α-Lipoic acid-based PPARγ agonists for treating inflammatory skin diseases
dc.contributor.author | Ho, Christopher I. | en_US |
dc.contributor.author | Varani, James | en_US |
dc.contributor.author | Benson, Stephen C. | en_US |
dc.contributor.author | Kurtz, Theodore W. | en_US |
dc.contributor.author | Meingassner, Josef | en_US |
dc.contributor.author | Pershadsingh, Harrihar A. | en_US |
dc.contributor.author | Avery, Mitchell A. | en_US |
dc.contributor.author | Ellis, Charles N. | en_US |
dc.contributor.author | Chittiboyina, Amar | en_US |
dc.contributor.author | Venkatraman, Meenakshi S. | en_US |
dc.date.accessioned | 2006-09-11T18:45:46Z | |
dc.date.available | 2006-09-11T18:45:46Z | |
dc.date.issued | 2004-08 | en_US |
dc.identifier.citation | Venkatraman, Meenakshi S.; Chittiboyina, Amar; Meingassner, Josef; Ho, Christopher I.; Varani, James; Ellis, Charles N.; Avery, Mitchell A.; Pershadsingh, Harrihar A.; Kurtz, Theodore W.; Benson, Stephen C.; (2004). "α-Lipoic acid-based PPARγ agonists for treating inflammatory skin diseases." Archives of Dermatological Research 296(3): 97-104. <http://hdl.handle.net/2027.42/47251> | en_US |
dc.identifier.issn | 1432-069X | en_US |
dc.identifier.issn | 0340-3696 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/47251 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=15221328&dopt=citation | en_US |
dc.description.abstract | Novel thiazolidinedione derivatives of the potent antioxidant, α-lipoic (thioctic, 1,2-dithiolane) acid, were prepared. The prototype N -(2-{4-[2,4-dioxo(1,3-thiazolidin-5-yl)methyl]phenoxy}ethyl)-5-(1,2-dithiolan-3-yl)- N -methylpentanamide (designated BP-1003), and dithioester derivatives thereof were shown to be potent activators of peroxisome proliferator-activated receptor gamma (PPARγ) (EC 50 range 15–101 n M ) and modest activators of PPARα (EC 50 5 μ M ). Both the relatively hydrophobic dithiolane prototype, BP-1003, and its water-soluble dithioglycinate derivative, BP-1017, were shown to inhibit the proliferation of human keratinocytes and suppress the production of interleukin-2 by human peripheral lymphocytes to a greater extent than the antidiabetic thiazolidinedione, rosiglitazone. Both oral and topical administration of BP-1017 showed significant antiinflammatory effects in the oxazolone-sensitized mouse model of allergic contact dermatitis (ACD). These findings suggest that water-soluble lipoic acid-based thiazolidinediones may be efficacious as oral and topical agents for treating inflammatory skin conditions such as contact dermatitis, atopic dermatitis, and psoriasis. | en_US |
dc.format.extent | 392748 bytes | |
dc.format.extent | 3115 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Springer-Verlag | en_US |
dc.subject.other | Thiazolidinedione | en_US |
dc.subject.other | Dermatitis | en_US |
dc.subject.other | Inflammation | en_US |
dc.subject.other | Peroxisome Proliferator-activated Receptor-γ | en_US |
dc.subject.other | Psoriasis | en_US |
dc.subject.other | α-Lipoic Acid | en_US |
dc.title | α-Lipoic acid-based PPARγ agonists for treating inflammatory skin diseases | en_US |
dc.type | Article | en_US |
dc.subject.hlbsecondlevel | Dermatology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Department of Dermatology, University of Michigan Medical School, Ann Arbor, MI, USA | en_US |
dc.contributor.affiliationum | Department of Pathology, University of Michigan Medical School, Ann Arbor, MI, USA | en_US |
dc.contributor.affiliationother | Department of Biological Sciences, California State University, 25800 Carlos Bee Blvd, Hayward, CA 94542, USA | en_US |
dc.contributor.affiliationother | Novartis Forschungsinstitut GmbH, Vienna, Austria | en_US |
dc.contributor.affiliationother | Bethesda Pharmaceuticals, Inc, Bakersfield, CA, USA; Department of Laboratory Medicine, University of California, San Francisco, CA, USA | en_US |
dc.contributor.affiliationother | Department of Family Medicine, Kern Medical Center, Bakersfield, CA, USA; Department of Family Medicine, University of California, Irvine, CA, USA | en_US |
dc.contributor.affiliationother | Department Medicinal Chemistry, University of Mississippi, University, MS, USA | en_US |
dc.contributor.affiliationother | Department Medicinal Chemistry, University of Mississippi, University, MS, USA | en_US |
dc.contributor.affiliationother | Department Medicinal Chemistry, University of Mississippi, University, MS, USA | en_US |
dc.contributor.affiliationother | Department of Biological Sciences, California State University, 25800 Carlos Bee Blvd, Hayward, CA 94542, USA | en_US |
dc.contributor.affiliationumcampus | Ann Arbor | en_US |
dc.identifier.pmid | 15221328 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/47251/1/403_2004_Article_480.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1007/s00403-004-0480-5 | en_US |
dc.identifier.source | Archives of Dermatological Research | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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