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MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-04-30 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00095 Douglas C. Beshore 1 , Christina N. Di Marco 1 , Ronald K. Chang 1 , Thomas J. Greshock 1 , Lei Ma 1 , Marion Wittmann 1 , Matthew A. Seager 1 , Kenneth A. Koeplinger 1 , Charles D. Thompson 1 , Joy Fuerst 1 , George D. Hartman 1 , Mark T. Bilodeau 1 , William J. Ray 1 , Scott D. Kuduk 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-04-30 00:00:00 , DOI: 10.1021/acsmedchemlett.8b00095 Douglas C. Beshore 1 , Christina N. Di Marco 1 , Ronald K. Chang 1 , Thomas J. Greshock 1 , Lei Ma 1 , Marion Wittmann 1 , Matthew A. Seager 1 , Kenneth A. Koeplinger 1 , Charles D. Thompson 1 , Joy Fuerst 1 , George D. Hartman 1 , Mark T. Bilodeau 1 , William J. Ray 1 , Scott D. Kuduk 1
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Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M1 muscarinic receptor that has entered Phase II studies in patients with Alzheimer’s disease.
中文翻译：
MK-7622：一流的M 1正变构调节剂开发候选人
数十年来一直寻求鉴定能选择性激活M 1毒蕈碱信号通路的配体，以治疗一系列神经系统疾病和认知障碍。本文中，我们描述了优化工作，重点是解决关键的理化和安全性问题，最终导致了临床候选药物MK-7622，M 1毒蕈碱受体的高度选择性正变构调节剂，已进入阿尔茨海默氏病患者的II期研究。
更新日期：2018-04-30
中文翻译：
MK-7622：一流的M 1正变构调节剂开发候选人
数十年来一直寻求鉴定能选择性激活M 1毒蕈碱信号通路的配体，以治疗一系列神经系统疾病和认知障碍。本文中，我们描述了优化工作，重点是解决关键的理化和安全性问题，最终导致了临床候选药物MK-7622，M 1毒蕈碱受体的高度选择性正变构调节剂，已进入阿尔茨海默氏病患者的II期研究。
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