Cytoskeletal inhibitor

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A cytoskeletal inhibitor is a small molecule compound that acts as an inhibitor of proteins in the cytoskeleton .

properties

Cytoskeletal inhibitors mostly bind to actin or tubulin and prevent the formation or dissolution of polymers of these two proteins ( microfilaments or microtubules ). For example, taxol prevents the depolymerization of microtubules, while cytochalasin D inhibits the polymerization of actin. In some cases, cytoskeleton inhibitors are also used as drugs in addition to their use in research , e.g. B. in chemotherapy .

Active ingredient Target protein effect Clinical application
Colchicine Microtubules prevents polymerisation gout
Cytochalasins Actin prevents polymerisation no
Demecolcine Microtubules leads to depolymerization chemotherapy
Latrunculin Actin prevents polymerisation no
Jasplakinolide Actin intensifies polymerization no
Nocodazole Microtubules prevents polymerisation no
Paclitaxel (Taxol) Microtubules prevents depolymerization and mitosis chemotherapy
Phalloidin Actin prevents depolymerization no
Swinholid Actin binds actin dimers no
Vinblastine Microtubules prevents polymerisation chemotherapy

Individual evidence

  1. ^ V. Thamilselvan, MD Basson: The role of the cytoskeleton in differentially regulating pressure-mediated effects on malignant colonocyte focal adhesion signaling and cell adhesion. In: Carcinogenesis . Volume 26, Number 10, October 2005, pp. 1687-1697, doi : 10.1093 / carcin / bgi135 , PMID 15917311 .
  2. ↑ a b M. A. Jordan, W. Leslie: Microtubules as a Target for Anticancer Drugs . In: Nature Reviews Cancer . 4, No. 4, 2004, pp. 253-265. doi : 10.1038 / nrc1317 . PMID 15057285 .
  3. ↑ A. Vandecandelaere, SR Martin, Y. Engelborghs: Response of microtubules to the addition of colchicine and tubulin-colchicine: evaluation of models for the interaction of drugs with microtubules . In: Biochem J . 323, No. Pt 1, April 1, 1997, pp. 189-196. PMID 9173881 . PMC 1218294 (free full text).
  4. ↑ JA Cooper: Effects of Cytochalasin and Phalloidin on Actin . (pdf) In: Journal of Cell Biology . 105, No. 4, 1987, pp. 1473-1478. doi : 10.1083 / jcb.105.4.1473 . PMID 3312229 . PMC 2114638 (free full text).
  5. ^ Mary Ann Jordan, Leslie Wilson: Microtubules as a target for anticancer drugs . In: Nature Reviews Cancer . 4, No. 4, 2004, pp. 253-65. doi : 10.1038 / nrc1317 . PMID 15057285 .
  6. ↑ EG Yarmola, T. Somasundaram, TA Boring, I. Spector, MR Bubb: Actin-Latrunculin A Structure and Function . In: Journal of Biological Chemistry . 275, No. 36, 2000, pp. 28120-28127. doi : 10.1074 / jbc.M004253200 . PMID 10859320 .
  7. ↑ F. Sasse et al .: The chondramides: cytostatic agents from myxobacteria acting on the actin cytoskeleton. . In: Journal of the National Cancer Institute . 90, No. 20, October 21, 1998, pp. 1559-63. doi : 10.1093 / jnci / 90.20.1559 . PMID 9790549 .
  8. ↑ Michael R. Bubb et al: Effects of Jasplakinolide on the Kinetics of Actin Polymerization . In: J Biol Chem . 275, No. 7, 2000, pp. 5163-70. doi : 10.1074 / jbc.275.7.5163 . PMID 10671562 .
  9. ↑ RJ Vasquez et al .: Nanomolar concentrations of nocodazole alter microtubule dynamic instability in vivo and in vitro . In: Mol Biol Cell . 8, 1997, pp. 973-985. doi : 10.1091 / mbc.8.6.973 .
  10. ↑ M. Wani, H. Taylor, M. Wall, P. Coggon, A. McPhail: Plant antitumor agents. VI. The isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia . In: J. Am. Chem. Soc. . 93, No. 9, 1971, pp. 2325-7. doi : 10.1021 / ja00738a045 . PMID 5553076 .
  11. ↑ Igor B. Buchwalow, Werner Böcker: Immunohistochemistry: Basics and Methods . Springer ,, 2010, ISBN 978-3-642-04608-7 , p. 92.
  12. ↑ MR Bubb, I. Spector, AD Bershadsky, ED Korn: Swinholide a is a microfilament disrupting marine toxin that stabilizes actin dimers and severs actin filaments . In: The Journal of Biological Chemistry . 270, No. 8, 1995, pp. 3463-6. doi : 10.1074 / jbc.270.8.3463 . PMID 7876075 .