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Shaw, Subrata; Bian, Zhiguo; Zhao, Bin; Tarr, James C; Veerasamy, Nagarathanam; Jeon, Kyu Ok; Belmar, Johannes; Arnold, Allison L; Fogarty, Stuart A; Perry, Evan; Sensintaffar, John L; Camper, DeMarco V; Rossanese, Olivia W; Lee, Taekyu; Olejniczak, Edward T; Fesik, Stephen W
Journal of medicinal chemistry, 03/2018, Letnik: 61, Številka: 6Journal Article
Myeloid cell leukemia 1 (Mcl-1), an antiapoptotic member of the Bcl-2 family of proteins, has emerged as an attractive target for cancer therapy. Mcl-1 upregulation is often found in many human cancers and is associated with high tumor grade, poor survival, and resistance to chemotherapy. Here, we describe a series of potent and selective tricyclic indole diazepinone Mcl-1 inhibitors that were discovered and further optimized using structure-based design. These compounds exhibit picomolar binding affinity and mechanism-based cellular efficacy, including growth inhibition and caspase induction in Mcl-1-sensitive cells. Thus, they represent useful compounds to study the implication of Mcl-1 inhibition in cancer and serve as potentially useful starting points toward the discovery of anti-Mcl-1 therapeutics.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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