An article Design, Synthesis, and Biological Evaluation of Novel Allosteric Protein Disulfide Isomerase Inhibitors WOS:000464768300019 published article about INDUCED NO PRODUCTION; MHC CLASS-I; CELL-DEATH; EXPRESSION; CHALCONES; GLIOBLASTOMA; DERIVATIVES; APOPTOSIS; GENE; TEMOZOLOMIDE in [Yang, Suhui; Shergalis, Andrea; Lu, Dan; Kyani, Anahita; Liu, Ziwei; Neamati, Nouri] Univ Michigan, Dept Med Chem, Coll Pharm, Rogel Canc Ctr, North Campus Res Complex,1600 Huron Pkwy, Ann Arbor, MI 48109 USA; [Ljungman, Mats] Univ Michigan, Sch Med, Rogel Canc Ctr, Dept Radiat Oncol, Ann Arbor, MI 48109 USA; [Ljungman, Mats] Sch Publ Hlth, Rogel Canc Ctr, Ann Arbor, MI 48109 USA; [Yang, Suhui] Amer Univ Hlth Sci, Sch Pharm, Dept Pharmaceut Sci, 1600 East Hill St, Signal Hill, CA 90755 USA in 2019.0, Cited 70.0. Product Details of 100-19-6. The Name is 1-(4-Nitrophenyl)ethanone. Through research, I have a further understanding and discovery of 100-19-6
Protein disulfide isomerase (PDI) is responsible for nascent protein folding in the endoplasmic reticulum (ER) and is critical for glioblastoma survival. To improve the potency of lead PDI inhibitor BAP2 ((E)-3-(3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl)benzonitrile), we designed and synthesized 67 analogues. We determined that PDI inhibition relied on the A ring hydroxyl group of the chalcone scaffold and cLogP increase in the sulfonamide chain improved potency. Docking studies revealed that BAP2 and analogues bind to His256 in the b’ domain of PDI, and mutation of His256 to Ala abolishes BAP2 analogue activity. BAP2 and optimized analogue 59 have modest thiol reactivity; however, we propose that PDI inhibition by BAP2 analogues depends on the b’ domain. Importantly, analogues inhibit glioblastoma cell growth, induce ER stress, increase expression of G2M checkpoint proteins, and reduce expression of DNA repair proteins. Cumulatively, our results support inhibition of PDI as a novel strategy to treat glioblastoma.
Product Details of 100-19-6. Welcome to talk about 100-19-6, If you have any questions, you can contact Yang, SH; Shergalis, A; Lu, D; Kyani, A; Liu, ZW; Ljungman, M; Neamati, N or send Email.
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Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem