Rev-erb receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [1-2]) have yet to be officially paired with an endogenous ligand, but are thought to be activated by heme.

* Key recommended reading is highlighted with an asterisk

* Benoit G, Cooney A, Giguere V, Ingraham H, Lazar M, Muscat G, Perlmann T, Renaud JP, Schwabe J, Sladek F, Tsai MJ, Laudet V. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol Rev, 58 (4): 798-836. [PMID:17132856]

Duez H, Staels B. (2009) Rev-erb-alpha: an integrator of circadian rhythms and metabolism. J Appl Physiol, 107 (6): 1972-80. [PMID:19696364]

Germain P, Staels B, Dacquet C, Spedding M, Laudet V. (2006) Overview of nomenclature of nuclear receptors. Pharmacol Rev, 58 (4): 685-704. [PMID:17132848]

* Gonzalez-Sanchez E, Firrincieli D, Housset C, Chignard N. (2015) Nuclear receptors in acute and chronic cholestasis. Dig Dis, 33 (3): 357-66. [PMID:26045270]

* Gustafson CL, Partch CL. (2015) Emerging models for the molecular basis of mammalian circadian timing. Biochemistry, 54 (2): 134-49. [PMID:25303119]

Huang P, Chandra V, Rastinejad F. (2010) Structural overview of the nuclear receptor superfamily: insights into physiology and therapeutics. Annu Rev Physiol, 72: 247-72. [PMID:20148675]

Kojetin DJ, Burris TP. (2014) REV-ERB and ROR nuclear receptors as drug targets. Nat Rev Drug Discov, 13 (3): 197-216. [PMID:24577401]

Marciano DP, Chang MR, Corzo CA, Goswami D, Lam VQ, Pascal BD, Griffin PR. (2014) The therapeutic potential of nuclear receptor modulators for treatment of metabolic disorders: PPARγ, RORs, and Rev-erbs. Cell Metab, 19 (2): 193-208. [PMID:24440037]

Phelan CA, Gampe RT, Lambert MH, Parks DJ, Montana V, Bynum J, Broderick TM, Hu X, Williams SP, Nolte RT, Lazar MA. (2010) Structure of Rev-erbalpha bound to N-CoR reveals a unique mechanism of nuclear receptor-co-repressor interaction. Nat Struct Mol Biol, 17 (7): 808-14. [PMID:20581824]

Sladek FM. (2011) What are nuclear receptor ligands?. Mol Cell Endocrinol, 334 (1-2): 3-13. [PMID:20615454]

* Sousa EH, Lopes LG, Gonzalez G, Gilles-Gonzalez MA. (2017) Drug discovery targeting heme-based sensors and their coupled activities. J Inorg Biochem, 167: 12-20. [PMID:27893989]

Yin L, Wu N, Lazar MA. (2010) Nuclear receptor Rev-erbalpha: a heme receptor that coordinates circadian rhythm and metabolism. Nucl Recept Signal, 8: e001. [PMID:20414452]

1. Alexander SPH, Cidlowski JA, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ et al.. (2019) THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Nuclear hormone receptors. Br J Pharmacol, 176 Suppl 1: S229-S246. [PMID:31710718]

2. Benoit G, Cooney A, Giguere V, Ingraham H, Lazar M, Muscat G, Perlmann T, Renaud JP, Schwabe J, Sladek F, Tsai MJ, Laudet V. (2006) International Union of Pharmacology. LXVI. Orphan nuclear receptors. Pharmacol Rev, 58 (4): 798-836. [PMID:17132856]

3. Grant D, Yin L, Collins JL, Parks DJ, Orband-Miller LA, Wisely GB, Joshi S, Lazar MA, Willson TM, Zuercher WJ. (2010) GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol, 5 (10): 925-32. [PMID:20677822]

4. Kojetin D, Wang Y, Kamenecka TM, Burris TP. (2011) Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chem Biol, 6 (2): 131-4. [PMID:21043485]

5. Matta-Camacho E, Banerjee S, Hughes TS, Solt LA, Wang Y, Burris TP, Kojetin DJ. (2014) Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist. J Biol Chem, 289 (29): 20054-66. [PMID:24872411]

6. Raghuram S, Stayrook KR, Huang P, Rogers PM, Nosie AK, McClure DB, Burris LL, Khorasanizadeh S, Burris TP, Rastinejad F. (2007) Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta. Nat Struct Mol Biol, 14 (12): 1207-13. [PMID:18037887]

7. Yin L, Wu N, Curtin JC, Qatanani M, Szwergold NR, Reid RA, Waitt GM, Parks DJ, Pearce KH, Wisely GB et al.. (2007) Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways. Science, 318 (5857): 1786-9. [PMID:18006707]