Role of Ligand-Based Drug Design Methodologies toward the Discovery of New Anti-Alzheimer Agents: Futures Perspectives in Fragment-Based Ligand Design

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

Authors

Speck Planche, A (Author) Other; Luan, F (Author) Other; Cordeiro, MNDS (Author) FCUP

Journal

Title: Current Medicinal Chemistry

Vol. 19

Pages: 1635-1645

ISSN: 0929-8673

Publisher: Bentham Science

Indexing

ISI Web of Knowledge - 37 Citations

Scopus - 39 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-BEV

DOI: 10.2174/092986712799945058

Abstract (EN): Alzheimer's disease (AD), a degenerative disease affecting the brain, is the single most common source of dementia in adults. The cause and the progression of AD still remains a mystery among medical experts. As a result, a cure has not yet been discovered, even after decade's worth of research that started since 1906, when the disease was first identified. Despite the efforts of the scientific community, several of the biological receptors associated with AD have not been sufficiently studied to date, limiting in turn the design of new and more potent anti-AD agents. Thus, the search for new drug candidates as inhibitors of different targets associated with AD constitutes an essential part towards the discovery of new and more efficient anti-AD therapies. The present work is focused on the role of the Ligand-Based Drug Design (LBDD) methodologies which have been applied for the elucidation of new molecular entities with high inhibitory activity against targets related with AD. Particular emphasis is given also to the current state of fragment-based ligand approaches as alternatives of the Fragment-Based Drug Discovery (FBDD) methodologies. Finally, several guidelines are offered to show how the use of fragment-based descriptors can be determinant for the design of multi-target inhibitors of proteins associated with AD.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11