Frank Loganzo

Summary

Affiliation: Wyeth Research
Country: USA

Publications

  1. ncbi request reprint HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo
    Frank Loganzo
    Oncology Research, Wyeth Research, Pearl River, New York 10965, USA
    Cancer Res 63:1838-45. 2003
  2. ncbi request reprint Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in alpha-tubulin
    Frank Loganzo
    Oncology Research, Wyeth Research, 401 North Middletown Road, 200 4709, Pearl River, NY 10965, USA
    Mol Cancer Ther 3:1319-27. 2004
  3. ncbi request reprint Paclitaxel-resistant cells have a mutation in the paclitaxel-binding region of beta-tubulin (Asp26Glu) and less stable microtubules
    Malathi Hari
    Discovery Oncology, Wyeth, 401 North Middletown Road, Room 4709, Building 200, Pearl River, NY 10965, USA
    Mol Cancer Ther 5:270-8. 2006
  4. ncbi request reprint Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: modification of the A segment
    Ayako Yamashita
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 14:5317-22. 2004
  5. ncbi request reprint Two photoaffinity analogues of the tripeptide, hemiasterlin, exclusively label alpha-tubulin
    Maria Nunes
    Oncology Research, Chemical and Screening Sciences, Radiosynthesis Group, and Bioorganic Enzymology, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    Biochemistry 44:6844-57. 2005
  6. ncbi request reprint Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2
    Allan Wissner
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem 15:3635-48. 2007
  7. ncbi request reprint Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286)
    Arie Zask
    Chemical and Screening Sciences, and Oncology Research, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 47:4774-86. 2004
  8. ncbi request reprint 2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2
    Allan Wissner
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 N Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 48:7560-81. 2005
  9. ncbi request reprint Hybrids of the hemiasterlin analogue taltobulin and the dolastatins are potent antimicrotubule agents
    Arie Zask
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Am Chem Soc 127:17667-71. 2005
  10. ncbi request reprint MAC-321, a novel taxane with greater efficacy than paclitaxel and docetaxel in vitro and in vivo
    Deepak Sampath
    Wyeth Research, Department of Oncology, Pearl River, NY 10965, USA
    Mol Cancer Ther 2:873-84. 2003

