PMID- 26706241
OWN - NLM
STAT- MEDLINE
DCOM- 20170317
LR  - 20170317
IS  - 1879-016X (Electronic)
IS  - 0163-7258 (Linking)
VI  - 162
DP  - 2016 Jun
TI  - Microtubule-stabilizing agents: New drug discovery and cancer therapy.
PG  - 134-43
LID - S0163-7258(15)00232-6 [pii]
LID - 10.1016/j.pharmthera.2015.12.006 [doi]
AB  - Microtubule-stabilizing agents (MSAs) have been highly successful in the 
      treatment of cancer in the past 20years. To date, three classes of MSAs have 
      entered the clinical trial stage or have been approved for clinical anticancer 
      chemotherapy, and more than 10 classes of novel structural MSAs have been derived 
      from natural resources. The microtubule typically contains two MSA-binding sites: 
      the taxoid site and the laulimalide/peloruside site. All defined MSAs are known 
      to bind at either of these sites, with subtle but significant differences. MSAs 
      with different binding sites may produce a synergistic effect. Although having 
      been extensively applied in the clinical setting, paclitaxel and other approved 
      MSAs still pose many challenges such as multidrug resistance, low 
      bioavailability, poor solubility, high toxicity, and low passage through the 
      blood-brain barrier. A variety of studies focus on the structure-activity 
      relationship in order to improve the pharmaceutical properties of these agents. 
      Here, the mechanisms of action, advancements in pharmacological research, and 
      clinical developments of defined MSAs during the past decade are discussed. The 
      latest discovered MSAs are also briefly introduced in this review. The increasing 
      number of natural MSAs indicates the potential discovery of more novel, natural 
      MSAs with different structural bases, which will further promote the development 
      of anticancer chemotherapy.
CI  - Copyright (c) 2016. Published by Elsevier Inc.
FAU - Zhao, Ying
AU  - Zhao Y
AD  - Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union 
      Medical College, Xiannongtan 1, Xicheng District, Beijing 100050, PR China; 
      Chinese Pharmacological Society, Beijing 100050, PR China. Electronic address: 
      zhaoying@imm.ac.cn.
FAU - Mu, Xin
AU  - Mu X
AD  - Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union 
      Medical College, Xiannongtan 1, Xicheng District, Beijing 100050, PR China; 
      Chinese Pharmacological Society, Beijing 100050, PR China. Electronic address: 
      muxin@imm.ac.cn.
FAU - Du, Guanhua
AU  - Du G
AD  - Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union 
      Medical College, Xiannongtan 1, Xicheng District, Beijing 100050, PR China; 
      Chinese Pharmacological Society, Beijing 100050, PR China. Electronic address: 
      dugh@imm.ac.cn.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20151217
PL  - England
TA  - Pharmacol Ther
JT  - Pharmacology & therapeutics
JID - 7905840
RN  - 0 (Antineoplastic Agents)
SB  - IM
MH  - Antineoplastic Agents/*pharmacology/*therapeutic use
MH  - Drug Discovery
MH  - Humans
MH  - Microtubules/*drug effects
MH  - Neoplasms/*drug therapy
OTO - NOTNLM
OT  - Cancer therapy
OT  - Epothilone
OT  - Microtubule-stabilizing agent
OT  - Natural product
OT  - Paclitaxel
EDAT- 2015/12/27 06:00
MHDA- 2017/03/18 06:00
CRDT- 2015/12/27 06:00
PHST- 2015/12/27 06:00 [entrez]
PHST- 2015/12/27 06:00 [pubmed]
PHST- 2017/03/18 06:00 [medline]
AID - S0163-7258(15)00232-6 [pii]
AID - 10.1016/j.pharmthera.2015.12.006 [doi]
PST - ppublish
SO  - Pharmacol Ther. 2016 Jun;162:134-43. doi: 10.1016/j.pharmthera.2015.12.006. Epub 
      2015 Dec 17.