Determination of retinoid activity by an enzyme-linked immunosorbent assay

Michel, Serge; Courseaux, Anouk; Miquel, Corinne; Bernardon, Jean-Michel; Schmidt, Rainer; Shroot, Braham; Thacher, Scott M.; Reichert, Uwe

doi:10.1016/0003-2697(91)90213-d

Cited by 24 publications

(9 citation statements)

References 14 publications

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“…The effect of an increasing concentration of tretinoin or adapalene on the expression of transglutaminase K can be quantified by using an enzyme-linked immu nosorbent assay [13]. As shown in Figure 3b, the concentration leading to half-maximum inhibition (IC50 value) transglutaminase K ex- pression is 10-fold lower for adapalene (IC50 = 2.5 nM ) than for tretinoin (IC50 = 24 nM).…”

Section: Adapalene Represses Kératinocyte Transglutaminase In Vitromentioning

confidence: 99%

Adapalene, a New Chemical Entity with Retinoid Activity

Bernard¹

1993

Skin Pharmacol Physiol

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Adapalene is a novel chemical entity which, in terms of pharmacology, behaves similar to tretinoin, but is chemically and photochemically stable. It has a particular selectivity profile for the known nuclear retinoic acid receptors with low affinity for RARΑ and no transactivating potential for RXRΑ. This receptor profile could imply that adapalene, in contrast to tretinoin, affects the terminal differentiation pathway of epidermal cells rather than their proliferation. Furthermore, adapalene does not bind to members of the cellular retinoic acid binding protein family. Adapalene has comedolytic activity in the topical rhino mouse model. It exerts a moderate-to-potent anti-inflammatory effect in a series of in vitro and in vivo models. In comparative clinical studies involving 72 acne patients, the efficacy of adapalene was comparable, if not superior, to tretinoin, but adapalene was better tolerated. The data reviewed in this paper indicate that adapalene should be particularly beneficial in the treatment of acne.

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Section: Adapalene Represses Kératinocyte Transglutaminase In Vitromentioning

confidence: 99%

Adapalene, a New Chemical Entity with Retinoid Activity

Bernard¹

1993

Skin Pharmacol Physiol

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“…That the RARγ subtype is predominantly expressed in the epidermis has been elegantly demonstrated by Elder et al [6]. The role of the dermis must not be overlooked in skin disease and since skin fibroblasts express RARβ, gene activation mediated through this receptor subtype should be an added advantage in this molecule.…”

Section: Resultsmentioning

confidence: 98%

“…The in vitro assays were used as described: F9 cell differentiation [5]; expression of transglutaminase by normal human keratinocytes [6]; HeLa cell proliferation [7]; retinoic acid receptor (RAR) binding assay [8]; the rhino mouse model [9] and the rabbit skin irritancy test [10]. …”

Section: Methodsmentioning

confidence: 99%

A New Concept of Drug Delivery for Acne

et al. 1998

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Adapalene is a stable naphthoic acid derivative that displays a strong retinoid agonist pharmacology. This drug controls cell proliferation and differentiation, and possesses significant anti-inflammatory action. The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RARβ and RARγ. We describe here how an aqueous gel containing adapalene was selected for the topical treatment of acne.

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“…After two additional freeze-thaw cycles, a normal ELISA-assay (Michel et al 1991) with primary antibody (B.Cl) (Thacher et al 1985) against TG-I, a differentiation marker was performed. Nonspecific adsorption of antibodies on the plates were blocked with 200 pl in PBS (NaC1 8 gA, KC1 0.2 g/l, NaZHPO4.…”

Section: Cell Culturesmentioning

confidence: 99%

“…Microplate assays for cell viability (Mosmann et al 1983) and human transglutaminase type I (TG-I) (Michel et al 1991) were combined in order to measure consecutively keratinocyte proliferation and keratinocyte differentiation in the same monolayer (Geysen et al 1996). The combination of methods resulted in improved sensitivity and reproducibility.…”

Section: Cell Culturesmentioning

confidence: 99%

Proliferation and Differentiation of Cultured Human Keratinocytes is Modulated by 1,25(OH)₂D₃ and Synthetic Vitamin D₃ Analogues in a Cell Density‐, Calcium‐ and Serum‐Dependent Manner*

