targetsTarget

Retinoid X receptor (RXR)

The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.

RXR alpha, beta and gamma are nuclear receptors that form heterodimers with retinoic acid receptors, the vitamin D receptor, thyroid hormone receptor, PPARs and LXR, so a single RXR ligand can alter many transcriptional programmes. Bexarotene, a selective RXR agonist (rexinoid), is approved for cutaneous T-cell lymphoma; its metabolic side effects (central hypothyroidism, hypertriglyceridaemia) follow directly from RXR partner activation. The related retinoic acid receptor is the target of all-trans retinoic acid in acute promyelocytic leukaemia.

Retinoid X receptor (RXR): what it is and how drugs act on it · animated generic schematic, not to scale

Target · the protein and the cell it sits on
Drug · antibody, small molecule, cell or radioligand
Effect · signal, damage or kill

In plain words · The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.

1 · What it is
The retinoid X receptor is a switch inside cells that vitamin A-like molecules turn on to change which genes are active; bexarotene uses it to make lymphoma cells in the skin mature and die.
2 · What goes wrong in cancer
Ligand binding recruits co-activators and drives differentiation and apoptosis genes in malignant T cells; RXR also modulates PPAR-gamma-dependent lipid metabolism.
3 · How drugs use it
1 product aims at Retinoid X receptor (RXR): small molecules. Drugs cut off the hormone supply, block the receptor so the hormone cannot bind, or send the receptor to the cell's waste disposal.

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Biology

Ligand binding recruits co-activators and drives differentiation and apoptosis genes in malignant T cells; RXR also modulates PPAR-gamma-dependent lipid metabolism.

Where it is found

Cutaneous T-cell lymphoma (bexarotene)

Class

nuclear receptor · RXRA, RXRB, RXRG

Products

1top

ApprovedSmall-molecule retinoid X receptor agonist

Bexarotene · Targretin

Bexarotene (Targretin) is a vitamin A-like capsule and gel for the skin disease of cutaneous T-cell lymphoma when other treatments have stopped working.