Cover Feature: Highly Selective and Potent Human β‐Secretase 2 (BACE2) Inhibitors against Type 2 Diabetes: Design, Synthesis, X‐ray Structure and Structure–Activity Relationship Studies (ChemMedChem 5/2019). (5th March 2019)

• Record Type: Journal Article
• Authors: Ghosh, Arun K.; Brindisi, Margherita; Yen, Yu‐Chen; Lendy, Emma K.; Kovela, Satish; Cárdenas, Emilio Leal; Reddy, Bhavanam Sekhara; Rao, Kalapala Venketeswara; Downs, Deborah; Huang, Xiangping; Tang, Jordan; Mesecar, Andrew D.
• Is Part Of: ChemMedChem. Volume 14:Number 5(2019)
• Page Start: 513
• Page End: 513
• Publication Date: 2019-03-05
• Subjects: BACE2 inhibitors -- structure-based design -- Tmem27 -- type 2 diabetes -- β-secretase 2; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201900100
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract : The Cover Feature shows the X‐ray structure of β‐secretase 1 bound to compound2a (top). The structure was utilized to create an active model of2a with β‐secretase 2, which led to the design and synthesis of highly potent and selective β‐secretase 2 inhibitor2d (CPK green picture, bottom) with potential for a new treatment of type 2 diabetes. A commemorative statue of Purdue graduate, Neil Armstrong, the first human to step on the moon surface (footsteps, bottom right), looks onward at Purdue University. He is forever a symbol of the incredible human spirit that continues to strive for that next great achievement. Cover art created by Anando John Ghosh. More information can be found in the Full Paper by Arun K. Ghosh et al. onpage 545 in Issue 5, 2019 (DOI:10.1002/cmdc.201800725 ).