PMID- 24456080 OWN - NLM STAT- MEDLINE DCOM- 20141218 LR - 20140319 IS - 1744-7674 (Electronic) IS - 1354-3776 (Linking) VI - 24 IP - 4 DP - 2014 Apr TI - Retinoid X receptor ligands: a patent review (2007 - 2013). PG - 443-52 LID - 10.1517/13543776.2014.880692 [doi] AB - INTRODUCTION: Retinoid X receptors (RXRs) are nuclear receptors that act as ligand-dependent transcription factors. RXRs function as homodimers or as heterodimers with other nuclear receptors, such as retinoic acid receptors, PPARs, liver X receptors, farnesoid X receptor, vitamin D receptor or thyroid hormone receptors. RXR ligands (agonists or antagonists) show various physiological effects, depending on their partner receptors. RXR agonist bexarotene (Targretin(R)) is used for the treatment of cutaneous T-cell lymphoma in clinical practice. RXR agonists were also reported to be useful for treatment of type 2 diabetes, autoimmune disease and Alzheimer's disease. RXR antagonists were also reported to be effective in type 2 diabetes treatment. AREAS COVERED: Here patent applications (2007 - 2013) concerning RXR ligands are summarized, and the usefulness of RXR ligands as pharmaceutical agents is discussed. EXPERT OPINION: RXR agonists show a wide variety of biological effects. However, they cause serious side effects, such as blood triglyceride elevation, hypothyroidism and others. Thus, for clinical application of RXR agonists, abrogation of these side effects is required. RXR heterodimer-selective agonists and RXR partial agonists exhibiting desired effects without side effects are expected to find clinical application. FAU - Yamada, Shoya AU - Yamada S AD - Okayama University Graduate School of Medicine, Division of Pharmaceutical Sciences, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-Naka, Kita-Ku, Okayama 700-8530 , Japan +81 086 251 7963 ; +81 086 251 7963 ; kakuta-h@cc.okayama-u.ac.jp. FAU - Kakuta, Hiroki AU - Kakuta H LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review DEP - 20140124 PL - England TA - Expert Opin Ther Pat JT - Expert opinion on therapeutic patents JID - 9516419 RN - 0 (Antineoplastic Agents) RN - 0 (Hypoglycemic Agents) RN - 0 (Hypolipidemic Agents) RN - 0 (Ligands) RN - 0 (Retinoid X Receptors) SB - IM MH - Alzheimer Disease/drug therapy MH - Animals MH - Antineoplastic Agents/therapeutic use MH - Diabetes Mellitus, Type 2/drug therapy MH - Drug Discovery MH - Humans MH - Hypoglycemic Agents/therapeutic use MH - Hypolipidemic Agents/therapeutic use MH - Ligands MH - Medicine, Chinese Traditional MH - *Patents as Topic MH - Protein Multimerization MH - Retinoid X Receptors/*agonists/chemistry EDAT- 2014/01/25 06:00 MHDA- 2014/12/19 06:00 CRDT- 2014/01/25 06:00 PHST- 2014/01/25 06:00 [entrez] PHST- 2014/01/25 06:00 [pubmed] PHST- 2014/12/19 06:00 [medline] AID - 10.1517/13543776.2014.880692 [doi] PST - ppublish SO - Expert Opin Ther Pat. 2014 Apr;24(4):443-52. doi: 10.1517/13543776.2014.880692. Epub 2014 Jan 24.