Browsing by Author "Chorev, Michael"
Now showing items 1-5 of 5
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1,4-Disubstituted-[1,2,3]triazolyl-Containing Analogues of MT-II: Design, Synthesis, Conformational Analysis, and Biological Activity
Testa, Chiara; Scrima, Mario; Grimaldi, Manuela; D’Ursi, Anna M.; Dirain, Marvin L.; Lubin-Germain, Nadège; Singh, Anamika; Haskell-Luevano, Carrie; Chorev, Michael; Rovero, Paolo; Papini, Anna M. (American Chemical Society, 2014)Side chain-to-side chain cyclizations represent a strategy to select a family of bioactive conformations by reducing the entropy and enhancing the stabilization of functional ligand-induced receptor conformations. This ... -
Chemical Genetics Identify eIF2α Kinase Heme Regulated Inhibitor as Anti-Cancer Target
Chen, Ting; Ozel, Duygu; Qiao, Yuan; Harbinski, Fred; Chen, Limo; Denoyelle, Séverine; He, Xiaoying; Zvereva, Nela; Supko, Jeffrey G.; Chorev, Michael; Halperin, Jose A.; Aktas, Bertal H. (2013)Translation initiation plays a critical role in cellular homeostasis, proliferation, differentiation and malignant transformation. Consistently, increasing the abundance of the eIF2·GTP·Met-tRNAi translation initiation ... -
Does Simvastatin Stimulate Bone Formation In Vivo?
von Stechow, Dietrich; Fish, Susan; Yahalom, Dror; Bab, Itai; Chorev, Michael; Müller, Ralph; Alexander, Joseph M (BioMed Central, 2003)Background: Statins, potent compounds that inhibit cholesterol synthesis in the liver have been reported to induce bone formation, both in tissue culture and in rats and mice. To re-examine potential anabolic effects of ... -
Synthesis of Rigidified eIF4E/eIF4G Inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein–Protein Interaction
Mahalingam, Poornachandran; Takrouri, Khuloud; Chen, Ting; Sahoo, Rupam; Papadopoulos, Evangelos; Chen, Limo; Wagner, Gerhard; Aktas, Bertal H.; Halperin, Jose A.; Chorev, Michael (American Chemical Society, 2014)The 4EGI-1 is the prototypic inhibitor of eIF4E/eIF4G interaction, a potent inhibitor of translation initiation in vitro and in vivo and an efficacious anticancer agent in animal models of human cancers. We report on the ... -
Tumor suppression by small molecule inhibitors of translation initiation
Chen, Limo; Aktas, Bertal H.; Wang, Yibo; He, Xiaoying; Sahoo, Rupam; Zhang, Nancy; Denoyelle, Severine; Kabha, Eihab; Yang, Hongwei; Freedman, Revital; Supko, Jeffrey G.; Chorev, Michael; Wagner, Gerhard; Halperin, Jose Alberto (Impact Journals LLC, 2012)Translation initiation factors are over-expressed and/or activated in many human cancers and may contribute to their genesis and/or progression. Removal of physiologic restraints on translation initiation causes malignant ...