Review of Synthesis, Assay, and Prediction of beta and gamma- secretase Inhibitors

• Type: Another Publication in an International Scientific Journal
• Date: 2012

Authors

Helena Nino (Author) Other; Jose Enrique Rodriguez Borges (Author) FCUP; Xerardo Garcia Mera (Author) Other; Francisco Prado Prado (Author) Other

Journal

Title: Current Topics in Medicinal Chemistry

Vol. 12

Pages: 828-844

ISSN: 1568-0266

Publisher: Bentham Science

Indexing

ISI Web of Knowledge - 7 Citations

Scopus - 9 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-BGW

DOI: 10.2174/156802612800166774

Abstract (EN): Alzheimer's disease (AD) is characterize with several pathologies this disease, amyloid plaques, composed of the beta-amyloid peptide and gamma-amyloid peptide are hallmark neuropathological lesions in Alzheimer's disease brain. Indeed, a wealth of evidence suggests that beta-amyloid is central to the pathophysiology of AD and is likely to play an early role in this intractable neurodegenerative disorder. AD is the most prevalent form of dementia, and current indications show that twenty-nine million people live with AD worldwide, a figure expected rise exponentially over the coming decades. Clearly, blocking disease progression or, in the best-case scenario, preventing AD altogether would be of benefit in both social and economic terms. However, current AD therapies are merely palliative and only temporarily slow cognitive decline, and treatments that address the underlying pathologic mechanisms of AD are completely lacking. While familial AD (FAD) is caused by autosomal dominant mutations in either amyloid precursor protein (APP) or the presenilin (PS1, PS2) genes. First, we revised Desing, synthesis, and Biological assay of beta and gamma-secretase inhibitors. Next, we review 2D QSAR, 3D QSAR, CoMFA, CoMSIA and Docking with different compound to find out the structural requirements. Next, we revised QSAR studies using method of Artificial Neural Network (ANN) in order to understand the essential structural requirement for binding with receptor for beta and gamma-secretase inhibitors.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 17