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Microtubule inhibitors

Related

  • Tubulin resources
    • Directly conjugated cytoskeletal markers
      • Organelle markers and dyes
        • Microtubule structure and dynamics
        • Cell biology resources
          • Imaging guide
            • Cell proliferation guide
            • Small molecule resources
              • Guide to using small molecules
                • Small molecules FAQ

                Use this guide to select the optimal compounds to target microtubules and key microtubule-associating proteins.


                Click to expand. Known microtubule binding sites for small molecule compounds.


                Target

                Role

                Compound

                Mechanism

                Tubulin

                Tubulin polymerization







                Microtubule elongation following GTP-dependent tubulin dimer addition

                Nocodazole

                Binds to αβ-tubulin dimers preventing assembly and promoting depolymerization.1

                Vinblastine

                Colchicine

                Binds to the colchicine binding site of β-tubulin, preventing αβ-tubulin dimer assembly.2,3

                Combretastatin A4 (CA-4)

                Glyoxbulin 59
                *New*

                Rigidin C2 Cpd 7 *New*

                Binds at Asn258 and Lys352 of β-tubulin and suppresses tubulin polymerization. Exhibits in vivo efficacy.4

                Tubstat3 Cpd 21 *New*

                Dual action, potent tubulin polymerization and STAT3 phosphorylation inhibitor.5

                Tubulin depolymerization

                Shortening of microtubules by αβ-tubulin dimer removal

                Paclitaxel

                Binds and stabilizes tubulin dimers, prevents depolymerization and affects microtubule dynamics.6


                Docetaxel

                Acetylation

                Posttranslational modification affecting cargo trafficking

                Trichostatin A (TSA)

                Deacetylase inhibitor that increases microtubule acetylation.7

                Polyamination

                Posttranslational modification essential for microtubule stabilization

                ZM 449829

                Potent transglutaminase inhibitor.8

                Microtubule Associating Proteins (MAPs)

                Tau



                Lattice binding MAPs that stabilize microtubules primarily in axons

                YM-01

                Potently reduces Tau levels in vitro and ex vivo.9

                MAP1, MAP2

                MDL 28170

                 Prevents MAP1,2 cleavage and degradation.10

                Trolox

                Amyloid β-peptide (1-40)

                Induces MAP1,2 protecolysis.10

                Doublecortin (DCx)


                Stabilizes and catalyzes tubulin dimer addition

                Okadaic cid

                Inhibits PP2A and affects DCx localization.11

                Nocodazole

                Dephosphorylates DCx.11

                Kinetochore formation

                γ-TuRC

                γ-tubulin ring complex essential for microtubule nucleation during mitosis

                SB 415286

                Inhibits GSK-3β mediated γ-TuRC recruitment to spindle poles.12

                Aurora B


                Microtubule stabilization during spindle formation

                AZD1152-HQPA

                Selective Aurora B kinase inhibitor inducing apoptosis and growth arrest.13


                ZM 447439

                Specific Aurora B inhibitor causing apoptosis.13

                Motility

                Kinesin Spindle Protein (KSP)/Eg5/KIF11


                Microtubule motor involved in mitotic pole separation

                Monastrol

                Inhibits kinesin Eg5 and alters its interaction with microtubules.14


                S-Trityl-cysteine

                Eg5 inhibitor that induces mitotic arrest.15

                Dynein

                Motor protein that facilitates cargo transport and microtubule sliding in cilia/flagella

                EHNA hydrochloride

                Interferes with dynein mediated motility in microtubules.16

                Dynactin

                Modulates interaction of motors to cargo the arrangement of microtubules

                Nordihydroguaiaretic acid (NDGA)

                Protects microtubules from depolymerization. Recruits dynein-dynactin complex to centrosome.17,18

                Myosin II

                Facilitaes crosstalk betweek microtubules and actin

                Blebbistatin

                Noncompetitive inhibitor of Myosin II.19

                ​

                References

                1. Jordan, M. a, Thrower, D. & Wilson, L. Effects of vinblastine, podophyllotoxin and nocodazole on mitotic spindles. Implications for the role of microtubule dynamics in mitosis. J. Cell Sci. 102 (Pt 3, 401–416 (1992).

                2. Lu, Y., Chen, J., Xiao, M., Li, W. & Miller, D. D. An overview of tubulin inhibitors that interact with the colchicine binding site. Pharm. Res. 29, 2943–2971 (2012).

                3. Colley, H. E. et al. An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer. J. Med. Chem. 58, 9309–9333 (2015).

                4. Medellin, D. C. et al. Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities. J. Med. Chem. 59, 480–485 (2016).

                5. Lai, M.-J. et al. N -Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling. J. Med. Chem. 58, 6549-58 (2015).

                6. Verweij, J., Clavel, M. & Chevalier, B. Paclitaxel (Taxol) and docetaxel (Taxotere): not simply two of a kind. Ann. Oncol. 5, 495–505 (1994).

                7. Godena, V. K. et al. Increasing microtubule acetylation rescues axonal transport and locomotor deficits caused by LRRK2 Roc-COR domain mutations. Nat. Commun. 5, 5245 (2014).

                8. Lai, T. S. et al. Identification of Chemical Inhibitors to Human Tissue Transglutaminase by Screening Existing Drug Libraries. Chem. Biol. 15, 969–978 (2008).

                9. Abisambra, J. et al. Allosteric heat shock protein 70 inhibitors rapidly rescue synaptic plasticity deficits by reducing aberrant tau. Biol. Psychiatry 74, 367–374 (2013).

                10. Fifre, A. et al. Microtubule-associated protein MAP1A, MAP1B, and MAP2 proteolysis during soluble amyloid β-peptide-induced neuronal apoptosis: Synergistic involvement of calpain and caspase-3. J. Biol. Chem. 281, 229–240 (2006).

                11. Schaar, B. T., Kinoshita, K. & McConnell, S. K. Doublecortin Microtubule Affinity Is Regulated by a Balance of Kinase and Phosphatase Activity at the Leading Edge of Migrating Neurons. Neuron 41, 203–213 (2004).

                12. Izumi, N., Fumoto, K., Izumi, S. & Kikuchi, A. GSK-3beta regulates proper mitotic spindle formation in cooperation with a component of the gamma-tubulin ring complex, GCP5. J. Biol. Chem. 283, 12981–12991 (2008).

                13. Yang, J. et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest,  apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood 110, 2034–2040 (2007).

                14. Krzysiak, T. C. et al. A structural model for monastrol inhibition of dimeric kinesin Eg5. EMBO J. 25, 2263–2273 (2006).

                15. Skoufias, D. A. et al. S-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression. J. Biol. Chem. 281, 17559–17569 (2006).

                16.  Lecland, N. & Lüders, J. The dynamics of microtubule minus ends in the human mitotic spindle. Nat. Cell Biol. 16, 770–8 (2014).

                17. Nakamura, M. et al. Nordihydroguaiaretic acid, of a new family of microtubule-stabilizing agents, shows effects differentiated from paclitaxel. Biosci. Biotechnol. Biochem. 67, 151–157 (2003).

                18. Arasaki, K., Tani, K., Yoshimori, T. & Stephens, D. Nordihydroguaiaretic acid affects multiple dynein-dynactin functions in interphase and mitotic cells. Mol. Pharmacol. 71, 454–460 (2007).

                19. Bond, L. M., Tumbarello, D. a, Kendrick-Jones, J. & Buss, F. Small-molecule inhibitors of myosin proteins. Future Med. Chem. 5, 41–52 (2013).

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