What is the clinical evidence from this study?

Intervention: EMD 57033. Primary outcome: Interaction with recombinant human cardiac TnC (hcTnC).

What question did this study set out to answer?

This research aims to explore the interaction between EMD 57033, a cardiotonic thiadiazinone derivative, and human cardiac troponin C (hcTnC).

January 1, 1996Journal of Biological ChemistryOpen Access

Interaction of Cardiotonic Thiadiazinone Derivatives with Cardiac Troponin C

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Key result

EMD 57033 interacts directly and stereo-selectively with recombinant human cardiac troponin C in a calcium-dependent manner, with a binding site likely residing in the carboxyl domain.

Key Points

This research aims to explore the interaction between EMD 57033, a cardiotonic thiadiazinone derivative, and human cardiac troponin C (hcTnC).
Tested direct interaction of EMD 57033 with recombinant hcTnC using fluorescence techniques and binding assays.
Determined the Kd for the drug-hcTnC interaction under varying calcium and magnesium conditions.
Assessed changes in tyrosine and bis-ANS fluorescence upon EMD 57033 treatment.
EMD 57033 demonstrated a Kd of approximately 40 µM for the drug-hcTnC interaction in the presence of Ca2+.
Binding was Ca2+ dependent and stereoselective, indicating significantly weaker interaction with the optical isomer of EMD 57033.
Interference with Ca2+-dependent binding of bis-ANS to hcTnC was observed, suggesting a new drug-binding site induced by Ca2+ binding.

Structured PICO

Population

Recombinant human cardiac troponin C (hcTnC)

Intervention

EMD 57033 (cardiotonic thiadiazinone derivative)

Outcome

Direct interaction and binding affinity (Kd) between EMD 57033 and hcTnCsurrogate

EMD 57033 binds directly to the carboxyl domain of human cardiac troponin C in a calcium-dependent manner, elucidating its mechanism of action on cardiac myofilaments.

Discussion

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Implication

Does not alter clinical practice; leaves open targeted myofilament modulation in human heart failure.

Cite This Study

Pan et al. (1996) studied this question. EMD 57033 was evaluated on Interaction with recombinant human cardiac TnC (hcTnC). EMD 57033 interacts directly and stereo-selectively with recombinant human cardiac troponin C in a calcium-dependent manner, with a binding site likely residing in the carboxyl domain.

synapsesocial.com/papers/6a0f7a9fd8c5cf602efcc288 https://doi.org/10.1074/jbc.271.2.817

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Interaction of Cardiotonic Thiadiazinone Derivatives with Cardiac Troponin C

Key Points

Structured PICO

Discussion

Implication

Cite This Study

Interaction of Cardiotonic Thiadiazinone Derivatives with Cardiac Troponin C

Key Points

Structured PICO

Discussion

Implication

Cite This Study

Also Consider

Also Consider