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Orphan nuclear receptor ligands act on nuclear receptors cloned before a natural ligand was known. The term dates from 1988, when estrogen-related receptors were identified by sequence similarity to the estrogen receptor. Many further superfamily members were found this way, as a 1995 review of the second decade of nuclear receptor research describes. Liver receptor homolog 1 (LRH-1, NR5A2) regulates development, metabolism and steroidogenesis. ML-180 is an LRH-1 inverse agonist, LRH-1 agonist-2 activates the receptor, and RJW100 activates LRH-1 together with steroidogenic factor 1 (SF-1). MI-883 activates and CINPA1 inhibits the constitutive androstane receptor (CAR). The set is mixed and also lists compounds for unrelated targets, such as splicing factor 3B subunit 1 (SF3B1).
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
