IndraLab

Statements

Erythromycin A inhibits KCNH2. 21 / 22
2 | 15 4
reach
"XREF_BIBR Hyperthermia exaggerates block of HERG by erythromycin in LTC cells as well as APD prolongation by this drug in mouse isolated ventricular myocytes."
19649147
reach
"Pretreatment with erythromycin induced an approximately 14-22-fold reduction in hERG affinity for pore binding drugs at concentrations of erythromycin, which by themselves only block hERG by 10% or less."
24417241
sparser
"Understanding how erythromycin inhibits the hERG could help us to decide which compounds are needed for further studies."
37446837
sparser
"Mean data comparing percentage of I hERG tail inhibition by 600 µM erythromycin is shown in Figure xref ."
32147975
reach
"At a concentration of 100muM, erythromycin causes no significant block of hERG currents at RT but significantly blocks currents at physiological temperature."
22131976
reach
"At higher concentrations (300muM), erythromycin did block hERG currents at RT by approximately 40% and gave an IC 50 of 427.5 muM calculated from the graph (n = 12)."
22131976
reach
"Erythromycin has been shown to block hERG channels at physiological temperature with an IC 50 of approximately 40muM."
22131976
reach
"It is noteworthy that the hERG blocker erythromycin blocks cell cycle in G2 phase if administered together with vincristine."
21850047
reach
"The results of this study document that both erythromycin and clarithromycin significantly inhibit the HERG potassium current at clinically relevant concentrations."
14674677
reach
"[Erythromycin inhibits the proliferation of HERG K+ channel highly expressing cancer cells and shows synergy with anticancer drugs]."
17313833
reach
"XREF_BIBR - XREF_BIBR, XREF_BIBR, XREF_BIBR Similar to AZA1 (C 47 H 71 NO 12), the macrolide antibiotic erythromycin (C 37 H 67 NO 13) also blocks hERG1 rapidly in an open-state dependent manner and analysis of mutant channels and molecular modeling indicate that it interacts with phenylalanine reside at position 656 but not with tyrosine reside at position 652."
22856456
ctd
No evidence text available
24052561
reach
"Erythromycin block of the HERG K+ channel : accessibility to F656 and Y652."
16446155
reach
"A metabolite of erythromycin, des-methyl erythromycin, was also found to inhibit HERG current with an IC (50) of 147.1 microM."
12065733
reach
"Compounds with strong APD prolonging ability include Ca 2+ channel agonists like Bay K8644; class Ia antiarrhythmics (e.g., quinidine); unintended hERG channel blockers like the antibiotic erythromycin; certain class III antiarrhythmics (e.g., E4031); and a large variety of neurotoxins (e.g., anemone toxin)."
30210937
reach
"At 300muM, erythromycin blocked hERG currents at 35degreesC by 70% and the IC 50 at this temperature was calculated to be 30.7 muM (n = 18)."
22131976
ctd
No evidence text available
15272206
reach
"The same was true for other hERG channel blockers (like erythromycin, moxifloxacin and sematilide) and multi-ion channel blockers."
29311989
reach
"Here we used whole-cell patch-clamp recording at 37 degrees C from heterologously expressed HERG channels in a mammalian cell line to show that erythromycin either produces a rapid open-state-dependent HERG channel inhibition, or components of both open-state-dependent and closed-state-dependent inhibition."
16446155
sparser
"Figure xref shows the concentration dependence of I hERG inhibition by erythromycin, terfenadine and thioridazine under the recording conditions of this study, with representative traces of effects of single drug concentrations shown in Figure xref i–ci and concentration–response relations shown in Figure xref ii–cii."
32147975
sparser
"The Strength of hERG Inhibition by Erythromycin at Different Temperatures Might Be Due to Its Interacting Features with the Channels."
37446837