Retinoid Receptor

Acitretin is a second generation retinoid and is typically used for psoriasis.

Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions.

Tazarotene is a prodrug and a member of the acetylenic class of retinoids.

Tretinoin is an endogenous agonist for retinoic acid receptors with IC50 value of 14 nM for RAR-alpha, RAR-beta and RAR-gamma receptors).

Bexarotene is a highly selective retinoid X receptor (RXR) agonist.

Adarotene belongs to the so-called class of atypical retinoids. The presence of the phenolic hydroxyl group on Adarotene structure allows a rapid O-glucuronidation as a major mechanism of elimination of the drug, favoring a fast excretion of its glucuronide metabolite in the urines.

Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro.

AM 580 is an analog of retinoic acid that acts as a selective RARα agonist.

CD 437 is a synthetic retinoid that is an RARγ-selective agonist.

Fenretinide is a synthetic retinoid agonist. It is an antiproliferative, antioxidant and anticancer agent with a long half-life in vivo.

AR7 was developed as a highly potent and selective enhancer of the chaperone-mediated autophagy (CMA) through antagonizing RARα.

TTNPB enhances reprogramming efficiency in chemically induced pluripotent stem cells (CiPSCs).

LG 100268 is a potent RXR agonist for evaluation in the treatment of non-insulin-dependent (type II) diabetes mellitus (NIDDM).

Etretinate is a second-generation retinoid to treat severe psoriasis; has been replaced by acitretin, a safer metabolite of etretinate.

LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.

UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.