List of Drugs in Development for Neurodegenerative Diseases

Valentine, Lisa; Kwon, Myoung-Ok; Herrling, Paul L.

doi:10.1159/000085066

Cited by 2 publications

(1 citation statement)

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“…Other series comprised sulfonamides [145] and sulfamides [146], as well as benzodiazepins [147] and benzolactams (Fig. However, none of these compounds, with the exception of LY450139 (currently in phase II clinical trials) [148,149], progressed beyond phase I clinical trials. Most -secretase inhibitors successfully abrogated generation of A peptides in in vitro systems and substantially reduced A levels in animal models.…”

Section: Intramembrane-cleaving Aspartic Pro-teases Presenilins and Sppmentioning

confidence: 99%

Aspartic Proteases in Drug Discovery

Eder¹,

Hommel²,

Cumin³

et al. 2007

CPD

119

103

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Aspartic proteases are the smallest class of human proteases with only 15 members. Over the past years, they have received considerable attention as potential targets for pharmaceutical intervention since many have been shown to play important roles in physiological and pathological processes. Despite numerous efforts, however, the only inhibitors for aspartic proteases currently on the market are directed against the HIV protease, an aspartic protease of viral origin. Nevertheless, several inhibitors including those targeting renin, BACE1 and gamma-secretase are in clinical or preclinical development, and some other aspartic proteases are discussed as potential drug target. The crystal structures of seven human aspartic proteases have now been solved and, together with a detailed kinetic understanding of their catalytic mechanism, this has greatly contributed to the design and discovery of novel inhibitors for this protease class. This review describes current aspartic protease drug targets and summarizes the drug discovery efforts in this field. In addition, it highlights recent developments which may lead to a new generation of aspartic protease inhibitors.

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Section: Intramembrane-cleaving Aspartic Pro-teases Presenilins and Sppmentioning

confidence: 99%

Aspartic Proteases in Drug Discovery

Eder¹,

Hommel²,

Cumin³

et al. 2007

CPD

119

103

View full text Add to dashboard Cite

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Novel cholinesterase inhibitors as future effective drugs for the treatment of Alzheimer’s disease

Martı́nez¹,

Castro²

2005

Expert Opinion on Investigational Drugs

106

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Current pharmacotherapy for Alzheimer's disease involves compounds that are aimed at increasing the levels of acetylcholine in the brain by facilitating cholinergic neurotransmission through inhibition of cholinesterase. These drugs, known as acetylcholinesterase inhibitors, have been shown to improve cognition and global functions but have little impact on improving the eventual progression of the disease; however, there is evidence that other cholinesterases such as butyrylcholinesterase can play an important role in cholinergic function in the brain, and the long-suspected non-cholinergic actions of acetylcholinesterase, mainly the interference with the beta-amyloid protein cascade, have recently driven a profound revolution in cholinesterase drug research. Several disease-modifying agents are under development that target these enzymes and have hope of becoming the next generation of effective drugs in the treatment of Alzheimer's disease.

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List of Drugs in Development for Neurodegenerative Diseases

Cited by 2 publications

References 0 publications

Aspartic Proteases in Drug Discovery

Aspartic Proteases in Drug Discovery

Novel cholinesterase inhibitors as future effective drugs for the treatment of Alzheimer’s disease

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