Alzheimer's disease, enzyme targets and drug discovery struggles: from natural products to drug prototypes

T Silva, J Reis, J Teixeira, F Borges - Ageing research reviews, 2014 - Elsevier
enzymatic targets for AD, like β- and γ-secretases, sirtuins, caspase proteins and glycogen
synthase kinase-3 (GSK-3). In addition, new mechanistic rationales for drug … recent enzymatic

Current advances in antitubercular drug discovery: Potent prototypes and new targets

G Felipe dos Santos Fernandes… - Current medicinal …, 2015 - ingentaconnect.com
… Thus, this enzyme has emerged as a promising target to treat TB. The screening of 1500
molecules from the AstraZeneca library identified the compound dihydrobenzofuranyl urea (78) …

Molecular hybridization: a useful tool in the design of new drug prototypes

C Viegas-Junior, A Danuello… - Current medicinal …, 2007 - ingentaconnect.com
… efficient antihypertensive drugs were inhibitors of the angiotensinconverting enzyme (ACE), …
of the resistance to the treatment by multi-target drugs. On the other hand, the inferior …

Donepezil: an important prototype to the design of new drug candidates for Alzheimer's disease

M Cecilia Rodrigues Simoes… - Mini reviews in …, 2014 - ingentaconnect.com
enzyme active site, blocking the access of the ligand to the binding site, although the new
ligand was capable to reach the enzymatic target with adequate lipophilicity (log P = 3.35) [12]. …

Targeting proteases: successes, failures and future prospects

B Turk - Nature reviews Drug discovery, 2006 - nature.com
… has since remained a prototype for a proteolytic cascade in … drug targets, and to be able to
validate them as targets and … zinc moiety in the enzyme's active site; and they target only the S1…

Developing drug prototypes: pharmacology replaces safety and tolerability?

AF Cohen - Nature Reviews Drug Discovery, 2010 - nature.com
… New medicines are designed to bind to receptors or enzymes and are tested in animal cells,
… has already led to an explosion of potential drug targets. These may not have led to the …

[HTML][HTML] Therapeutic potential of prodrugs towards targeted drug delivery

AP Mishra, S Chandra, R Tiwari… - The open medicinal …, 2018 - ncbi.nlm.nih.gov
… to target specific enzymes or carriers by considering enzyme-substrate specificity or
carrier-substrate specificity in order to overcome various undesirable drug … active prototypes or …

Target-related applications of first principles quantum chemical methods in drug design

A Cavalli, P Carloni, M Recanatini - Chemical reviews, 2006 - ACS Publications
enzymes of this family are very important targets for therapeutic interventions, while others
have a fundamental role in the metabolism of drugs and … ) receptor, the prototype of the ligand-…

New approaches to difficult drug targets: the phosphatase story

JS Lazo, KE McQueeney… - … Advancing Life Sciences …, 2017 - journals.sagepub.com
… tyrosine phosphatase dysfunction and use some prototype contemporary strategies to illustrate
… protein drug targets into three major groups. The most common drug targets are enzymes

New targets and screening approaches in antimicrobial drug discovery

ED Brown, GD Wright - Chemical reviews, 2005 - ACS Publications
… The ideal target typically is an enzyme with fully elucidated function and mechanism (Table …
structure is circularly permuted relative to prototype GTPases such as Ras. Biochemical …