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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 대한약리학회 The Korean Journal of Physiology & Pharmacology The Korean Journal of Physiology & Pharmacology 제24권 제1호
- 발행연도
- 2020.1
- 수록면
- 101 - 110 (10page)
이용수
초록· 키워드
오류제보하기
Transient receptor potential canonical 4 (TRPC4) channel is a nonselective calcium-permeable cation channels. In intestinal smooth muscle cells, TRPC4 currents contribute more than 80% to muscarinic cationic current (mIcat). With its inward-rectifying current-voltage relationship and high calcium permeability, TRPC4 channels permit calcium influx once the channel is opened by muscarinic receptor stimulation. Polyamines are known to inhibit nonselective cation channels that mediate the generation of mIcat. Moreover, it is reported that TRPC4 channels are blocked by the intracellular spermine through electrostatic interaction with glutamate residues (E728, E729). Here, we investigated the correlation between the magnitude of channel inactivation by spermine and the magnitude of channel conductance. We also found additional spermine binding sites in TRPC4. We evaluated channel activity with electrophysiological recordings and revalidated structural significance based on Cryo-EM structure, which was resolved recently. We found that there is no correlation between magnitude of inhibitory action of spermine and magnitude of maximum current of the channel. In intracellular region, TRPC4 attracts spermine at channel periphery by reducing access resistance, and acidic residues contribute to blocking action of intracellular spermine; channel periphery, E649; cytosolic space, D629, D649, and E687.
목차
등록된 정보가 없습니다.
참고문헌 (30)
참고문헌 신청
Beech DJ / 2005 / TRPC1 : store-operated channel and more / Pflugers Arch 451:53~60
Zholos AV / 2014 / TRPC5 / Handb Exp Pharmacol 222:129~156
Kim YC / 1998 / Suppression of the carbachol-activated nonselective cationic current by antibody against alpha subunit of Go protein in guineapig gastric myocytes / Pflugers Arch 436:494~496
Sakamoto T / 2007 / Three distinct muscarinic signalling pathways for cationic channel activation in mouse gut smooth muscle cells / J Physiol 582(Pt 1):41~61
Tsvilovskyy VV / 2009 / Deletion of TRPC4 and TRPC6 in mice impairs smooth muscle contraction and intestinal motility in vivo / Gastroenterology 137:1415~1424
Zholos AV / 2014 / TRPC5 / Handb Exp Pharmacol 222:129~156
Kim YC / 1998 / Suppression of the carbachol-activated nonselective cationic current by antibody against alpha subunit of Go protein in guineapig gastric myocytes / Pflugers Arch 436:494~496
Sakamoto T / 2007 / Three distinct muscarinic signalling pathways for cationic channel activation in mouse gut smooth muscle cells / J Physiol 582(Pt 1):41~61
Tsvilovskyy VV / 2009 / Deletion of TRPC4 and TRPC6 in mice impairs smooth muscle contraction and intestinal motility in vivo / Gastroenterology 137:1415~1424
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