lead compounds of an eef2k inhibitor (Chembridge)
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lead compounds of an eef2k inhibitor
Lead Compounds Of An Eef2k Inhibitor, supplied by Chembridge, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/lead+compounds+of+an+eef2k+inhibitor/lead+compounds+of+an+eef2k+inhibitor/pm29202403-47-11-14
Average 90 stars, based on 1 article reviews
Lead Compounds Of An Eef2k Inhibitor, supplied by Chembridge, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/lead+compounds+of+an+eef2k+inhibitor/lead+compounds+of+an+eef2k+inhibitor/pm29202403-47-11-14
Average 90 stars, based on 1 article reviews
lead compounds of an eef2k inhibitor - by Bioz Stars,
2026-10
90/100 stars
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Modification:Article Title: Design, synthesis and structure-activity relationship of a focused library of β-phenylalanine derivatives as novel eEF2K inhibitors with apoptosis-inducing mechanisms in breast cancer. Article Snippet: Eukaryotic elongation factor 2 kinase (eEF2K) is a Ca2þ/calmudulin-dependent protein kinase, belonging to a small family of an atypical Ser/Thr-protein kinase. eEF2K has been recently reported to be highly activated or overexpressed in many types of cancer; therefore, eEF2K would be regarded as a promising therapeutic target.. In this study, we discovered a b-phenylalanine scaffold by virtual high-throughput screening, as well as designed and synthesized 46 derivatives with assessment of inhibition activity against eEF2K and cytotoxicity.. After several rounds of kinase and anti-proliferative activity screening, we discovered an eEF2K inhibitor (21l) with best eEF2K enzymatic activity (IC50 of 5.5 mM) and antiproliferative activity (MDA-MB-231 cells, IC50 of 12.6 mM, MDA-MB-436 cells, IC50 of 19.8 mM). |