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Identification of Potential Off-target Toxicity Liabilities of Catechol-O-methyltransferase Inhibitors by Differential Competition Capture Compound Mass Spectrometry.
Author: BarthoKathrin, DregerMathias, GraebnerOlivia, KoesterHubert, KrollFriedrich, LuoYan, MichaelisSimon, SchliefMarén, SchreyAnna K, SefkowMichael, von KleistLisa
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
Dr.Camel's Paper Summary Blogラクダ博士について
ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
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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 :
- Date Completed 2017-05-29
- Date Revised 2017-12-26
Further Info :
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English
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