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Fungal Pathogens: Life Cycle, Infection, Host Immunity, and Drug Discovery 真菌病原体：生命周期、感染、宿主免疫和药物发现
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-24 DOI: 10.1021/acsmedchemlett.5c0020310.1021/acsmedchemlett.5c00203
Kaustuv Sanyal,  and , Jayanta Haldar*, 
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引用次数: 0
Gold(I) N-Heterocyclic Carbene Complexes as Ferroptosis Inducing Anticancer Agents 金(I) n -杂环卡宾配合物作为诱导铁下垂的抗癌剂
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-24 DOI: 10.1021/acsmedchemlett.5c0009610.1021/acsmedchemlett.5c00096
Evelyn Schlegel, Zisis Papadopoulos, Nicolás Montesdeoca, Vladislav A. Voloshkin, Steven P. Nolan, Stephan A. Hahn*, Thomas Scattolin* and Johannes Karges*, 
{"title":"Gold(I) N-Heterocyclic Carbene Complexes as Ferroptosis Inducing Anticancer Agents","authors":"Evelyn Schlegel,&nbsp;Zisis Papadopoulos,&nbsp;Nicolás Montesdeoca,&nbsp;Vladislav A. Voloshkin,&nbsp;Steven P. Nolan,&nbsp;Stephan A. Hahn*,&nbsp;Thomas Scattolin* and Johannes Karges*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0009610.1021/acsmedchemlett.5c00096","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00096https://doi.org/10.1021/acsmedchemlett.5c00096","url":null,"abstract":"<p >This study presents the chemical synthesis and biological evaluation of a series of gold(I)-N-heterocyclic carbene complexes as potential anticancer agents. The compounds demonstrated broad activity against various cancer cell lines, exhibiting cytotoxicity in the low micromolar range. Mechanistic investigations revealed that these complexes preferentially accumulate in the mitochondria of cancer cells, where they induce the generation of reactive oxygen species and lipid peroxides, ultimately triggering ferroptosis. Further studies in multicellular tumor spheroids confirmed the compounds’ ability to penetrate three-dimensional cellular structures and effectively eradicate them at low micromolar concentrations. This work represents the first known example of a gold(I)-N-heterocyclic carbene complex inducing ferroptosis, expanding the therapeutic potential of gold(I)-based metallodrugs.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"856–864 856–864"},"PeriodicalIF":3.5,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917121","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
Fungal Pathogens: Life Cycle, Infection, Host Immunity, and Drug Discovery. 真菌病原体：生命周期、感染、宿主免疫和药物发现。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-24 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00203
Kaustuv Sanyal, Jayanta Haldar
{"title":"Fungal Pathogens: Life Cycle, Infection, Host Immunity, and Drug Discovery.","authors":"Kaustuv Sanyal, Jayanta Haldar","doi":"10.1021/acsmedchemlett.5c00203","DOIUrl":"10.1021/acsmedchemlett.5c00203","url":null,"abstract":"","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"700-701"},"PeriodicalIF":3.5,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067110/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143952815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Virtual High-Throughput Screening of Ligands for Disrupting PRMT5/pICLn Interaction in Prostate Cancer Cells 干扰前列腺癌细胞中PRMT5/pICLn相互作用的虚拟高通量配体筛选
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-24 DOI: 10.1021/acsmedchemlett.5c0012610.1021/acsmedchemlett.5c00126
Zhihang Shen, Gustavo Seabra and Chenglong Li*, 
{"title":"Virtual High-Throughput Screening of Ligands for Disrupting PRMT5/pICLn Interaction in Prostate Cancer Cells","authors":"Zhihang Shen,&nbsp;Gustavo Seabra and Chenglong Li*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0012610.1021/acsmedchemlett.5c00126","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00126https://doi.org/10.1021/acsmedchemlett.5c00126","url":null,"abstract":"<p >Prostate cancer (PC) is the most commonly diagnosed cancer in men worldwide. While androgen deprivation therapy (ADT) is initially effective, many patients develop resistance, progressing to castration-resistant prostate cancer (CRPC). Recent studies have identified the interaction between PRMT5 (protein arginine methyltransferase 5) and pICLn as a promising therapeutic target, as it promotes the transcription of double-strand break (DSB) repair genes that contribute to therapy resistance. To target this pathway, a screening campaign identified J021-0199 as a potential hit compound that disrupts the PRMT5/pICLn interaction. Biochemical assays demonstrated that J021-0199 binds to the N-terminal TIM barrel domain of PRMT5. In CRPC cell lines (LNCaP and 22Rv1), J021-0199 selectively inhibited cancer cell growth. qPCR analysis further revealed downregulation of DNA damage response (DDR) genes involved in homologous recombination, nonhomologous end joining, and G2 arrest. These results support J021-0199 as a promising lead compound for overcoming resistance in CRPC.