Literature DB >> 15582402

Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).

Arun K Ghosh1, Thippeswamy Devasamudram, Lin Hong, Christopher DeZutter, Xiaoming Xu, Vajira Weerasena, Gerald Koelsch, Geoffrey Bilcer, Jordan Tang.   

Abstract

A series of novel macrocyclic amide-urethanes was designed and synthesized based upon the X-ray crystal structure of our lead inhibitor (1, OM99-2 with eight residues) bound to memapsin 2. Ring size and substituent effects have been investigated. Cycloamide-urethanes containing 14- to 16-membered rings exhibited low nanomolar inhibitory potencies against human brain memapsin 2 (beta-secretase).

Entities:  

Mesh：

Substances：

Year:  2005        PMID： 15582402     DOI： 10.1016/j.bmcl.2004.10.084

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


  13 in total

1.  Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.

Authors:  Arun K Ghosh; Nagaswamy Kumaragurubaran; Lin Hong; Sarang Kulkarni; Xiaoming Xu; Heather B Miller; Dandepally Srinivasa Reddy; Vajira Weerasena; Robert Turner; Wanpin Chang; Gerald Koelsch; Jordan Tang
Journal:  Bioorg Med Chem Lett       Date:  2008-01-03       Impact factor: 2.823

2.  In silico screening of potential β-secretase (BACE1) inhibitors from VIETHERB database.

Authors:  Nguyen Thao Nhung; Nhung Duong; Huong Thi Thu Phung; Quan V Vo; Nguyen Minh Tam
Journal:  J Mol Model       Date:  2022-02-14       Impact factor: 1.810

3.  Development of an Efficient Enzyme Production and Structure-Based Discovery Platform for BACE1 Inhibitors.

Authors:  Yu-Chen Yen; Annalissa M Kammeyer; Katherine C Jensen; Jagannadharao Tirlangi; Arun K Ghosh; Andrew D Mesecar
Journal:  Biochemistry       Date:  2019-10-22       Impact factor: 3.162

Review 4.  beta-Secretase as a therapeutic target for Alzheimer's disease.

Authors:  Arun K Ghosh; Sandra Gemma; Jordan Tang
Journal:  Neurotherapeutics       Date:  2008-07       Impact factor: 7.620

5.  Protein flexibility in virtual screening: the BACE-1 case study.

Authors:  Sandro Cosconati; Luciana Marinelli; Francesco Saverio Di Leva; Valeria La Pietra; Angela De Simone; Francesca Mancini; Vincenza Andrisano; Ettore Novellino; David S Goodsell; Arthur J Olson
Journal:  J Chem Inf Model       Date:  2012-10-08       Impact factor: 4.956

Review 6.  Disease-modifying approach to the treatment of Alzheimer's disease: from alpha-secretase activators to gamma-secretase inhibitors and modulators.

Authors:  Francesco Panza; Vincenzo Solfrizzi; Vincenza Frisardi; Cristiano Capurso; Alessia D'Introno; Anna M Colacicco; Gianluigi Vendemiale; Antonio Capurso; Bruno P Imbimbo
Journal:  Drugs Aging       Date:  2009       Impact factor: 3.923

Review 7.  Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.

Authors:  Arun K Ghosh
Journal:  J Med Chem       Date:  2009-04-23       Impact factor: 7.446

8.  Structure of the complex of porcine pancreatic elastase with a trimacrocyclic peptide inhibitor FR901451.

Authors:  Takayoshi Kinoshita; Tomoya Kitatani; Masaichi Warizaya; Toshiji Tada
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2005-08-31

Review 9.  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

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
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.