The DOI matches its Crossref record; 13 of the 13 references it cites were found in a registry or an index.
Pharmacology and chemistry of adapalene
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.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 RAR beta and RAR gamma mediate the retinoid activity of adapalene.
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“Adapalene—a third-generation retinoid that modulates cellular keratinization, differentiation, and proliferation [8, 18]—has the advantage of being one of the most tolerable retinoids [19] that also retains its stability in the presence of BPO [9].”
Citations
Cites
The retinoid signaling pathway: molecular and genetic analyses
Chambon, P. (1994) · Seminars in Cell Biology · doi:10.1006/scel.1994.1015 · Cited by 502
Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor γ
Bernard, B. A., Bernardon, J., Delescluse, C., Martin, B., Lenoir, M.-C., Maignan, J., Charpentier, B., Pilgrim, W. R., Reichert, U., & Shroot, B. (1992) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(92)90842-9 · Cited by 201
Self-citationCharpentier, B., Bernardon, J., Eustache, J., Millois, C., Martin, B., Michel, S., & Shroot, B. (1995) · Journal of Medicinal Chemistry · doi:10.1021/jm00026a006 · Cited by 122
Self-citationProstaglandin and Leukotriene Synthesis in Mouse Ears Inflamed by Arachidonic Acid
Opas, E. E., Bonney, R. J., & Humes, J. L. (1985) · Journal of Investigative Dermatology · doi:10.1111/1523-1747.ep12265320 · Cited by 120
Differential Regulation of Retinoic Acid Receptors and Binding Proteins in Human Skin
Elder, J. T., Åström, A., Pettersson, U., Tavakkol, A., Griffiths, C. E. M., Krust, A., Kastner, P., Chambon, P., & Voorhees, J. J. (1992) · Journal of Investigative Dermatology · doi:10.1111/1523-1747.ep12499896 · Cited by 116
Lotan, R., Krämer, R., Neumann, G., Lotan, D., & Nicolson, G. L. (1980) · Experimental Cell Research · doi:10.1016/0014-4827(80)90018-x · Cited by 63
Darmon, M. Y., Rocher, M. N., Cavey, M. T., Martin, B., Rabilloud, T., Delescluse, C., & Shroot, B. (2009) · Skin Pharmacology · doi:10.1159/000210770 · Cited by 57
Self-citationGriffiths, C. E. M., Elder, J. T., Bernard, B. A., Rossio, P., Cromie, M. A., Finkel, L. J., Shroot, B., & Voorhees, J. J. (1993) · Journal of Investigative Dermatology · doi:10.1111/1523-1747.ep12365480 · Cited by 49
Self-citationBouclier, M., Chatelus, A., Ferracin, J., Delain, C., Shroot, B., & Hensby, C. N. (2009) · Skin Pharmacology · doi:10.1159/000210926 · Cited by 45
Self-citationAsselineau, D., Cavey, M. T., Shroot, B., & Darmon, M. Y. (1992) · Journal of Investigative Dermatology · doi:10.1111/1523-1747.ep12555633 · Cited by 36
Self-citationDetermination of retinoid activity by an enzyme-linked immunosorbent assay
Michel, S., Courseaux, A., Miquel, C., Bernardon, J., Schmidt, R., Shroot, B., Thacher, S. M., & Reichert, U. (1991) · Analytical Biochemistry · doi:10.1016/0003-2697(91)90213-d · Cited by 25
Self-citationBouclier, M., Luginbuhl, B., Shroot, B., & Hensby, C. N. (1990) · Inflammation Research · doi:10.1007/bf01964722 · Cited by 17
Self-citationBailly, J., Delescluse, C., Bernardon, J., Charpentier, B., Martin, B., Pilgrim, W. R., Shroot, B., & Darmon, M. Y. (2009) · Skin Pharmacology · doi:10.1159/000210878 · Cited by 13
Self-citation
Research works printed but not linked: 1
- Bouclier, 1984, A rapid and simple test system for the evaluation of the inhibitory activity of topical retinoids on cellotape stripping-induced ODC activity in the hairless rat, Dermatologica, 169, 242
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Wanka, L., Iqbal, K., & Schreiner, P. R. (2013) · Chemical Reviews · doi:10.1021/cr100264t · Cited by 712
Pharmaceuticals that contain polycyclic hydrocarbon scaffolds
Stockdale, T. P., & Williams, C. M. (2015) · Chemical Society Reviews · doi:10.1039/c4cs00477a · Cited by 254
Thiboutot, D. M., Weiss, J., Bucko, A., Eichenfield, L., Jones, T., Clark, S., Liu, Y., Graeber, M., & Kang, S. (2007) · Journal of the American Academy of Dermatology · doi:10.1016/j.jaad.2007.06.006 · Cited by 183
Understanding innate immunity and inflammation in acne: implications for management
Dréno, B., Gollnick, H. P. M., Kang, S., Thiboutot, D. M., Bettoli, V., Torres, V., Leyden, J., & the Global Alliance to Improve Outcomes in Acne (2015) · Journal of the European Academy of Dermatology and Venereology · doi:10.1111/jdv.13190 · Cited by 191
Adapalene loaded solid lipid nanoparticles gel: An effective approach for acne treatment
Jain, A., Jain, A., Garg, N. K., Agarwal, A., Jain, A., Jain, S. A., Tyagi, R. K., Jain, R. K., Agrawal, H., & Agrawal, G. P. (2014) · Colloids and Surfaces B Biointerfaces · doi:10.1016/j.colsurfb.2014.05.041 · Cited by 176
Metadata
- Authors
- Shroot, B., & Michel, S.
- Affiliations
- Galderma (France) (FR)
- ORCID
- Shroot, Braham
- Venue
- Journal of the American Academy of Dermatology
- Publisher
- Elsevier BV
- Published
- 1997-06
- Volume
- 36
- Issue
- 6
- Pages
- S96-S103
- ISSN
- 0190-9622 (ISSN-L)
- OpenAlex
- W2144493708
- Cited by
- 140
- References
- 13
- Citations by year
- 2026: 5 · 2025: 5 · 2024: 8 · 2023: 2 · 2022: 2 · 2021: 7 · 2020: 6 · 2019: 5 · 2018: 2 · 2017: 1 · 2016: 8 · 2015: 4 · 2014: 13 · 2013: 6
- FWCI
- 8.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of the American Academy of Dermatology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Dermatology › Acne and Rosacea Treatments and Effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Retinoids in leukemia and cellular processes
- Health Sciences › Medicine › Dermatology › Dermatology and Skin Diseases
- Keywords
- adapalene, retinoids, acne treatment, topical retinoids, retinoic acid receptor, RARβ, RARγ, naphthoic acid derivatives, cell proliferation, cell differentiation, anti-inflammatory activity, all-trans retinoic acid, drug stability
- MeSH terms
- Adapalene, Administration, Topical, Animals, Anti-Inflammatory Agents, Non-Steroidal, Cell Differentiation, Cell Division, Cells, Cultured, HeLa Cells, Humans, Naphthalenes, Skin, Signal Transduction, Gene Expression
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