Svendsen

Daneels

Geysen

et al. 1997

Pharmacology & Toxicology

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Abstract:The natural form of vitamin D3, 1,25-dihydroxyvitamin D3 ( 1,25(OH)2D3) decreases proliferation and promotes terminal differentiation of cultured human epidermal keratinocytes. The purpose of this study was to find out to what extent the culture conditions determine the sensitivety of keratinocytes to 1,25(OH)2D3 and synthetic vitamin D analogues.Human keratinocytes were grown in microplates. Cell proliferation (MTTassay) and differentiation (quantity of transglutaminase type I) were measured consecutively in the same monolayer. When vitamin D3 analogues were added to 50-60% confluent keratinocytes grown in serum-free keratinocyte growth medium with 0.09 mM CaZ+, stimulation of the proliferation was either minimal or non-existent, while differentiation was unaffected or slightly inhibited. There was no difference in the sensitivity to 1,25(OH)2D3 and the vitamin D3 analogues. When 1,25(OH)2D3 was added to less confluent keratinocytes (30%) a marked antiproliferative effect was observed. Addition of 3% charcoal stripped foetal calf serum further enhanced the antiproliferative effect of 1,25(OH)2D3, and a difference in the sensitivity of the vitamin D3 analogues was noted. If, finally, the Ca2+ concentration was raised to 0.3 mM, 1,25(OH)2D3 and the vitamin D3 analogues stimulated differentiation. Also, a biphasic effect on proliferation occurred: stimulation at low vitamin D concentrations and inhibition at higher concentrations. Furthermore, keratinocytes became more sensitive to the synthetic vitamin D3 analogues than to 1.25(OH)2D3: KH1060>EB1089>GS1500~EBl2l3>calcipotriol> 1,25(0H)2D3. For all compounds tested differentiation occurred at concentrations 10 to 30 times lower than for proliferation. These results indicate that the sensitivity to vitamin D3 analogues as well as the direction of the response to vitamin D3 analogues is dependent on the keratinocyte density, the availability of serum and Ca2+ concentrations.The active form of vitamin D3, 1,25-dihydroxy vitamin D3 (1,25(OH)2D3), decreases the proliferation and increases the terminal differentiation of cultured mouse (Hosomi et al. 1983) and human (Bikle et al. 1993;Smith et al. 1986) epidermal keratinocytes. The action of vitamin D3 is probably mediated through the classical intracellular vitamin D receptor present in the epidermis (Berger et al. 1988). The effect of 1,25(OH)$3 on keratinocyte proliferation may be mediated by an altered expression of transforming growth factor p (Kim et al. 1992) and c-myc (Matsumoto et al. 1990), while differentiation may be induced via increased transglutaminase and involucrin transcription (Su et al. 1994). In addition, vitamin D3 has nongenomic actions involving altered phosphoinositide metabolism (Sorensen et al. 1993, protein kinase C activation (Hannafin et al. 1995, and a rise in intracellular Ca2+ (Jones et al. 1994). The ef- fect of 1,25(OH)2D3 on intracellular Ca2+ may be important for the differentiation-promoting effect of 1,25(OH)2D3. The effect of vitamin D3 on epidermal proliferation and dif...

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Determination of retinoid activity by an enzyme-linked immunosorbent assay

Cited by 24 publications

References 14 publications

Adapalene, a New Chemical Entity with Retinoid Activity

Adapalene, a New Chemical Entity with Retinoid Activity

A New Concept of Drug Delivery for Acne

Proliferation and Differentiation of Cultured Human Keratinocytes is Modulated by 1,25(OH)₂D₃ and Synthetic Vitamin D₃ Analogues in a Cell Density‐, Calcium‐ and Serum‐Dependent Manner*

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Determination of retinoid activity by an enzyme-linked immunosorbent assay

Cited by 24 publications

References 14 publications

Adapalene, a New Chemical Entity with Retinoid Activity

Adapalene, a New Chemical Entity with Retinoid Activity

A New Concept of Drug Delivery for Acne

Proliferation and Differentiation of Cultured Human Keratinocytes is Modulated by 1,25(OH)2D3 and Synthetic Vitamin D3 Analogues in a Cell Density‐, Calcium‐ and Serum‐Dependent Manner*

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Product

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Proliferation and Differentiation of Cultured Human Keratinocytes is Modulated by 1,25(OH)₂D₃ and Synthetic Vitamin D₃ Analogues in a Cell Density‐, Calcium‐ and Serum‐Dependent Manner*