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Last Updated: 05/10/22

Tubulin Biochemistry and Pharmacology Lab

The Tubulin Biochemistry and Pharmacology Laboratory is interested in all aspects of tubulin biochemistry and pharmacology, particularly the discovery and analysis of novel molecular entities and how they interact with tubulin. The Tubulin Biochemistry and Pharmacology Laboratory maintains expertise in evaluating entities that interact with all drug binding sites on tubulin. This laboratory joined the Developmental Therapeutics Program in 1996 with a mission to extend tubulin biochemistry and pharmacology expertise to assist extramural laboratories. The Tubulin Biochemistry and Pharmacology Laboratory is engaged in multiple extramural collaborations with research groups all over the world.

References

Bai R, Cruz-Monserrate Z, Fenical W, Pettit GR, Hamel E. Interaction of diazonamide A with tubulin. Arch Biochem Biophys 2020; 680: 108217.

Spanò V, Barreca M, Rocca R, Bortolozzi R, Bai R, Carbone A, Raimondi MV, Piccionello AP, Montalbano A, Alcaro S, Hamel E, Viola G, Barraja P. Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors. Eur J Med Chem 2021; 212: 113122.

Horne EA, Diaz P, Cimino PJ, Jung E, Xu C, Hamel E, Wagenbach M, Kumasaka D, Wageling NB, Azorín DD, Winkler F, Wordeman LG, Holland EC, Stella N. A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis. Neurooncol Adv 2020; 3: vdaa165.

Choudhary S, Doshi A, Luckett-Chastain L, Ihnat M, Hamel E, Mooberry SL, Gangjee A. Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. Bioorg Med Chem 2021; 35: 116061.

Peerzada MN, Hamel E, Bai R, Supuran CT, Azam A. Deciphering the key heterocyclic scaffolds in targeting microtubules, kinases and carbonic anhydrases for cancer drug development. Pharmacol Ther 2021; 225: 107860.

Saito Y, Taniguchi Y, Hirazawa S, Miura Y, Tsurimoto H, Nakayoshi T, Oda A, Hamel E, Yamashita K, Goto M, Nakagawa-Goto K. Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives. Eur J Med Chem 2021; 222: 113578.

Romagnoli R, Preti D, Hamel E, Bortolozzi R, Viola G, Brancale A, Ferla S, Morciano G, Pinton P. Concise synthesis and biological evaluation of 2-aryl-3-anilinobenzo[b]thiophene derivatives as potent apoptosis-inducing agents. Bioorg Chem 2021; 112: 104919.

Puxeddu M, Shen H, Bai R, Coluccia A, Bufano M, Nalli M, Sebastiani J, Brancaccio D, Da Pozzo E, Tremolanti C, Martini C, Orlando V, Biagioni S, Sinicropi MS, Ceramella J, Iacopetta D, Coluccia AML, Hamel E, Liu T, Silvestri R, La Regina G. Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia. Eur J Med Chem 2021; 221: 113532.

Diaz P, Horne E, Xu C, Hamel E, Wagenbach M, Petrov RR, Uhlenbruck B, Haas B, Hothi P, Wordeman L, Gussio R, Stella N. Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells. Eur J Med Chem 2018; 159: 74-89.

Xiang W, Quadery TM, Hamel E, Luckett-Chastain LR, Ihnat MA, Mooberry SL, Gangjee A. The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affect their potency as microtubule targeting agents and their antitumor activity. Bioorg Med Chem 2021; 29: 115887.

About the Branch Chief

Dr. Mary K. Wolpert, Ph.D. Dr. Beverly A. Teicher PhD is Chief of the Molecular Pharmaco-logy Branch at NCI, a position that she assumed in early 2011. One focus of the Molecular Pharmacology Branch is target and drug discovery for rare and recalcitrant cancers such as sarcoma and small cell lung cancer. Dr. Teicher completed a PhD in Bioorganic Chemistry at the Johns Hopkins University and postdoctoral training at Yale University School of Medicine. More…