{"title":"负变构调节剂A2AR：癌症免疫治疗的新武器？","authors":"Alfonso Zambon","doi":"10.1021/acs.jmedchem.5c00137","DOIUrl":null,"url":null,"abstract":"Adenosine-mediated activation of A<sub>2A</sub>R drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A<sub>2A</sub>R with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target limitations, NAMs leverage a noncompetitive, saturable mechanism that enhances receptor selectivity. The development of a novel series of A<sub>2A</sub>R NAMs demonstrates potent activity within high-adenosine TMEs, underscoring a significant translational potential in oncology.","PeriodicalId":46,"journal":{"name":"Journal of Medicinal Chemistry","volume":"5 1","pages":""},"PeriodicalIF":6.8000,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Negative Allosteric Modulators of A2AR: A New Weapon for Cancer Immunotherapy?\",\"authors\":\"Alfonso Zambon\",\"doi\":\"10.1021/acs.jmedchem.5c00137\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Adenosine-mediated activation of A<sub>2A</sub>R drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A<sub>2A</sub>R with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target limitations, NAMs leverage a noncompetitive, saturable mechanism that enhances receptor selectivity. The development of a novel series of A<sub>2A</sub>R NAMs demonstrates potent activity within high-adenosine TMEs, underscoring a significant translational potential in oncology.\",\"PeriodicalId\":46,\"journal\":{\"name\":\"Journal of Medicinal Chemistry\",\"volume\":\"5 1\",\"pages\":\"\"},\"PeriodicalIF\":6.8000,\"publicationDate\":\"2025-01-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.jmedchem.5c00137\",\"RegionNum\":1,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.jmedchem.5c00137","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Negative Allosteric Modulators of A2AR: A New Weapon for Cancer Immunotherapy?
Adenosine-mediated activation of A2AR drives immunosuppressive signaling in high-adenosine tumor microenvironments (TMEs), impeding anticancer immunity. Targeting A2AR with negative allosteric modulators (NAMs) is a promising approach for cancer immunotherapy: unlike the orthosteric antagonists currently in use, which face competitive and off-target limitations, NAMs leverage a noncompetitive, saturable mechanism that enhances receptor selectivity. The development of a novel series of A2AR NAMs demonstrates potent activity within high-adenosine TMEs, underscoring a significant translational potential in oncology.
期刊介绍：
The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents.
The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.
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