February 24, 2003Proceedings of the National Academy of Sciences

Modulation of cardiac Ca V 1.2 channels by dihydropyridine and phosphatase inhibitor requires Ser-1142 in the domain III pore loop

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Population

Recombinant cardiac calcium channel, Ca(V)1.2 (alpha(1)C) in cell-attached patches

Comparison

Dihydropyridine and okadaic acid vs Mutant channels (Ser-1142 to Ala or Cys)

Design

Preclinical

Authors

CEChristian ErxlebenLoyola University Chicago CGClaudio GómezNational Agricultural Technology Institute TDThomas A. DardenNew Mexico Department of Health

Discussion

Member takes

Implication

May guide CaV1.2 modulator development; leaves open relevance to human cardiac disease or therapy.

Structured PICO

Population

Recombinant cardiac calcium channel, Ca(V)1.2 (alpha(1)C) in cell-attached patches

Intervention

Dihydropyridine (BayK8644) and okadaic acid (inhibitor of SerThr protein phosphatases)

Comparator

Mutant channels (Ser-1142 to Ala or Cys)

Outcome

Channel gating activity (mode 2 gating and prevention of rundown)surrogate

BayK binding stabilizes mode 2 gating allosterically by either protecting a phospho Ser/Thr on the alpha(1)C subunit or mimicking phosphorylation at Ser-1142.

Cite This Study

Erxleben et al. (2003) studied this question.

synapsesocial.com/papers/6a21cbee4c1bee377cecaeaf https://doi.org/10.1073/pnas.2628046100

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Modulation of cardiac Ca V 1.2 channels by dihydropyridine and phosphatase inhibitor requires Ser-1142 in the domain III pore loop

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Modulation of cardiac Ca V 1.2 channels by dihydropyridine and phosphatase inhibitor requires Ser-1142 in the domain III pore loop

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider