发布求助
文献互助 智能选刊 最新文献

ACS Medicinal Chemistry Letters最新文献

筛选
英文 中文
The Development of Inhibitors for NLRP3 Inflammasome NLRP3炎性体抑制剂的研究进展
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-30 DOI: 10.1021/acsmedchemlett.5c00437
Xin Zhou,  and , Steven H. Liang*, 
{"title":"The Development of Inhibitors for NLRP3 Inflammasome","authors":"Xin Zhou,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00437","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00437","url":null,"abstract":"<p >This patent highlights the preparation, pharmaceutical compositions, and therapeutic applications of NLRP3 inflammasome inhibitors. NLRP3 [NOD (Nucleotide-binding Oligomerization Domain)-like receptor family pyrin domain containing 3] is a versatile protein that plays a significant role in the immune system, particularly in mediating responses to tissue infections and damage. NLRP3 is crucial in the innate immune response through the formation of a multiprotein complex known as the inflammasome.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1513–1514"},"PeriodicalIF":4.0,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826204","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors for the Treatment of Parkinson’s Disease 新型富亮氨酸重复激酶2 （LRRK2）抑制剂治疗帕金森病
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-30 DOI: 10.1021/acsmedchemlett.5c00438
Zhendong Song,  and , Steven H. Liang*, 
{"title":"Novel Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors for the Treatment of Parkinson’s Disease","authors":"Zhendong Song,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00438","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00438","url":null,"abstract":"<p >This patent describes novel leucine-rich repeat kinase 2 (LRRK2) inhibitors featuring a 2,4,12,13-tetrahydro-11<i>H</i>-5,7-(azenometheno)dipyrazolo[3,4-<i>b</i>:5′,1′-<i>g</i>][1]oxa[4,6,8]triazacycloundecine scaffold. These LRRK2 inhibitors exhibit therapeutic potential for the treatment of Parkinson’s disease.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1511–1512"},"PeriodicalIF":4.0,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826245","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Compounds as 5-HT2A Agonists for Treating Depression 新化合物作为5-HT2A激动剂治疗抑郁症
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-30 DOI: 10.1021/acsmedchemlett.5c00441
Ram W. Sabnis*, 
{"title":"Novel Compounds as 5-HT2A Agonists for Treating Depression","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00441","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00441","url":null,"abstract":"<p >Provided herein are novel compounds as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating depression, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1522–1523"},"PeriodicalIF":4.0,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826222","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Non-hallucinogenic Neurite Growth Compounds as 5-HT2A Agonists for Treating Stress-Related Disorders, Namely Depression, Anxiety, and PTSD 新型非致幻神经突生长化合物作为5-HT2A激动剂治疗应激相关疾病，即抑郁、焦虑和创伤后应激障碍
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-30 DOI: 10.1021/acsmedchemlett.5c00440
Ram W. Sabnis*, 
{"title":"Novel Non-hallucinogenic Neurite Growth Compounds as 5-HT2A Agonists for Treating Stress-Related Disorders, Namely Depression, Anxiety, and PTSD","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00440","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00440","url":null,"abstract":"<p >Provided herein are novel non-hallucinogenic neurite growth compounds as 5-HT2A agonists, pharmaceutical compositions, use of such compounds in treating stress-related disorders, namely depression, anxiety, and post-traumatic stress disorder (PTSD), and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1524–1525"},"PeriodicalIF":4.0,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826294","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Thieno[3,2-b]Pyridine Derivatives in the Treatment of Huntington’s Disease 新型Thieno[3,2-b]吡啶衍生物治疗亨廷顿舞蹈病
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-30 DOI: 10.1021/acsmedchemlett.5c00436
Taoqian Zhao,  and , Steven H. Liang*, 
{"title":"Novel Thieno[3,2-b]Pyridine Derivatives in the Treatment of Huntington’s Disease","authors":"Taoqian Zhao,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00436","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00436","url":null,"abstract":"<p >The present invention relates to novel thieno[3,2-<i>b</i>]pyridine derivatives represented by Formula I. These compounds are specifically designed to modulate HTT expression, providing enhanced therapeutic potential for the treatment of Huntington’s disease.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1515–1516"},"PeriodicalIF":4.0,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826165","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Compounds as Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis 新化合物作为emopamil结合蛋白抑制剂治疗多发性硬化
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-29 DOI: 10.1021/acsmedchemlett.5c00425
Ram W. Sabnis*, 
{"title":"Novel Compounds as Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00425","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00425","url":null,"abstract":"<p >Provided herein are novel compounds as Emopamil-Binding Protein (EBP) inhibitors, pharmaceutical compositions, use of such compounds in treating multiple sclerosis, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1509–1510"},"PeriodicalIF":4.0,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Mixed Serotonin Receptor Binder Compounds as 5-HT2C Agonists for Treating Psychotic Disorders 新型混合5-羟色胺受体结合剂作为5-HT2C激动剂治疗精神障碍
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-29 DOI: 10.1021/acsmedchemlett.5c00427
Ram W. Sabnis*, 
{"title":"Novel Mixed Serotonin Receptor Binder Compounds as 5-HT2C Agonists for Treating Psychotic Disorders","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00427","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00427","url":null,"abstract":"<p >Provided herein are novel mixed serotonin receptor binder compounds as 5-HT2C agonists, pharmaceutical compositions, use of such compounds in treating psychotic disorders, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1505–1506"},"PeriodicalIF":4.0,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of a Small Molecule TREM2 Agonist with Improved In Vitro Pharmacokinetic Profile and Validated Target Engagement 一种小分子TREM2激动剂的发现，具有改善的体外药代动力学特征和有效的靶标结合
