Pharmacology and chemistry of adapalene
Background: Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins...
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Veröffentlicht in: | Journal of the American Academy of Dermatology 1997-06, Vol.36 (6), p.S96-S103 |
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container_title | Journal of the American Academy of Dermatology |
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creator | Shroot, Braham Michel, Serge |
description | Background:
Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins and hormones.
1
Objective:
We sought molecules with an optimal balance between stability, efficacy, and local tolerance for topical acne therapy.
Methods:
In vitro and in vivo bioassay systems were used to test the ability of retinoids to modulate cell proliferation and differentiation. In addition, antiinflammatory properties were assessed. Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).
Results and Conclusion:
Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation. In addition it has significant antiinflammatory action. The nuclear gene transcription factors RARβ and RARγ mediate the retinoid activity of adapalene. (J Am Acad Dermatol 1997;36:S96-103.) |
doi_str_mv | 10.1016/S0190-9622(97)70050-1 |
format | Article |
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Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins and hormones.
1
Objective:
We sought molecules with an optimal balance between stability, efficacy, and local tolerance for topical acne therapy.
Methods:
In vitro and in vivo bioassay systems were used to test the ability of retinoids to modulate cell proliferation and differentiation. In addition, antiinflammatory properties were assessed. Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).
Results and Conclusion:
Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation. In addition it has significant antiinflammatory action. The nuclear gene transcription factors RARβ and RARγ mediate the retinoid activity of adapalene. (J Am Acad Dermatol 1997;36:S96-103.)</description><identifier>ISSN: 0190-9622</identifier><identifier>EISSN: 1097-6787</identifier><identifier>DOI: 10.1016/S0190-9622(97)70050-1</identifier><identifier>PMID: 9204085</identifier><language>eng</language><publisher>United States: Mosby, Inc</publisher><subject>Adapalene ; Administration, Topical ; Animals ; Anti-Inflammatory Agents, Non-Steroidal - chemistry ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Cell Differentiation - drug effects ; Cell Division - drug effects ; Cells, Cultured ; Gene Expression - drug effects ; HeLa Cells ; Humans ; Naphthalenes - chemistry ; Naphthalenes - pharmacology ; Signal Transduction - drug effects ; Skin - cytology ; Skin - drug effects</subject><ispartof>Journal of the American Academy of Dermatology, 1997-06, Vol.36 (6), p.S96-S103</ispartof><rights>1997 American Academy of Dermatology, Inc</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c360t-b3c54778ace004bf3939b3654627280bf07991354ede0f18e91fb8d1ed7ab9303</citedby><cites>FETCH-LOGICAL-c360t-b3c54778ace004bf3939b3654627280bf07991354ede0f18e91fb8d1ed7ab9303</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0190-9622(97)70050-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/9204085$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shroot, Braham</creatorcontrib><creatorcontrib>Michel, Serge</creatorcontrib><creatorcontrib>From CIRD Galderma, Sophia Antipolis</creatorcontrib><title>Pharmacology and chemistry of adapalene</title><title>Journal of the American Academy of Dermatology</title><addtitle>J Am Acad Dermatol</addtitle><description>Background:
Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins and hormones.
1
Objective:
We sought molecules with an optimal balance between stability, efficacy, and local tolerance for topical acne therapy.
Methods:
In vitro and in vivo bioassay systems were used to test the ability of retinoids to modulate cell proliferation and differentiation. In addition, antiinflammatory properties were assessed. Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).
