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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Tubulins are a family of intracellular proteins most commonly associated with microtubules, part of the cytoskeleton. They are exploited for therapeutic gain in cancer chemotherapy as targets for agents derived from a variety of natural products: taxanes, colchicine and vinca alkaloids. These are thought to act primarily through β-tubulin, thereby interfering with the normal processes of tubulin polymer formation and disassembly.
* Key recommended reading is highlighted with an asterisk
* Kaur R, Kaur G, Gill RK, Soni R, Bariwal J. (2014) Recent developments in tubulin polymerization inhibitors: An overview. Eur J Med Chem, 87: 89-124. [PMID:25240869]
* Lu Y, Chen J, Xiao M, Li W, Miller DD. (2012) An overview of tubulin inhibitors that interact with the colchicine binding site. Pharm. Res., 29 (11): 2943-71. [PMID:22814904]
* Perdiz D, Mackeh R, Poüs C, Baillet A. (2011) The ins and outs of tubulin acetylation: more than just a post-translational modification?. Cell. Signal., 23 (5): 763-71. [PMID:20940043]
* Schappi JM, Krbanjevic A, Rasenick MM. (2014) Tubulin, actin and heterotrimeric G proteins: coordination of signaling and structure. Biochim. Biophys. Acta, 1838 (2): 674-81. [PMID:24071592]
* Song Y, Brady ST. (2015) Post-translational modifications of tubulin: pathways to functional diversity of microtubules. Trends Cell Biol., 25 (3): 125-36. [PMID:25468068]
* Yu I, Garnham CP, Roll-Mecak A. (2015) Writing and Reading the Tubulin Code. J. Biol. Chem., 290 (28): 17163-72. [PMID:25957412]
1. Cifuentes M, Schilling B, Ravindra R, Winter J, Janik ME. (2006) Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs. Bioorg. Med. Chem. Lett., 16 (10): 2761-4. [PMID:16504507]
2. Gangjee A, Zhao Y, Raghavan S, Rohena CC, Mooberry SL, Hamel E. (2013) Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents. J. Med. Chem., 56 (17): 6829-44. [PMID:23895532]
3. Narayan S, Carlson EM, Cheng H, Condon K, Du H, Eckley S, Hu Y, Jiang Y, Kumar V, Lewis BM et al.. (2011) Novel second generation analogs of eribulin. Part III: Blood-brain barrier permeability and in vivo activity in a brain tumor model. Bioorg. Med. Chem. Lett., 21 (6): 1639-43. [PMID:21324687]
4. Ouyang X, Piatnitski EL, Pattaropong V, Chen X, He HY, Kiselyov AS, Velankar A, Kawakami J, Labelle M, Smith 2nd L et al.. (2006) Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines. Bioorg. Med. Chem. Lett., 16 (5): 1191-6. [PMID:16377187]
Database page citation:
Tubulins. Accessed on 29/04/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=858.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Buneman OP, Catterall WA, Cidlowski JA, Davenport AP, Fabbro D, Fan G, McGrath JC, Spedding M, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Overview. Br J Pharmacol. 172: 5729-5743.