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-29 DOI: 10.1021/acsmedchemlett.5c00299
Shaoren Yuan, Farida El Gaamouch, Sungwoo Cho, Katarzyna Kuncewicz, Hossam Nada and Moustafa T. Gabr*, 
{"title":"Discovery of a Small Molecule TREM2 Agonist with Improved In Vitro Pharmacokinetic Profile and Validated Target Engagement","authors":"Shaoren Yuan,&nbsp;Farida El Gaamouch,&nbsp;Sungwoo Cho,&nbsp;Katarzyna Kuncewicz,&nbsp;Hossam Nada and Moustafa T. Gabr*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00299","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00299","url":null,"abstract":"<p >The microglial lipid-sensing receptor TREM2 is a promising therapeutic target for Alzheimer’s disease. We report the discovery of <b>C1</b>, a racemic structural analog of the clinical-stage TREM2 agonist <b>VG-3927</b>. Synthesized via a concise, modular, and enantioselective-free route using sequential Suzuki couplings, <b>C1</b> enables rapid scaffold diversification. Compared to <b>VG-3927</b>, this stereochemically simplified derivative exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells, demonstrating validated target engagement. Direct binding of <b>C1</b> to TREM2 was unequivocally confirmed by both surface plasmon resonance (SPR) and microscale thermophoresis (MST). Critically, <b>C1</b> displays a superior in vitro pharmacokinetic profile to <b>VG-3927</b>: enhanced metabolic stability in human and mouse liver microsomes, favorable passive permeability (PAMPA), and a CNS-compatible log D<sub>7</sub>.<sub>4</sub>. Docking studies suggest a potential binding mode for <b>C1</b> within TREM2’s extracellular domain, revealing key interactions. These attributes establish <b>C1</b> as an accessible and pharmacokinetically favorable lead compound with strong potential for developing TREM2-targeted therapies.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1634–1640"},"PeriodicalIF":4.0,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evolving Landscape: Accounts of Academic-Industrial Collaborations in Chemistry Technology 不断发展的景观：化学技术的学术-工业合作
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-28 DOI: 10.1021/acsmedchemlett.5c00373
Aristidis Vasilopoulos*,  and , Ying Wang*, 
{"title":"Evolving Landscape: Accounts of Academic-Industrial Collaborations in Chemistry Technology","authors":"Aristidis Vasilopoulos*,&nbsp; and ,&nbsp;Ying Wang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00373","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00373","url":null,"abstract":"<p >Academic-industrial collaborations in the pharmaceutical industry have led to advances in novel science and pipeline goals. These partnerships find success by leveraging the resources and expertise of the industrial sector with the creativity and depth of knowledge of academic researchers. Here, we discuss case studies of several past and present academic-industrial collaborations from a chemistry technology group and their evolution from operating under funding-driven models to more reciprocal exchanges of effort and information. Effective partnerships depend on the careful selection of the right collaborators and projects, and they require clear communication, alignment of interests, and patience throughout the phases of a collaboration. Research areas of high interest for academic collaborations are discussed, such as advancements in synthetic methodology and drug discovery platforms such as DNA-encoded libraries and PROTACS.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1473–1479"},"PeriodicalIF":4.0,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826201","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of an All-Hydrocarbon Stapled Peptide Targeting BRK1 in Triple-Negative Breast Cancer 三阴性乳腺癌中靶向BRK1的全碳氢钉接肽的开发
IF 4 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-07-28 DOI: 10.1021/acsmedchemlett.5c00221
Matthew K. Whittaker, Taylor C. Dill, Ameya J. Limaye, Nicholas J. Tsavaris, Nicholas W. Tawadrous and Eileen J. Kennedy*, 
{"title":"Development of an All-Hydrocarbon Stapled Peptide Targeting BRK1 in Triple-Negative Breast Cancer","authors":"Matthew K. Whittaker,&nbsp;Taylor C. Dill,&nbsp;Ameya J. Limaye,&nbsp;Nicholas J. Tsavaris,&nbsp;Nicholas W. Tawadrous and Eileen J. Kennedy*,&nbsp;","doi":"10.1021/acsmedchemlett.5c00221","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00221","url":null,"abstract":"<p >Wiskott-Aldrich syndrome protein family (WASF) members are key regulators of actin cytoskeleton dynamics at the leading edge of the cell membrane. WASF3 has been demonstrated to directly promote cancer invasion and metastasis in triple-negative breast cancer. WASF3 is incorporated into a heteropentameric protein complex with BRK1, CYFIP1/2, NCKAP1/1L, and ABI1/2/3 termed the WASF Regulatory Complex (WRC) that links upstream signaling pathways to Arp2/3-mediated actin nucleation. Disruption of the complex inhibits actin remodeling and presents a novel approach to targeting cancer invasion and metastasis. Here we report the development of a first-generation all-hydrocarbon stapled BRK1 mimetic peptide, BASH-2, designed to inhibit BRK1 binding within the WRC to disrupt proper WRC assembly and function. BASH-2 was found to permeate cells, bind to WASF3 and ABI2, and inhibit cancer cell migration and invasion in a dose-dependent manner. BASH-2 may present a novel approach to targeting WASF3-promoted invasion and metastasis in triple-negative breast cancer.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 8","pages":"1585–1591"},"PeriodicalIF":4.0,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144826163","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
首页 上一页 下一页 尾页
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整，为了账户安全，请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们：info@booksci.cn Book学术提供免费学术资源搜索服务，方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号：604180095
Book学术官方微信