Literature DB >> 16690314

BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.

Craig A Coburn1, Shawn J Stachel, Kristen G Jones, Thomas G Steele, Diane M Rush, Jillian DiMuzio, Beth L Pietrak, Ming-Tain Lai, Qian Huang, Janet Lineberger, Lixia Jin, Sanjeev Munshi, M Katharine Holloway, Amy Espeseth, Adam Simon, Daria Hazuda, Samuel L Graham, Joseph P Vacca.   

Abstract

A series of beta-site amyloid precursor protein cleaving enzyme (BACE-1) inhibitors containing a psi(CH2NH) reduced amide bond were synthesized. Incorporation of this reduced amide isostere as a non-cleavable peptide surrogate afforded inhibitors possessing low nanomolar potencies in both an enzymatic and cell-based assay.

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Year:  2006        PMID： 16690314     DOI： 10.1016/j.bmcl.2006.04.076

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  12 in total

1.  Modulation of lipid membrane structural and mechanical properties by a peptidomimetic derived from reduced amide scaffold.

Authors:  Nawal K Khadka; Peng Teng; Jianfeng Cai; Jianjun Pan
Journal:  Biochim Biophys Acta Biomembr       Date:  2017-01-26       Impact factor: 3.747

2.  Small Antimicrobial Agents Based on Acylated Reduced Amide Scaffold.

Authors:  Peng Teng; Da Huo; Alekhya Nimmagadda; Jianfeng Wu; Fengyu She; Ma Su; Xiaoyang Lin; Jiyu Yan; Annie Cao; Chuanwu Xi; Yong Hu; Jianfeng Cai
Journal:  J Med Chem       Date:  2016-08-25       Impact factor: 7.446

3.  D3R Grand Challenge 4: ligand similarity and MM-GBSA-based pose prediction and affinity ranking for BACE-1 inhibitors.

Authors:  Sukanya Sasmal; Léa El Khoury; David L Mobley
Journal:  J Comput Aided Mol Des       Date:  2019-11-28       Impact factor: 3.686

Review 4.  The structural evolution of β-secretase inhibitors: a focus on the development of small-molecule inhibitors.

Authors:  Stefania Butini; Simone Brogi; Ettore Novellino; Giuseppe Campiani; Arun K Ghosh; Margherita Brindisi; Sandra Gemma
Journal:  Curr Top Med Chem       Date:  2013       Impact factor: 3.295

Review 5.  The "Sticky Patch" Model of Crystallization and Modification of Proteins for Enhanced Crystallizability.

Authors:  Zygmunt S Derewenda; Adam Godzik
Journal:  Methods Mol Biol       Date:  2017

Review 6.  BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease.

Authors:  Arun K Ghosh; Heather L Osswald
Journal:  Chem Soc Rev       Date:  2014-10-07       Impact factor: 54.564

7.  Structure-based design of highly selective β-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.

Authors:  Arun K Ghosh; Kalapala Venkateswara Rao; Navnath D Yadav; David D Anderson; Navnath Gavande; Xiangping Huang; Simon Terzyan; Jordan Tang
Journal:  J Med Chem       Date:  2012-09-06       Impact factor: 7.446

8.  It's all in the crystals….

Authors:  Zygmunt S Derewenda
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2011-03-18

9.  Potent BACE-1 inhibitor design using pharmacophore modeling, in silico screening and molecular docking studies.

Authors:  Shalini John; Sundarapandian Thangapandian; Sugunadevi Sakkiah; Keun Woo Lee
Journal:  BMC Bioinformatics       Date:  2011-02-15       Impact factor: 3.169

10.  Exploring the binding of BACE-1 inhibitors using comparative binding energy analysis (COMBINE).

Authors:  Shu Liu; Rao Fu; Xiao Cheng; Sheng-Ping Chen; Li-Hua Zhou
Journal:  BMC Struct Biol       Date:  2012-08-27
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