October 9, 2014British Journal of PharmacologyOpen Access

Kv11.1(hERG)‐induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypicalKv11.1(hERG) inhibitors

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Population

In vitro model evaluating 15 prototypical Kv11.1 (hERG) inhibitors

Design

Preclinical

Authors

ZYZhiyi YuShandong University AIAdriaan P. IJzermanLeiden University LHLaura H. HeitmanLeiden University

Discussion

Member takes

Implication

Hypothesis-generating for association-rate focused hERG screening; leaves open translation to clinical QT risk assessment.

Structured PICO

Population

In vitro model evaluating 15 prototypical Kv11.1 (hERG) inhibitors

Intervention

Binding kinetics evaluation using [(3)H]-dofetilide competition association assay and HPLC analysis

Outcome

Affinity (Ki values), association rates, dissociation rates, lipophilicity (logKW - C8), and membrane partitioning (logKW - IAM)surrogate

A compound's affinity for the Kv11.1 (hERG) channel is driven by its association rate rather than dissociation rate or lipophilicity, providing mechanistic insights into drug-induced cardiotoxicity.

Cite This Study

Yu et al. (2014) studied this question.

synapsesocial.com/papers/6a8085e69fb6070370cae455 https://doi.org/10.1111/bph.12967

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Kv11.1(hERG)‐induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypicalKv11.1(hERG) inhibitors

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Kv11.1(hERG)‐induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypicalKv11.1(hERG) inhibitors

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Also Consider

Also Consider