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"875–879 875–879"},"PeriodicalIF":3.5,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917032","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 Thieno[3,2-b]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5. 代谢性谷氨酸受体亚型5的Thieno[3,2-b]吡啶-5-羧酰胺和2,3-二氟苯酰胺负变构调节剂的发现
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-22 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00119
Katherine E Crocker, Scott H Henderson, Rory A Capstick, David L Whomble, Aaron M Bender, Andrew S Felts, Changho Han, Julie L Engers, Natasha B Billard, Mallory A Maurer, Hyekyung P Cho, Alice L Rodriguez, Colleen M Niswender, Jordan O'Neill, Katherine J Watson, Sichen Chang, Anna L Blobaum, Olivier Boutaud, Weimin Peng, Jerri M Rook, P Jeffrey Conn, Craig W Lindsley, Kayla J Temple
{"title":"Discovery of Thieno[3,2-<i>b</i>]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5.","authors":"Katherine E Crocker, Scott H Henderson, Rory A Capstick, David L Whomble, Aaron M Bender, Andrew S Felts, Changho Han, Julie L Engers, Natasha B Billard, Mallory A Maurer, Hyekyung P Cho, Alice L Rodriguez, Colleen M Niswender, Jordan O'Neill, Katherine J Watson, Sichen Chang, Anna L Blobaum, Olivier Boutaud, Weimin Peng, Jerri M Rook, P Jeffrey Conn, Craig W Lindsley, Kayla J Temple","doi":"10.1021/acsmedchemlett.5c00119","DOIUrl":"10.1021/acsmedchemlett.5c00119","url":null,"abstract":"<p><p>This Letter describes the discovery of novel mGlu<sub>5</sub> NAMs <b>VU6031545</b> and <b>VU6024945</b>. Starting from previously reported picolinamide compounds, a structure-activity relationship study of various core isosteres was conducted, leading to the identification of thieno[3,2-<i>b</i>]pyridine-5-carboxamide and 2,3-difluorobenzamide as competent core replacements. These compounds are highly potent as well as brain penetrant with an IVIVC agreement and improved oral bioavailability in rats.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"865-874"},"PeriodicalIF":3.5,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067350/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of Thieno[3,2-b]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 代谢性谷氨酸受体亚型5的Thieno[3,2-b]吡啶-5-羧酰胺和2,3-二氟苯酰胺负变构调节剂的发现
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-22 DOI: 10.1021/acsmedchemlett.5c0011910.1021/acsmedchemlett.5c00119
Katherine E. Crocker*, Scott H. Henderson, Rory A. Capstick, David L. Whomble, Aaron M. Bender, Andrew S. Felts, Changho Han, Julie L. Engers, Natasha B. Billard, Mallory A. Maurer, Hyekyung P. Cho, Alice L. Rodriguez, Colleen M. Niswender, Jordan O’Neill, Katherine J. Watson, Sichen Chang, Anna L. Blobaum, Olivier Boutaud, Weimin Peng, Jerri M. Rook, P. Jeffrey Conn, Craig W. Lindsley and Kayla J. Temple*, 
{"title":"Discovery of Thieno[3,2-b]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5","authors":"Katherine E. Crocker*,&nbsp;Scott H. Henderson,&nbsp;Rory A. Capstick,&nbsp;David L. Whomble,&nbsp;Aaron M. Bender,&nbsp;Andrew S. Felts,&nbsp;Changho Han,&nbsp;Julie L. Engers,&nbsp;Natasha B. Billard,&nbsp;Mallory A. Maurer,&nbsp;Hyekyung P. Cho,&nbsp;Alice L. Rodriguez,&nbsp;Colleen M. Niswender,&nbsp;Jordan O’Neill,&nbsp;Katherine J. Watson,&nbsp;Sichen Chang,&nbsp;Anna L. Blobaum,&nbsp;Olivier Boutaud,&nbsp;Weimin Peng,&nbsp;Jerri M. Rook,&nbsp;P. Jeffrey Conn,&nbsp;Craig W. Lindsley and Kayla J. Temple*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0011910.1021/acsmedchemlett.5c00119","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00119https://doi.org/10.1021/acsmedchemlett.5c00119","url":null,"abstract":"<p >This Letter describes the discovery of novel mGlu<sub>5</sub> NAMs <b>VU6031545</b> and <b>VU6024945</b>. Starting from previously reported picolinamide compounds, a structure–activity relationship study of various core isosteres was conducted, leading to the identification of thieno[3,2-<i>b</i>]pyridine-5-carboxamide and 2,3-difluorobenzamide as competent core replacements. These compounds are highly potent as well as brain penetrant with an IVIVC agreement and improved oral bioavailability in rats.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"865–874 865–874"},"PeriodicalIF":3.5,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/epdf/10.1021/acsmedchemlett.5c00119","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917143","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Nonpeptide as Oxytocin Receptor Agonist. 新型非肽作为催产素受体激动剂。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00191
