An article Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the Selectivity Pocket, Substrate-Binding Site, and NAD(+)-Binding Site WOS:000473251200008 published article about HISTONE DEACETYLASE SIRT6; GLUCOSE-HOMEOSTASIS; TUMOR-SUPPRESSOR; PROTEIN; CANCER; PROMOTES; PGC-1-ALPHA; ACTIVATION; CHROMAN-4-ONE; ACETYLATION in [Mellini, Paolo; Itoh, Yukihiro; Elboray, Elghareeb E.; Li, Ying; Suzuki, Miki; Takahashi, Yukari; Tojo, Toshifumi; Kurohara, Takashi; Miyake, Yuka; Kitao, Yuki; Kotoku, Masayuki; Iida, Tetsuya; Suzuki, Takayoshi] Kyoto Prefectural Univ Med, Grad Sch Med Sci, Sakyo Ku, 1-5 Shimogamohangi Cho, Kyoto 6060823, Japan; [Elboray, Elghareeb E.] South Valley Univ, Fac Sci, Chem Dept, Qena 83523, Egypt; [Tsumoto, Hiroki; Miura, Yuri] Tokyo Metropolitan Inst Gerontol, Res Team Mech Aging, Itabashi Ku, 35-2 Sakae Cho, Tokyo 1730015, Japan; [Suzuki, Takayoshi] Japan Sci & Technol Agcy JST, CREST, 4-1-8 Honcho Kawaguchi, Saitama 3320012, Japan in 2019, Cited 90. Name: 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6
The NAD(+)-dependent deacetylase SIRT2 represents an attractive target for drug development. Here, we designed and synthesized drug-like SIRT2-selective inhibitors based on an analysis of the putative binding modes of recently reported SIRT2-selective inhibitors and evaluated their SIRT2-inhibitory activity. This led us to develop a more drug-like diketopiperazine structure as a hydrogen bond (H-bond) hunter to target the substrate-binding site of SIRT2. Thioamide 53, a conjugate of diketopiperazine and 2-anilinobenzamide which is expected to occupy the selectivity pocket of SIRT2, exhibited potent SIRT2-selective inhibition. Inhibition of SIRT2 by 53 was mediated by the formation of a 53-ADP-ribose conjugate, suggesting that 53 is a mechanism-based inhibitor targeting the selectivity pocket, substrate-binding site, and NAD(+)-binding site. Furthermore, 53 showed potent antiproliferative activity toward breast cancer cells and promoted neurite outgrowth of Neuro-2a cells. These findings should pave the way for the discovery of novel therapeutic agents for cancer and neurological disorders.
Welcome to talk about 88-68-6, If you have any questions, you can contact Mellini, P; Itoh, Y; Elboray, EE; Tsumoto, H; Li, Y; Suzuki, M; Takahashi, Y; Tojo, T; Kurohara, T; Miyake, Y; Miura, Y; Kitao, Y; Kotoku, M; Iida, T; Suzuki, T or send Email.. Name: 2-Aminobenzamide
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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem