivas, M. Menéndez, J. Andreu, 1998, The Journal of Biological Chemistry.

Assembly of purified GDP-tubulin into microtubules induced by taxol and taxotere: reversibility, ligand stoichiometry, and competition.

J. Díaz, J. Andreu, J M Andreu, 1993, Biochemistry.

Overcoming Tumor Drug Resistance with High‐Affinity Taxanes: A SAR Study of C2‐Modified 7‐Acyl‐10‐Deacetyl Cephalomannines

I. Barasoain, F. Sharom, Ronghua Liu, 2007, ChemMedChem.

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

S. Pieraccini, M. Sironi, M. Christodoulou, 2019, ChemPlusChem.

Studies toward the Synthesis of an Oxazole-Based Analog of (-)-Zampanolide.

K. Altmann, D. Lucena‐Agell, B. Pfeiffer, 2021, Organic Letters.

The bound conformation of microtubule-stabilizing agents: NMR insights into the bioactive 3D structure of discodermolide and dictyostatin.

Jesús Jiménez-Barbero, Ian Paterson, I. Paterson, 2008, Chemistry.

Microtubule interactions with chemically diverse stabilizing agents: thermodynamics of binding to the paclitaxel site predicts cytotoxicity.

I. Barasoain, P. Giannakakou, R. Buey, 2005, Chemistry & biology.

Probing the pore drug binding site of microtubules with fluorescent taxanes: evidence of two binding poses.

Maurizio Botta, Mattia Mori, Giorgio Maccari, 2010, Chemistry & biology.

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

Alexandre Cardoso-Taketa, M. Villarreal, L. Alvarez, 2015, Evidence-based complementary and alternative medicine : eCAM.

Synthesis and antimitotic and tubulin interaction profiles of novel pinacol derivatives of podophyllotoxins.

I. Barasoain, C. Trigili, J. Andreu, 2012, Journal of medicinal chemistry.

Structural basis of noscapine activation for tubulin binding.

M. Steinmetz, A. Prota, Á. Canales, 2020, Journal of medicinal chemistry.

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

A. Nogales, I. Barasoain, I. Ojima, 2014, Bioorganic & medicinal chemistry.

Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites.

K. Altmann, J. Miller, A. Prota, 2017, Journal of natural products.

Effect of Clinically Used Microtubule Targeting Drugs on Viral Infection and Transport Function

D. Lucena‐Agell, V. Palomo, I. Galindo, 2022, International journal of molecular sciences.

Insights into the Distinct Mechanisms of Action of Taxane and Non-Taxane Microtubule Stabilizers from Cryo-EM Structures.

Kenneth H. Downing, Eva Nogales, E. Nogales, 2017, Journal of molecular biology.

Fucoidans: The importance of processing on their anti-tumoral properties

Á. González-Fernández, H. Domínguez, N. Flórez-Fernández, 2020, Algal Research.

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

P. Chacón, G. Diakun, J. Valpuesta, 1998, The Journal of Biological Chemistry.

Taxanes convert regions of perturbed microtubule growth into rescue sites

M. Steinmetz, K. Altmann, J. Díaz, 2019, Nature Materials.

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

S. Liekens, M. Camarasa, Marta Gargantilla, 2019, European journal of medicinal chemistry.

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

R. Buey, J. F. Díaz, J. Andreu, 2006, Biochemistry.

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

M. Steinmetz, K. Altmann, D. Lucena‐Agell, 2018, Nature Communications.

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

J. F. Díaz, R. Núnez-Ramírez, O. Llorca, 2017, Biophysical journal.

Au@p4VP core@shell pH-sensitive nanocomposites suitable for drug entrapment.

M. Laurenti, A. Fery, P. Formánek, 2017, Journal of colloid and interface science.

Mass Spectrometry for Studying the Interaction between Small Molecules and Proteins

E. Calvo, J. López, E. Camafeita, 2008 .

Structural and Functional Insights Into Skl and Pal Endolysins, Two Cysteine-Amidases With Anti-pneumococcal Activity. Dithiothreitol (DTT) Effect on Lytic Activity

R. Buey, M. Menéndez, Palma Rico-Lastres, 2021, Frontiers in Microbiology.

Cpl-7, a Lysozyme Encoded by a Pneumococcal Bacteriophage with a Novel Cell Wall-binding Motif*

N. Campillo, N. Campillo, M. Menéndez, 2010, The Journal of Biological Chemistry.

Possible binding site for paclitaxel at microtubule pores

M. Botta, J. F. Díaz, G. Maccari, 2009, The FEBS journal.

Structural insight into the stabilization of microtubules by taxanes

M. Steinmetz, K. Altmann, F. Gago, 2022, bioRxiv.

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

K. Altmann, J. Miller, P. Northcote, 2017, International journal of molecular sciences.

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

J. F. Díaz, H. Arst, M. Peñalva, 2015, Proceedings of the National Academy of Sciences.

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.