Results and Conclusion:
Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation. In addition it has significant antiinflammatory action. The nuclear gene transcription factors RARβ and RARγ mediate the retinoid activity of adapalene. (J Am Acad Dermatol 1997;36:S96-103.)</description><subject>Adapalene</subject><subject>Administration, Topical</subject><subject>Animals</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - chemistry</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</subject><subject>Cell Differentiation - drug effects</subject><subject>Cell Division - drug effects</subject><subject>Cells, Cultured</subject><subject>Gene Expression - drug effects</subject><subject>HeLa Cells</subject><subject>Humans</subject><subject>Naphthalenes - chemistry</subject><subject>Naphthalenes - pharmacology</subject><subject>Signal Transduction - drug effects</subject><subject>Skin - cytology</subject><subject>Skin - drug effects</subject><issn>0190-9622</issn><issn>1097-6787</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1997</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkElPwzAQhS0EKqXwEyrlxHIIjGMntk8IVWxSJZCAs-VlQoOyFDtF6r8nXcSV0xzee_NmPkKmFK4p0OLmDaiCVBVZdqnElQDIIaUHZExBibQQUhyS8Z_lmJzE-AUAijMxIiOVAQeZj8nF68KExriu7j7XiWl94hbYVLEP66QrE-PN0tTY4ik5Kk0d8Ww_J-Tj4f599pTOXx6fZ3fz1LEC-tQyl3MhpHEIwG3JFFOWFTkvMpFJsCUIpSjLOXqEkkpUtLTSU_TCWMWATcj5bu8ydN8rjL0ejnFY16bFbhW1UCAFzzfGfGd0oYsxYKmXoWpMWGsKegNIbwHpzfdaCb0FpOmQm-4LVrZB_5faExn0252Ow5c_FQYdXYWtQ18FdL32XfVPwy_DvXNs</recordid><startdate>19970601</startdate><enddate>19970601</enddate><creator>Shroot, Braham</creator><creator>Michel, Serge</creator><general>Mosby, Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19970601</creationdate><title>Pharmacology and chemistry of adapalene</title><author>Shroot, Braham ; Michel, Serge</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c360t-b3c54778ace004bf3939b3654627280bf07991354ede0f18e91fb8d1ed7ab9303</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1997</creationdate><topic>Adapalene</topic><topic>Administration, Topical</topic><topic>Animals</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - chemistry</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</topic><topic>Cell Differentiation - drug effects</topic><topic>Cell Division - drug effects</topic><topic>Cells, Cultured</topic><topic>Gene Expression - drug effects</topic><topic>HeLa Cells</topic><topic>Humans</topic><topic>Naphthalenes - chemistry</topic><topic>Naphthalenes - pharmacology</topic><topic>Signal Transduction - drug effects</topic><topic>Skin - cytology</topic><topic>Skin - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shroot, Braham</creatorcontrib><creatorcontrib>Michel, Serge</creatorcontrib><creatorcontrib>From CIRD Galderma, Sophia Antipolis</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of the American Academy of Dermatology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shroot, Braham</au><au>Michel, Serge</au><aucorp>From CIRD Galderma, Sophia Antipolis</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacology and chemistry of adapalene</atitle><jtitle>Journal of the American Academy of Dermatology</jtitle><addtitle>J Am Acad Dermatol</addtitle><date>1997-06-01</date><risdate>1997</risdate><volume>36</volume><issue>6</issue><spage>S96</spage><epage>S103</epage><pages>S96-S103</pages><issn>0190-9622</issn><eissn>1097-6787</eissn><abstract>Background:
Retinoid research in the field of dermatology has been influenced by the clinical success of topical tretinoin and oral isotretinoin in the treatment of acne, and by the discovery of high-affinity binding proteins for retinoic acid mediating its action and interaction with other vitamins and hormones.
1
Objective:
We sought molecules with an optimal balance between stability, efficacy, and local tolerance for topical acne therapy.
Methods:
In vitro and in vivo bioassay systems were used to test the ability of retinoids to modulate cell proliferation and differentiation. In addition, antiinflammatory properties were assessed. Binding and transactivation assays were used to compare affinities and transcriptional activities of adapalene and tretinoin for the nuclear transcription factors, retinoic acid receptors (RARs).
Results and Conclusion:
Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation. In addition it has significant antiinflammatory action. The nuclear gene transcription factors RARβ and RARγ mediate the retinoid activity of adapalene. (J Am Acad Dermatol 1997;36:S96-103.)</abstract><cop>United States</cop><pub>Mosby, Inc</pub><pmid>9204085</pmid><doi>10.1016/S0190-9622(97)70050-1</doi></addata></record> |
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language | eng |
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source | MEDLINE; Access via ScienceDirect (Elsevier) |
subjects | Adapalene Administration, Topical Animals Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Cell Differentiation - drug effects Cell Division - drug effects Cells, Cultured Gene Expression - drug effects HeLa Cells Humans Naphthalenes - chemistry Naphthalenes - pharmacology Signal Transduction - drug effects Skin - cytology Skin - drug effects |
title | Pharmacology and chemistry of adapalene |
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