IUPHAR/BPS Guide to Pharmacology CITE
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Calcium- and sodium-activated potassium channels (KCa, KNa) in GtoPdb v.2025.3
Full text linkCalcium- and sodium- activated potassium channels are members of the 6TM family of K channels which comprises the voltage-gated KV subfamilies, including the KCNQ subfamily, the EAG subfamily (which includes hERG channels), the Ca2+-activated Slo subfamily (actually with 6 or 7TM) and the Ca2+- and Na+-activated SK subfamily (nomenclature as agreed by the NC-IUPHAR Subcommittee on Calcium- and sodium-activated potassium channels [144]). As for the 2TM family, the pore-forming a subunits form tetramers and heteromeric channels may be formed within subfamilies (e.g. KV1.1 with KV1.2; KCNQ2 with KCNQ3)
Inwardly rectifying potassium channels (KIR) in GtoPdb v.2025.3
Full text linkThe 2TM domain family of K channels are also known as the inward-rectifier K channel family. This family includes the strong inward-rectifier K channels (Kir2.x) that are constitutively active, the G-protein-activated inward-rectifier K channels (Kir3.x) and the ATP-sensitive K channels (Kir6.x, which combine with sulphonylurea receptors (SUR1-3)). The pore-forming α subunits form tetramers, and heteromeric channels may be formed within subfamilies (e.g. Kir3.2 with Kir3.3)
SLC15 family of peptide transporters in GtoPdb v.2025.3
Full text linkThe Solute Carrier 15 (SLC15) family of peptide transporters, alias H+-coupled oligopeptide cotransporter family, is a group of membrane transporters known for their key role in the cellular uptake of di- and tripeptides (di/tripeptides). Of its members, SLC15A1 (PEPT1) chiefly mediates intestinal absorption of luminal di/tripeptides from overall dietary protein digestion, SLC15A2 (PEPT2) mainly allows renal tubular reuptake of di/tripeptides from ultrafiltration and brain-to-blood efflux of di/tripeptides in the choroid plexus, SLC15A3 (PHT2) and SLC15A4 (PHT1) interact with both di/tripeptides and histidine, e.g. in certain immune cells, and SLC15A5 has unknown physiological function. In addition, the SLC15 family of peptide transporters variably interacts with a very large number of peptidomimetics and peptide-like drugs. It is conceivable, based on the currently acknowledged structural and functional differences, to divide the SLC15 family of peptide transporters into two subfamilies [3]
SLC39 family of metal ion transporters in GtoPdb v.2025.3
Full text linkAlong with the SLC30 family, SLC39 family members regulate zinc movement in cells. SLC39 metal ion transporters accumulate zinc into the cytosol. Membrane topology modelling suggests the presence of eight TM regions with both termini extracellular or in the lumen of intracellular organelles. The mechanism for zinc transport for many members is unknown but appears to involve co-transport of bicarbonate ions [3, 5]
Adenosine turnover in GtoPdb v.2025.3
Full text linkA multifunctional, ubiquitous molecule, adenosine acts at cell-surface G protein-coupled receptors, as well as numerous enzymes, including protein kinases and adenylyl cyclase. Extracellular adenosine is thought to be produced either by export or by metabolism, predominantly through ecto-5’-nucleotidase activity (also producing inorganic phosphate). It is inactivated either by extracellular metabolism via adenosine deaminase (also producing ammonia) or, following uptake by nucleoside transporters, via adenosine deaminase or adenosine kinase (requiring ATP as co-substrate). Intracellular adenosine may be produced by cytosolic 5’-nucleotidases or through S-adenosylhomocysteine hydrolase (also producing L-homocysteine)
GDNF Family Receptor (GFR) in GtoPdb v.2025.3
Full text linkGDNF family receptors (GFR) are extrinsic co-receptors, where ligand binding to the extracellular domain of the glycosylphosphatidylinositol-linked cell-surface GFRs activates a transmembrane tyrosine kinase enzyme, RET. The endogenous ligands are typically dimeric, linked through disulphide bridges: glial cell-derived neurotrophic factor GDNF (211 aa); neurturin (197 aa); artemin (237 aa) and persephin (156 aa), referred to as GDNF family ligands (GFLs). There is evidence for RET-dependent and RET-independent signalling [5]. Growth/Differentiation Factor 15 (GDF15) has been shown to activate GFRAL, a transmembrane protein that similarly forms a complex with RET [8, 10]
Type XII RTKs: TIE family of angiopoietin receptors in GtoPdb v.2025.3
Full text linkThe TIE family were initially associated with formation of blood vessels (angiogenesis). Endogenous ligands are angiopoietin-1, angiopoietin-2, and angiopoietin-4. angiopoietin-2 appears to act as an endogenous antagonist of angiopoietin-1 function, thus blocking TIE2-mediated signalling. Due to roles in blood vessel formation, monoclonal antibodies are being developed against the ligand Ang2 (cyamemazine57) or a bispecific antibody against VEGF and Ang2 (faricimab) for the treatment of ocular diseases
Succinate receptor in GtoPdb v.2025.3
Full text linkNomenclature as recommended by NC-IUPHAR [8]. The succinate receptor (GPR91, SUCNR1) is activated by the tricarboxylic acid (or Krebs) cycle intermediate succinate and other dicarboxylic acids with less clear physiological relevance such as maleate [17]. Since its pairing with its endogenous ligand in 2004, intense research has focused on the receptor-ligand pair role in various (patho)physiological processes such as regulation of renin production [17, 40], ischemia injury [17], fibrosis [26], retinal angiogenesis [35], inflammation [26, 24], immune response [33], obesity [45, 27, 21], diabetes [43, 22, 40], platelet aggregation [39, 37] or cancer [29, 47]. The succinate receptor is coupled to Gi/o [11, 17] and Gq/11 protein families [32, 17, 41], whilst coupling to these G proteins is dependent on the cellular, metabolic and spatial context [23, 41]. Although the receptor is, upon ligand addition, rapidly desensitized [19, 32], and in some cells internalized [17], it seems to recruit arrestins weakly [10]. The cellular activation of the succinate receptor triggers various signalling pathways such as decrease of cAMP levels, [Ca2+]i mobilization and activation of kinases (ERK, c-Jun, Akt, Src, p38, PI3Kβ, etc.) [12]. The receptor is broadly expressed but is notably abundant in immune cells (M2 macrophages [41, 21], monocytes [33], immature dendritic cells [33], adipocytes [45], platelets [39, 37], etc.) and in the kidney [17]
Type XVIII RTKs: LMR family in GtoPdb v.2025.3
Full text linkThe lemur tail kinase (LMR) family are are unusual amongst the RTKs in possessing a short extracellular domain and extended intracellular domain (hence the \u27Lemur\u27 name reflecting the long tail). LMR1 was identified as a potential marker of apoptosis [2], giving rise to the name AATYK (Apoptosis-Associated Tyrosine Kinase); while over-expression induces differentiation in neuroblastoma cells [3]. The LMTK/LMR family have since been identified to have serine/threonine kinase activity, as opposed to tyrosine kinase [4]
S33: Prolyl aminopeptidase in GtoPdb v.2025.3
Full text linkPeptidase family S33 contains mainly exopeptidases that act at the N-terminus of peptides