Collaborators

Detail Information

Publications16

  1. ncbi request reprint HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo
    Frank Loganzo
    Oncology Research, Wyeth Research, Pearl River, New York 10965, USA
    Cancer Res 63:1838-45. 2003
    ....
  2. ncbi request reprint Cells resistant to HTI-286 do not overexpress P-glycoprotein but have reduced drug accumulation and a point mutation in alpha-tubulin
    Frank Loganzo
    Oncology Research, Wyeth Research, 401 North Middletown Road, 200 4709, Pearl River, NY 10965, USA
    Mol Cancer Ther 3:1319-27. 2004
    ..These data suggest that HTI-286 resistance may be partially mediated by mutation of alpha-tubulin and by an ATP-binding cassette drug pump distinct from P-glycoprotein, ABCG2, MRP1, or MRP3...
  3. ncbi request reprint Paclitaxel-resistant cells have a mutation in the paclitaxel-binding region of beta-tubulin (Asp26Glu) and less stable microtubules
    Malathi Hari
    Discovery Oncology, Wyeth, 401 North Middletown Road, Room 4709, Building 200, Pearl River, NY 10965, USA
    Mol Cancer Ther 5:270-8. 2006
    ..These results suggest that a mutation in tubulin might affect microtubule stability as well as drug binding and contribute to the observed resistance profile...
  4. ncbi request reprint Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: modification of the A segment
    Ayako Yamashita
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 14:5317-22. 2004
    ....
  5. ncbi request reprint Two photoaffinity analogues of the tripeptide, hemiasterlin, exclusively label alpha-tubulin
    Maria Nunes
    Oncology Research, Chemical and Screening Sciences, Radiosynthesis Group, and Bioorganic Enzymology, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    Biochemistry 44:6844-57. 2005
    ..In addition, we speculate that antimitotic peptides mimic the interaction of stathmin with tubulin...
  6. ncbi request reprint Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2
    Allan Wissner
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem 15:3635-48. 2007
    ..The relative dependence of the IC(50) values on the concentration of ATP used in the assays suggests that these compounds appear to function as irreversible inhibitors of each kinase...
  7. ncbi request reprint Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286)
    Arie Zask
    Chemical and Screening Sciences, and Oncology Research, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 47:4774-86. 2004
    ..Groups tolerant of modification, leading to novel analogues, are reported. Potent analogues identified through in vivo studies in tumor xenograft models include one superior analogue, HTI-042...
  8. ncbi request reprint 2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2
    Allan Wissner
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 N Middletown Road, Pearl River, New York 10965, USA
    J Med Chem 48:7560-81. 2005
    ..Unequivocal evidence, from mass spectral studies, indicates that these inhibitors form a covalent interaction with Cys-1045. One member of this series displays antitumor activity in an in vivo model...
  9. ncbi request reprint Hybrids of the hemiasterlin analogue taltobulin and the dolastatins are potent antimicrotubule agents
    Arie Zask
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401 North Middletown Road, Pearl River, New York 10965, USA
    J Am Chem Soc 127:17667-71. 2005
    ....
  10. ncbi request reprint MAC-321, a novel taxane with greater efficacy than paclitaxel and docetaxel in vitro and in vivo
    Deepak Sampath
    Wyeth Research, Department of Oncology, Pearl River, NY 10965, USA
    Mol Cancer Ther 2:873-84. 2003
    ..MAC-321 was also highly effective when given as single i.v. dose. Our findings suggest that MAC-321, which is currently under clinical evaluation, may have broad therapeutic value...
  11. ncbi request reprint D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors
    Arie Zask
    Wyeth Research, Chemical and Screening Sciences, 401 North Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 14:4353-8. 2004
    ..Synthetic modifications of the carboxylic acid could be carried out selectively using a wide range of synthetic reagents. Proline analog 3 was found to be effective in a human xenograft model in athymic mice...
  12. ncbi request reprint Biophysical characterization of the interactions of HTI-286 with tubulin heterodimer and microtubules
    Girija Krishnamurthy
    Biophysics Enzymology, Screening Sciences, Oncology Research, and Chemical Sciences, Wyeth Research, Pearl River, New York 10965, USA
    Biochemistry 42:13484-95. 2003
    ..In contrast to the microtubule-stabilizing effects of paclitaxel, both HTI-286 and hemiasterlin depolymerize preassembled microtubules at micromolar concentrations...
  13. ncbi request reprint Tubulin inhibitors. Synthesis and biological activity of HTI-286 analogs with B-segment heterosubstituents
    Chuan Niu
    Chemical and Screening Sciences, Discovery Medicinal Chemistry, Wyeth Research, 401 N Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 14:4329-32. 2004
    ..These analogs were more potent than paclitaxel against P-glycoprotein expressing KB-8-5 and KB-V1 cell lines. Several analogs showed strong inhibition of tubulin polymerization...
  14. ncbi request reprint Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles
    Allan Wissner
    Chemical and Screening Sciences and Oncology Research, Wyeth Research, 401N Middletown Road, Pearl River, NY 10965, USA
    Bioorg Med Chem Lett 14:1411-6. 2004
    ..Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations...
  15. ncbi request reprint Targeting vascular and avascular compartments of tumors with C. novyi-NT and anti-microtubule agents
    Long H Dang
    Howard Hughes Medical Institute and Sidney Kimmel Cancer Center, Johns Hopkins Medical Institutions, Baltimore, Maryland, USA
    Cancer Biol Ther 3:326-37. 2004
    ..novyi-NT spores could germinate. A single intravenous injection of C. novyi-NT plus selected anti-microtubule agents was able to cause regressions of several human tumor xenografts in nude mice in the absence of excessive toxicity...
  16. ncbi request reprint Tumor cells resistant to a microtubule-depolymerizing hemiasterlin analogue, HTI-286, have mutations in alpha- or beta-tubulin and increased microtubule stability
    Marianne S Poruchynsky
    Cancer Therapeutics Branch, The NCI Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20892, USA
    Biochemistry 43:13944-54. 2004
    ..Unlike reports of mutations resulting in reduced drug affinity, the experimental data and location of mutations are consistent with resistance to HTI-286 mediated by microtubule-stabilizing mutations in beta- or alpha-tubulin...