Yinlong Li, Steven H Liang
{"title":"Novel Nonpeptide as Oxytocin Receptor Agonist.","authors":"Yinlong Li, Steven H Liang","doi":"10.1021/acsmedchemlett.5c00191","DOIUrl":"10.1021/acsmedchemlett.5c00191","url":null,"abstract":"<p><p>This highlight describes a series of novel 1,4-benzodiazepine-based nonpeptides as oxytocin receptor (OT) agonists. The reported compounds demonstrate enhanced potency and selectivity compared to reference compounds, warranting further investigation for potential therapeutic applications in the treatment of OT-related pathologies.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"750-751"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067107/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143951741","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Pyrrolidinone Urea as FPR2 Agonists for Treating Atherosclerosis and Heart Failure 新型吡咯烷酮脲作为FPR2激动剂治疗动脉粥样硬化和心力衰竭
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 DOI: 10.1021/acsmedchemlett.5c0019610.1021/acsmedchemlett.5c00196
Ram W. Sabnis*, 
{"title":"Novel Pyrrolidinone Urea as FPR2 Agonists for Treating Atherosclerosis and Heart Failure","authors":"Ram W. Sabnis*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0019610.1021/acsmedchemlett.5c00196","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00196https://doi.org/10.1021/acsmedchemlett.5c00196","url":null,"abstract":"<p >Provided herein are novel pyrrolidinone urea as FPR2 agonists, pharmaceutical compositions, use of such compounds in treating atherosclerosis and heart failure, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"756–757 756–757"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917133","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 Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation. 新型磺胺衍生物作为Nav1.5钠通道阻滞剂治疗心房颤动。
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 eCollection Date: 2025-05-08 DOI: 10.1021/acsmedchemlett.5c00192
Siyan Feng, Steven H Liang
{"title":"Novel Sulfonamide Derivatives as Nav1.5 Sodium Channel Blockers for Treating Atrial Fibrillation.","authors":"Siyan Feng, Steven H Liang","doi":"10.1021/acsmedchemlett.5c00192","DOIUrl":"10.1021/acsmedchemlett.5c00192","url":null,"abstract":"<p><p>This highlight describes a novel class of sulfonamide-based Nav1.5 sodium channel blockers. These compounds preferentially inhibit Nav1.5 in atrial cardiomyocytes, extending the effective refractory period and preventing arrhythmic, rapid contraction of the atria. The novel Nav1.5 blockers possess the potential to treat Atrial Fibrillation without affecting the function of the rest of the heart.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"748-749"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12067141/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144007241","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders 新型四氢苯并[b]吡唑啉[3,4-e][1,4]二氮卓类化合物治疗自闭症谱系障碍的催产素受体激动剂
IF 3.5 3区 医学
ACS Medicinal Chemistry Letters Pub Date : 2025-04-21 DOI: 10.1021/acsmedchemlett.5c0019010.1021/acsmedchemlett.5c00190
Zhendong Song,  and , Steven H. Liang*, 
{"title":"Novel Tetrahydrobenzo[b]pyrazolo[3,4-e][1,4]diazepine Compounds as Oxytocin Receptor Agonists for Treating Autism Spectrum Disorders","authors":"Zhendong Song,&nbsp; and ,&nbsp;Steven H. Liang*,&nbsp;","doi":"10.1021/acsmedchemlett.5c0019010.1021/acsmedchemlett.5c00190","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00190https://doi.org/10.1021/acsmedchemlett.5c00190","url":null,"abstract":"<p >The present invention reveals a series of novel nonpeptidergic compounds as oxytocin receptor (OT-R) agonists. These agonists, featuring a tetrahydrobenzo[<i>b</i>]pyrazolo[3,4-<i>e</i>][1,4]diazepine scaffold, hold the therapeutic potential for the treatment of autism spectrum disorders.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 5","pages":"752–753 752–753"},"PeriodicalIF":3.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143917130","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
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