TY - JOUR
T1 - Microtubule inhibitors
T2 - Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance
AU - Perez, Edith A.
PY - 2009/8/1
Y1 - 2009/8/1
N2 - Microtubules are important cellular targets for anticancer therapy because of their key role in mitosis. Microtubule inhibitors (MTI) such as taxanes, vinca alkaloids, and epothilones stabilize or destabilize microtubules, thereby suppressing microtubule dynamics required for proper mitotic function, effectively blocking cell cycle progression and resulting in apoptosis. In spite of their antitumor activity, innate or acquired drug resistance to MTIs such as the taxanes is common, limiting their overall clinical efficacy. Further insight into the mechanisms of action of microtubule-targeting drugs has lead to the discovery of novel agents that may provide higher efficacy with limited toxicity and help overcome resistance to conventional MTIs. This review will focus on the different mechanisms of action of MTIs, potential factors related to resistance and tolerability, and will discuss the recent approval as well as the development of new antineoplastic agents.
AB - Microtubules are important cellular targets for anticancer therapy because of their key role in mitosis. Microtubule inhibitors (MTI) such as taxanes, vinca alkaloids, and epothilones stabilize or destabilize microtubules, thereby suppressing microtubule dynamics required for proper mitotic function, effectively blocking cell cycle progression and resulting in apoptosis. In spite of their antitumor activity, innate or acquired drug resistance to MTIs such as the taxanes is common, limiting their overall clinical efficacy. Further insight into the mechanisms of action of microtubule-targeting drugs has lead to the discovery of novel agents that may provide higher efficacy with limited toxicity and help overcome resistance to conventional MTIs. This review will focus on the different mechanisms of action of MTIs, potential factors related to resistance and tolerability, and will discuss the recent approval as well as the development of new antineoplastic agents.
UR - http://www.scopus.com/inward/record.url?scp=68849087436&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=68849087436&partnerID=8YFLogxK
U2 - 10.1158/1535-7163.MCT-09-0366
DO - 10.1158/1535-7163.MCT-09-0366
M3 - Short survey
C2 - 19671735
AN - SCOPUS:68849087436
SN - 1535-7163
VL - 8
SP - 2086
EP - 2095
JO - Molecular cancer therapeutics
JF - Molecular cancer therapeutics
IS - 8
ER -