Target Information

Target General Infomation
Target ID
T67063
Former ID
TTDI01980
Target Name
Maxi K potassium channel
Gene Name
KCNMB4
Synonyms
Calcium activated potassium KCNMA1 (maxiK) channel; KCNMB4
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Erectile dysfunction [ICD9: 302.72, 607.84; ICD10: F52.2, N48.4]
Function
Regulatory subunit of the calcium activated potassium KCNMA1 (maxiK) channel. Modulates the calcium sensitivity and gating kinetics of KCNMA1, thereby contributing to KCNMA1 channel diversity. Increases the apparent Ca(2+)/voltage sensitivity of the KCNMA1 channel. It also modifies KCNMA1 channel kinetics and alters its pharmacological properties. It slows down the activation and the deactivation kinetics of the channel. Acts as a negative regulator of smooth muscle contraction by enhancing the calcium sensitivity to KCNMA1. Its presence is also a requirement for internal binding of the KCNMA1 channel opener dehydrosoyasaponin I (DHS-1) triterpene glycoside and for external binding of the agonist hormone 17-beta-estradiol (E2). Increases the binding activity of charybdotoxin (CTX) toxin to KCNMA1 peptide blocker by increasing the CTX association rate and decreasing the dissociation rate.
BioChemical Class
Calcium-activated potassium channel
UniProt ID
Q86W47
Sequence
MAKLRVAYEYTEAEDKSIRLGLFLIISGVVSLFIFGFCWLSPALQDLQATEANCTVLSVQ
QIGEVFECTFTCGADCRGTSQYPCVQVYVNNSESNSRALLHSDEHQLLTNPKCSYIPPCK
RENQKNLESVMNWQQYWKDEIGSQPFTCYFNQHQRPDDVLLHRTHDEIVLLHCFLWPLVT
FVVGVLIVVLTICAKSLAVKAEAMKKRKFS
Structure
2K44; 3MT5; 3NAF
Drugs and Mode of Action
Drug(s) BMS-223131 Drug Info Phase 2 Erectile dysfunction [527426]
CNS-1237 Drug Info Terminated Cerebrovascular ischaemia [545045]
NS-1619 Drug Info Terminated Asthma [467609], [545014]
Modulator BMS-223131 Drug Info [527426]
CNS-1237 Drug Info [534454]
NS-1619 Drug Info
Inhibitor iberiotoxin Drug Info [543803]
tetraethylammonium Drug Info [543803]
Blocker (channel blocker) paxilline Drug Info [534285]
slotoxin Drug Info [526152]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cGMP-PKG signaling pathway
Vascular smooth muscle contraction
Insulin secretion
Salivary secretion
Pancreatic secretion
Reactome cGMP effects
WikiPathways Potassium Channels
Platelet homeostasis
References
Ref 467609(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4272).
Ref 527426Effect of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), a novel opener of large conductance Ca2+-activated K+ (maxi-K) channels on normal and stress-aggravated colonic motility and visceral nociception. J Pharmacol Exp Ther. 2005 May;313(2):840-7. Epub 2005 Feb 8.
Ref 545014Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001878)
Ref 545045Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001959)
Ref 526152Slotoxin, alphaKTx1.11, a new scorpion peptide blocker of MaxiK channels that differentiates between alpha and alpha+beta (beta1 or beta4) complexes. FEBS Lett. 2001 Sep 21;505(3):369-73.
Ref 527426Effect of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), a novel opener of large conductance Ca2+-activated K+ (maxi-K) channels on normal and stress-aggravated colonic motility and visceral nociception. J Pharmacol Exp Ther. 2005 May;313(2):840-7. Epub 2005 Feb 8.
Ref 534285Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology. 1996;35(7):963-8.
Ref 534454Effects of Ca2+ and Na+ channel inhibitors in vitro and in global cerebral ischaemia in vivo. Eur J Pharmacol. 1997 Aug 6;332(2):121-31.
Ref 543803(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 380).

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