| A bright approach to the immunoproteasome: Development of LMP2/β1i-specific imaging probes. | |
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MedLine Citation:
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PMID: 21741845 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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While the constitutive, 26S proteasome plays an important role in regulating many important cellular processes, a variant form known as the immunoproteasome is thought to primarily function in adaptive immune responses. However, recent studies indicate an association of immunoproteasomes with many physiological disorders such as cancer, neurodegenerative, and inflammatory diseases. Despite this, the detailed functions of the immunoproteasome remain poorly understood. Immunoproteasome-specific probes are essential to gain insight into immunoproteasome function. Here, we describe for the first time the development of cell-permeable activity-based fluorescent probes, UK101-Fluor and UK101-B660, which selectively target the catalytically active LMP2/β1i subunit of the immunoproteasome. These probes facilitate rapid detection of the cellular localization of catalytically active immunoproteasomes in living cells, providing a valuable tool to analyze immunoproteasome functions. Additionally, as LMP2/β1i may serve as a potential tumor biomarker, an LMP2/β1i-targeting fluorescent imaging probe may be applicable to a rapid readout assay to determine tumor LMP2/β1i levels. |
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Authors:
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Kimberly Cornish Carmony; Do-Min Lee; Ying Wu; Na-Ra Lee; Marie Wehenkel; Jason Lee; Chang-Guo Zhan; Kyung-Bo Kim |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-7-7 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: - ISSN: 1464-3391 ISO Abbreviation: - Publication Date: 2011 Jul |
Date Detail:
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Created Date: 2011-7-11 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Pharmaceutical Science, College of Pharmacy, University of Kentucky, Lexington, KY 40536, USA. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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