Second-generation CK2α inhibitors targeting the αd pocket
Chemical Science, ISSN: 2041-6539, Vol: 9, Issue: 11, Page: 3041-3049
2018
- 32Citations
- 40Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations32
- Citation Indexes32
- 32
- CrossRef30
- Captures40
- Readers40
- 40
Article Description
CK2 is a critical cell cycle regulator that also promotes various anti-apoptotic mechanisms. Development of ATP-non-competitive inhibitors of CK2 is a very attractive strategy considering that the ATP binding site is highly conserved among other kinases. We have previously utilised a pocket outside the active site to develop a novel CK2 inhibitor, CAM4066. Whilst CAM4066 bound to this new pocket it was also interacting with the ATP site: herein, we describe an example of a CK2α inhibitor that binds completely outside the active site. This second generation αD-site binding inhibitor, compound CAM4712 (IC = 7 μM, GI = 10.0 ± 3.6 μM), has numerous advantages over the previously reported CAM4066, including a reduction in the number of rotatable bonds, the absence of amide groups susceptible to the action of proteases and improved cellular permeability. Unlike with CAM4066, there was no need to facilitate cellular uptake by making a prodrug. Moreover, CAM4712 displayed no drop off between its ability to inhibit the kinase in vitro (IC) and the ability to inhibit cell proliferation (GI).
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85044064325&origin=inward; http://dx.doi.org/10.1039/c7sc05122k; http://www.ncbi.nlm.nih.gov/pubmed/29732088; https://xlink.rsc.org/?DOI=C7SC05122K; https://dx.doi.org/10.1039/c7sc05122k; https://pubs.rsc.org/en/content/articlelanding/2018/sc/c7sc05122k
Royal Society of Chemistry (RSC)
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