Current Medicinal Chemistry
Current Medicinal Chemistry
5 years ago

Allosteric Targeting of Aurora A Kinase Using Small Molecules: A Step Forward Towards Next Generation Medicines?

Srinivasan R, Panicker RC, Coyne AG
Aurora A (AurA) kinase is a key mitotic protein essential for carrying out numerous cellular functions. Overexpression or malfunction of this enzyme results in numerous human diseases most notably in cancer. Several small molecule inhibitors targeting the ATP binding site of this enzyme are in various stages of clinical development. However, ATP binding site inhibitors can result in selectivity problems often leading to undesirable off-target effects. Moreover, these drugs are prone to drug resistance problem rendering them unfit for long-term administration. Allosteric inhibition of kinases using small molecules is an alternative strategy to target these enzymes and these could serve as the seeds for next generation medicines and minimize any selectivity problems associated with ATP binding site inhibitors. This review discusses the developments in the non-ATP site binding small molecule inhibitors of AurA and their prospect as future therapeutics and tools for chemical biology.

Publisher URL: https://www.ncbi.nlm.nih.gov/pubmed/28748768

DOI: PubMed:28748768

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.