{"title":"靶向治疗的新领域:利用 PROTAC 和先进给药系统","authors":"Robert B. Kargbo*, ","doi":"10.1021/acsmedchemlett.4c0048910.1021/acsmedchemlett.4c00489","DOIUrl":null,"url":null,"abstract":"<p >In the rapidly evolving field of oncology, the need for innovative therapeutic strategies is more pressing than ever. Many cancers, especially those driven by gene mutations like KRAS, remain challenging to treat. Traditional approaches, which often rely on small-molecule inhibitors, face significant limitations, particularly in addressing “undruggable” targets or delivering large therapeutic molecules across cellular membranes. As highlighted by four essential patents, the recent advancements in Proteolysis Targeting Chimeras (PROTACs) and intracellular delivery systems offer novel and promising strategies to overcome these challenges.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"15 11","pages":"1818–1820 1818–1820"},"PeriodicalIF":3.5000,"publicationDate":"2024-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A New Frontier in Targeted Therapies: Harnessing PROTACs and Advanced Delivery Systems\",\"authors\":\"Robert B. Kargbo*, \",\"doi\":\"10.1021/acsmedchemlett.4c0048910.1021/acsmedchemlett.4c00489\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >In the rapidly evolving field of oncology, the need for innovative therapeutic strategies is more pressing than ever. Many cancers, especially those driven by gene mutations like KRAS, remain challenging to treat. Traditional approaches, which often rely on small-molecule inhibitors, face significant limitations, particularly in addressing “undruggable” targets or delivering large therapeutic molecules across cellular membranes. As highlighted by four essential patents, the recent advancements in Proteolysis Targeting Chimeras (PROTACs) and intracellular delivery systems offer novel and promising strategies to overcome these challenges.</p>\",\"PeriodicalId\":20,\"journal\":{\"name\":\"ACS Medicinal Chemistry Letters\",\"volume\":\"15 11\",\"pages\":\"1818–1820 1818–1820\"},\"PeriodicalIF\":3.5000,\"publicationDate\":\"2024-10-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acsmedchemlett.4c00489\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acsmedchemlett.4c00489","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
A New Frontier in Targeted Therapies: Harnessing PROTACs and Advanced Delivery Systems
In the rapidly evolving field of oncology, the need for innovative therapeutic strategies is more pressing than ever. Many cancers, especially those driven by gene mutations like KRAS, remain challenging to treat. Traditional approaches, which often rely on small-molecule inhibitors, face significant limitations, particularly in addressing “undruggable” targets or delivering large therapeutic molecules across cellular membranes. As highlighted by four essential patents, the recent advancements in Proteolysis Targeting Chimeras (PROTACs) and intracellular delivery systems offer novel and promising strategies to overcome these challenges.
期刊介绍:
ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to:
Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics)
Biological characterization of new molecular entities in the context of drug discovery
Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc.
Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry
Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources
Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response
Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic
Mechanistic drug metabolism and regulation of metabolic enzyme gene expression
Chemistry patents relevant to the medicinal chemistry field.