Display options
Cite
Khwaja S, Kumar K, Das R, et al. Microtubule associated proteins as targets for anticancer drug development. Bioorg Chem. 2021;116:105320doi: 10.1016/j.bioorg.2021.105320.
Khwaja, S., Kumar, K., Das, R., & Negi, A. S. (2021). Microtubule associated proteins as targets for anticancer drug development. Bioorganic chemistry, 116105320. https://doi.org/10.1016/j.bioorg.2021.105320
Khwaja, Sadiya, et al. "Microtubule associated proteins as targets for anticancer drug development." Bioorganic chemistry vol. 116 (2021): 105320. doi: https://doi.org/10.1016/j.bioorg.2021.105320
Khwaja S, Kumar K, Das R, Negi AS. Microtubule associated proteins as targets for anticancer drug development. Bioorg Chem. 2021 Nov;116:105320. doi: 10.1016/j.bioorg.2021.105320. Epub 2021 Sep 01. PMID: 34492559.
Copy Download .nbib Format: NLM
Share it on

Bioorg Chem. 2021 Nov;116:105320. doi: 10.1016/j.bioorg.2021.105320. Epub 2021 Sep 01.

Microtubule associated proteins as targets for anticancer drug development.

Bioorganic chemistry

Sadiya Khwaja, Kapil Kumar, Ranjana Das, Arvind Singh Negi

Affiliations

  1. CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.
  2. CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India.
  3. CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address: [email protected].

PMID: 34492559 DOI: 10.1016/j.bioorg.2021.105320

Abstract

The dynamic equilibrium of tubulin-microtubule is an essential aspect of cell survivality. Modulation of this dynamics has become an important target for the cancer drug development. Tubulin exists in the alpha-beta dimer form which polymerizes to form microtubule and further depolymerizes back to tubulin dimer. The microtubule plays an essential role in mitosis and cell multiplication. Antitubulin drugs disturb the microtubule dynamics which is essentially required for DNA segregation and cell division during mitosis so killing the cancerous cells. Microtubule Associated Proteins (MAPs) interact with cellular cytoskeletal microtubules. MAPs bind to the either polymerized or depolymerized tubulin dimers within the cell and mostly causing stabilization of microtubules. Some of the tubulin binding drugs are in clinical use and others in clinical trial. MAPs inhibitors are also in clinical trial. Post-translational modification of lysine-40 either in histone or in alpha tubulin has an important role in gene expression and is balanced between histone deacetylases (HDACs) and histone acetyltransferases (HATs). HDAC inhibitors have the anticancer properties to form a drug for the treatment of cancer. They act by inducing cell cycle arrest and cell death. Some of the HDAC inhibitors are approved to be used as anticancer drug while others are under different phases of clinical trial. The present review updates on various MAPs, their role in cancer progression, MAPs inhibitors and their future prospects.

Copyright © 2021 Elsevier Inc. All rights reserved.

Keywords: Cancer chemotherapeutics; Histone acetyl transferase; Histone deacetylase; Microtubule associated proteins; Tubulin

Publication Types