IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F70/2019.4

CatSper and Two-Pore channels (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database



Jean-Ju Chung1, David E. Clapham1, David L. Garbers2 and Dejian Ren3
  1. Harvard Medical School, USA
  2. Formerly of the University of Texas, USA
  3. University of Pennsylvania, USA


Abstract

CatSper channels (CatSper1-4, nomenclature as agreed by NC-IUPHAR [13]) are putative 6TM, voltage-gated, alkalinization-activated calcium permeant channels that are presumed to assemble as a tetramer of α-like subunits and mediate the current ICatSper [21]. In mammals, CatSper subunits are structurally most closely related to individual domains of voltage-activated calcium channels (Cav) [36]. CatSper1 [36], CatSper2 [33] and CatSpers 3 and 4 [25, 19, 32], in common with a putative 2TM auxiliary CatSperβ protein [24] and two putative 1TM associated CatSperγ and CatSperδ proteins [42, 11], are restricted to the testis and localised to the principle piece of sperm tail. The novel cross-species CatSper channel inhibitor, RU1968, has been proposed as a useful tool to aid characterisation of native CatSper channels [37].

Two-pore channels (TPCs) are structurally related to CatSpers, CaVs and NaVs. TPCs have a 2x6TM structure with twice the number of TMs of CatSpers and half that of CaVs. There are three animal TPCs (TPC1-TPC3). Humans have TPC1 and TPC2, but not TPC3. TPC1 and TPC2 are localized in endosomes and lysosomes [4]. TPC3 is also found on the plasma membrane and forms a voltage-activated, non-inactivating Na+ channel [5]. All the three TPCs are Na+-selective under whole-cell or whole-organelle patch clamp recording [44, 7, 6]. The channels may also conduct Ca2+ [29].

Contents

This is a citation summary for CatSper and Two-Pore channels in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts.

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

CatSper and Two-Pore channels
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=70
Introduction to CatSper and Two-Pore channels
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=70
    Channels and Subunits
            CatSper1
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=388
            CatSper2
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=389
            CatSper3
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=390
            CatSper4
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=391
            TPC1
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=392
            TPC2
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=393

References

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