| The potential for caspases in drug discovery. | |
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MedLine Citation:
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PMID: 20812148 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Caspases are a family of proteases that are involved in the execution of apoptosis and the inflammatory response. A plethora of diseases occur as a result of the dysregulation of apoptosis and inflammation, and caspases have been targeted as a therapeutic strategy to halt the progression of such diseases. Hundreds of peptide and peptidomimetic inhibitors have been designed and tested, but only a few have advanced to clinical trials because of poor drug-like properties and pharmacological constraints. Although much effort has been focused on inhibiting caspases, there are many diseases that result from a decrease in apoptosis, thus activating procaspases could also be a viable therapeutic strategy. To this end, recent efforts have focused on the design of procaspase-3 activators. This review highlights the current progress in the rational design of both specific and pan-caspase inhibitors, as well as procaspase-3 activators. |
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Authors:
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Sarah H MacKenzie; Joshua L Schipper; A Clay Clark |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Current opinion in drug discovery & development Volume: 13 ISSN: 2040-3437 ISO Abbreviation: Curr Opin Drug Discov Devel Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-09-02 Completed Date: 2011-01-18 Revised Date: 2012-02-29 |
Medline Journal Info:
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Nlm Unique ID: 100887519 Medline TA: Curr Opin Drug Discov Devel Country: England |
Other Details:
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Languages: eng Pagination: 568-76 Citation Subset: IM |
Affiliation:
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North Carolina State University, Department of Molecular and Structural Biochemistry, 128 Polk Hall, Raleigh, NC 27695, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Allosteric Regulation Allosteric Site Animals Apoptosis / drug effects Caspases / antagonists & inhibitors, metabolism* Drug Discovery / methods* Enzyme Activation / drug effects Enzyme Inhibitors / chemistry, pharmacology* Humans Models, Molecular Molecular Structure Peptidomimetics / chemistry, pharmacology* Small Molecule Libraries / chemistry, pharmacology* Structure-Activity Relationship |
| Grant Support | |
ID/Acronym/Agency:
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R01 GM065970-07/GM/NIGMS NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Enzyme Inhibitors; 0/Peptidomimetics; 0/Small Molecule Libraries; EC 3.4.22.-/Caspases |
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