Paper Details 
Original Abstract of the Article :
Structurally related inhibitors of a shared therapeutic target may differ regarding potential toxicity issues that are caused by different off-target bindings. We devised a differential competition capture compound mass spectrometry (dCCMS) strategy to effectively differentiate off-target profiles. ...See full text at original site
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引用元:
https://doi.org/10.1021/acs.jmedchem.5b01970

データ提供:米国国立医学図書館(NLM)

Navigating the Desert of Drug Discovery: Identifying Off-Target Toxicity Liabilities of COMT Inhibitors

Imagine the vast desert of [drug discovery], where researchers explore the intricate landscape of molecules and their interactions with the human body. This research, like a team of skilled pharmacologists, delves into the potential toxicity liabilities of [catechol-O-methyltransferase (COMT)] inhibitors, medications used to treat [Parkinson's disease]. The authors, like astute detectives, investigate the off-target binding of COMT inhibitors, seeking to identify potential sources of toxicity.

Their findings, like a well-charted oasis in the desert, reveal that the COMT inhibitor [tolcapone] exhibits off-target binding to [3-hydroxyisobutyryl-CoA hydrolase (HIBCH)], a protein not targeted by the less toxic COMT inhibitor [entacapone]. This discovery offers valuable insights into the structure-activity relationships of COMT inhibitors and provides a foundation for developing safer and more specific medications.

A Journey Towards Safer Drugs: Understanding Off-Target Binding in Drug Development

The study's findings emphasize the importance of understanding the off-target binding profiles of drugs during the development process. The authors highlight the need for careful evaluation of potential toxicity liabilities to ensure that medications are safe and effective for patients.

A Desert of Uncertainty: The Search for Safer and More Effective Treatments

This research underscores the ongoing need for innovation and vigilance in [drug discovery]. The authors emphasize the importance of developing new strategies to identify and mitigate potential toxicity liabilities, ensuring that patients receive safe and effective treatments.

Dr. Camel's Conclusion

This study reminds us that the desert of [drug discovery] is a complex and challenging terrain. By diligently exploring the intricacies of molecular interactions and potential off-target effects, we can guide the development of safer and more effective medications for patients.

Date :
  1. Date Completed 2017-05-29
  2. Date Revised 2017-12-26
Further Info :

Pubmed ID

27074629

DOI: Digital Object Identifier

10.1021/acs.jmedchem.5b01970

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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