Arun K. Ghosh, P. Giannakakou, A. O'brate, 2002, Biochemistry.

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

M. Redondo-Horcajo, I. Barasoain, J. Díaz, 2016, Archiv der Pharmazie.

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.

I. Paterson, C. Trigili, Á. Canales, 2011, ACS chemical biology.

Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

D. Lucena‐Agell, A. Akhmanova, J. Coll, 2020, bioRxiv.

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

M. Steinmetz, I. Barasoain, J. Díaz, 2017, International journal of molecular sciences.

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

Antonio Morreale, A. Morreale, R. Gil-Redondo, 2010, Biochemistry.

Molecular recognition of epothilones by microtubules and tubulin dimers revealed by biochemical and NMR approaches.

K. Altmann, F. Gago, T. Carlomagno, 2014, ACS chemical biology.

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

M. Redondo-Horcajo, I. Barasoain, P. Lastres, 2018, Oncology reports.

The Diamagnetic Susceptibility of the Tubulin Dimer

G. Diakun, W. Bras, J. Torbet, 2014, Journal of biophysics.

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

I. Barasoain, Jorge Rubio-Retama, Isabel Barasoain, 2015, ACS applied materials & interfaces.

Structural intermediates in the assembly of taxoid-induced microtubules and GDP-tubulin double rings: time-resolved X-ray scattering.

G. Diakun, J. Bordas, J. Andreu, 1996, Biophysical journal.

Molecular Recognition of Taxol by Microtubules

Y. Engelborghs, A. A. Souto, J. Andreu, 2000, The Journal of Biological Chemistry.

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

J. Snyder, I. Barasoain, Ana A. Alcaraz, 2007, Bioorganic & Medicinal Chemistry Letters.

Apo‐Hsp90 coexists in two open conformational states in solution

R. Buey, Daniel Thomas, P. Barbier, 2008, Biology of the cell.

Synthesis and Biological Evaluation of C(13)/C(13′)‐Bis(desmethyl)disorazole Z

K. Altmann, D. Lucena‐Agell, M. A. Oliva, 2022, Angewandte Chemie.

Identification of the guanine nucleotide exchange factor for SAR1 in the filamentous fungal model Aspergillus nidulans.

J. F. Díaz, Miguel Hernández-González, M. Peñalva, 2019, Biochimica et biophysica acta. Molecular cell research.

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

I. Barasoain, Xi Xiao, Y. Li, 2011, Bioorganic & medicinal chemistry letters.

Crystal structures of taxane-tubulin complexes: Implications for the mechanism of microtubule stabilization by Taxol

M. Steinmetz, K. Altmann, D. Lucena‐Agell, 2021 .

Comparative Binding Energy (COMBINE) Analysis Supports a Proposal for the Binding Mode of Epothilones to β‐Tubulin

F. Gago, A. Morreale, J. F. Díaz, 2012, ChemMedChem.

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

J. Bordas, J. Andreu, E. Pantos, 1994, Journal of molecular biology.

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

Jesús Jiménez-Barbero, R. Buey, P. Northcote, 2006, Journal of the American Chemical Society.

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

E. Novellino, M. Steinmetz, L. Altucci, 2019, European journal of medicinal chemistry.

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

M. Steinmetz, K. Altmann, D. Lucena‐Agell, 2018, Nature Communications.

Targeting the colchicine site in tubulin through cyclohexanedione derivatives

S. Noppen, S. Liekens, M. Camarasa, 2016 .

Alternative Approaches to Understand Microtubule Cap Morphology and Function

F. Gago, M. A. Oliva, J. Díaz, 2023, ACS omega.

Structure, Thermodynamics, and Kinetics of Plinabulin Binding to two Tubulin Isotypes

F. Viti, A. Cavalli, M. Steinmetz, 2019, Chem.

Maytansinol Derivatives: Side Reactions as a Chance for New Tubulin Binders

K. Altmann, D. Lucena‐Agell, F. Vasile, 2021, Chemistry.

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

M. Carda, Raül Agut, E. Falomir, 2020, Medicinal chemistry.

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.

I. Paterson, C. Trigili, Á. Canales, 2011, ACS chemical biology.

PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin

D. Lucena‐Agell, P. Avilés, M. Guillén, 2024, Journal of Medicinal Chemistry.

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

M. Steinmetz, K. Altmann, D. Lucena‐Agell, 2018, Nature Communications.