IUPHAR/BPS Guide to Pharmacology CITE
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Opioid receptors in GtoPdb v.2025.3
Get PDFOpioid and opioid-like receptors are activated by a variety of endogenous peptides including [Met]enkephalin (met), [Leu]enkephalin (leu), β-endorphin (β-end), α-neodynorphin, dynorphin A (dynA), dynorphin B (dynB), big dynorphin (Big dyn), nociceptin/orphanin FQ (N/OFQ); endomorphin-1 and endomorphin-2 are also potential endogenous peptides. The Greek letter nomenclature for the opioid receptors, μ, δ and κ, is well established, and NC-IUPHAR considers this nomenclature appropriate, along with the symbols spelled out (mu, delta, and kappa), and the acronyms, MOP, DOP, and KOP [127, 103, 94]. However the acronyms MOR, DOR and KOR are still widely used in the literature. The human N/OFQ receptor, NOP, is considered \u27opioid-related\u27 rather than opioid because, while it exhibits a high degree of structural homology with the conventional opioid receptors [313, 94], it displays a distinct pharmacology. Currently there are numerous clinically used drugs, such as morphine and many other opioid analgesics, as well as antagonists such as naloxone. The majority of clinically used opiates are relatively selective μ agonists or partial agonists, though there are some μ/κ compounds, such as butorphanol, in clinical use. κ opioid agonists, such as the alkaloid nalfurafine and the peripherally acting peptide difelikefalin, are in clinical use for itch
Vasopressin and oxytocin receptors in GtoPdb v.2025.3
Get PDFVasopressin (AVP) and oxytocin (OT) receptors (nomenclature as recommended by NC-IUPHAR [98]) are activated by the endogenous cyclic nonapeptides vasopressin and oxytocin. These peptides are derived from precursors which also produce neurophysins (neurophysin I for oxytocin; neurophysin II for vasopressin). Vasopressin and oxytocin differ at only 2 amino acids (positions 3 and 8). There are metabolites of these neuropeptides that may be biologically active [71]
Voltage-gated potassium channels (Kv) in GtoPdb v.2025.3
Get PDFThe 6TM family of K channels comprises the voltage-gated KV subfamilies, the EAG subfamily (which includes hERG channels), the Ca2+-activated Slo subfamily (actually with 7TM, termed BK) and the Ca2+-activated SK subfamily. These channels possess a pore-forming α subunit that comprise tetramers of identical subunits (homomeric) or of different subunits (heteromeric). Heteromeric channels can only be formed within subfamilies (e.g. Kv1.1 with Kv1.2; Kv7.2 with Kv7.3). The pharmacology largely reflects the subunit composition of the functional channel.Kv7 channelsKv7.1-Kv7.5 (KCNQ1-5) K+ channels are voltage-gated K+ channels with major roles in neurons, muscle cells and epithelia where they underlie physiologically important K+ currents, such as the neuronal M-current and the cardiac IKs. Genetic deficiencies in all five KCNQ genes result in human excitability disorders, including epilepsy, autism spectrum disorders, cardiac arrhythmias and deafness. Thanks to the recent knowledge of the structure and function of human KCNQ-encoded proteins, these channels are increasingly used as drug targets for treating diseases [333, 2, 777, 294]
1H. Liver X receptor-like receptors in GtoPdb v.2025.3
Get PDFLiver X and farnesoid X receptors (LXR and FXR, nomenclature as agreed by the NC-IUPHAR Subcommittee on Nuclear Hormone Receptors [78, 3]) are members of a steroid analogue-activated nuclear receptor subfamily, which form heterodimers with members of the retinoid X receptor family. Endogenous ligands for LXRs include hydroxycholesterols (OHC), while FXRs appear to be activated by bile acids. In humans and primates, NR1H5P is a pseudogene. However, in other mammals, it encodes a functional nuclear hormone receptor that appears to be involved in cholesterol biosynthesis [83]
3A. Estrogen receptors in GtoPdb v.2025.3
Get PDFEstrogen receptor (ER) activity regulates diverse physiological processes via transcriptional modulation of target genes [2]. The selection of target genes and the magnitude of the response, be it induction or repression, are determined by many factors, including the effect of the hormone ligand and DNA binding on ER structural conformation, and the local cellular regulatory environment. The cellular environment defines the specific complement of DNA enhancer and promoter elements present and the availability of coregulators to form functional transcription complexes. Together, these determinants control the resulting biological response
Eicosanoid turnover in GtoPdb v.2025.3
Get PDFEicosanoids are 20-carbon fatty acids, where the usual focus is the polyunsaturated analogue arachidonic acid and its metabolites. Arachidonic acid is thought primarily to derive from phospholipase A2 action on membrane phosphatidylcholine, and may be re-cycled to form phospholipid through conjugation with coenzyme A and subsequently glycerol derivatives. Oxidative metabolism of arachidonic acid is conducted through three major enzymatic routes: cyclooxygenases; lipoxygenases and cytochrome P450-like epoxygenases, particularly CYP2J2. Isoprostanes are structural analogues of the prostanoids (hence the nomenclature D-, E-, F-isoprostanes and isothromboxanes), which are produced in the presence of elevated free radicals in a non-enzymatic manner, leading to suggestions for their use as biomarkers of oxidative stress. Molecular targets for their action have yet to be defined
Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family in GtoPdb v.2025.3
Get PDFType III RTKs include PDGFR, CSF-1R (Ems), Kit and FLT3, which function as homo- or heterodimers. Endogenous ligands of PDGF receptors are homo- or heterodimeric: PDGFA, PDGFB, VEGFE and PDGFD combine as homo- or heterodimers to activate homo- or heterodimeric PDGF receptors. SCF is a dimeric ligand for KIT. Ligands for CSF1R are either monomeric or dimeric glycoproteins, while the endogenous agonist for FLT3 is a homodimer
Type VII RTKs: Neurotrophin receptor/Trk family in GtoPdb v.2025.3
Get PDFThe neurotrophin receptor family of RTKs include tropomyosin-related kinase (Trk) receptors TrkA, TrkB and TrkC. Their cognate ligands are NGF, BDNF and neurotrophin-3, respectively. They are associated primarily with proliferative and migration effects in neural systems. Various isoforms of neurotrophin receptors exist, including truncated forms of TrkB and TrkC, which lack catalytic domains. p75 (TNFRSF16, also known as nerve growth factor receptor) can interact with neurotrophins and their propeptides. While p75 can lead to apoptosis, it can also form a complex with Trk receptors to mediate survival signalling [10]
Peptidyl-prolyl cis/trans isomerases in GtoPdb v.2025.3
Get PDFPeptidyl-prolyl cis/trans isomerases (PPIases) are an enzyme family which catalyse the cis/trans isomerisation of proline peptide bonds to promote the folding and re-folding of peptides and proteins. Three subfamilies have been identified: cyclophilins, FK506-binding proteins and parvulins. Individual PPIases are overexpressed in a number of cancers [65], and family members have been targetted for immunosuppressant effects
Receptor tyrosine phosphatase (RTP) family in GtoPdb v.2025.3
Get PDFReceptor tyrosine phosphatases (RTP)- also referred to as receptor-type tyrosine-protein phosphatases (PTPR) - are cell-surface proteins with a single TM region and intracellular phosphatase activity at phosphorylated tyrosine residues. There are 20 family members of classic RPTPs. Many family members exhibit constitutive activity upon heterologous expression, dephosphorylating intracellular targets such as Src tyrosine kinase (SRC) to activate signalling cascades. Family members bind components of the extracellular matrix or cell-surface proteins indicating a role in intercellular communication