Ryan A. Bragg*, Jonas Bergare, Markus Artelsmair, William J. Kerr, Troels Skrydstrup and Charles S. Elmore*,
{"title":"","authors":"Ryan A. Bragg*, Jonas Bergare, Markus Artelsmair, William J. Kerr, Troels Skrydstrup and Charles S. Elmore*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 7","pages":"XXX-XXX 12260–12268"},"PeriodicalIF":3.5,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.5c00338","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144587258","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}
{"title":"Novel Indole Derivatives as Serotonergic Psychedelic Agents for Treating Psychosis, Mental Illness, and CNS Disorders.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00380","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00380","url":null,"abstract":"<p><p>Provided herein are novel indole derivatives as serotonergic psychedelic agents, pharmaceutical compositions, use of such compounds in treating psychosis, mental illness and central nervous system (CNS) disorders, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 7","pages":"1270-1271"},"PeriodicalIF":3.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12257407/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144641215","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}
Nobuki Kazuta, Kazuma Nakashima, Hiroyuki Watanabe, Masahiro Ono
{"title":"Development of Novel Integrin α<sub>v</sub>β<sub>3</sub>‑Targeted Radioligand for Enhanced Tumor Accumulation.","authors":"Nobuki Kazuta, Kazuma Nakashima, Hiroyuki Watanabe, Masahiro Ono","doi":"10.1021/acsmedchemlett.5c00231","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00231","url":null,"abstract":"<p><p>Effective tumor delivery of radioligands is crucial for cancer diagnosis and therapy. Integrin α<sub>v</sub>β<sub>3</sub> is an attractive target for cancer treatment, and the development of integrin α<sub>v</sub>β<sub>3</sub>-targeted radioligands with high-level tumor accumulation is desired. Albumin binder (ALB) is a useful moiety to enhance tumor accumulation of radioligands. Furthermore, the introduction of dual amino acid linkers to an ALB-containing prostate-specific membrane antigen-targeted radioligand enhances the tumor accumulation by increasing its albumin-binding affinity. In this study, we newly developed two integrin α<sub>v</sub>β<sub>3</sub>-targeted radioligands: one containing both dual amino acid linkers and ALB ([<sup>111</sup>In]-In-RGD-DA6) and another containing only ALB ([<sup>111</sup>In]-In-RGD-DA1). In albumin-binding assays, [<sup>111</sup>In]-In-RGD-DA6 showed higher albumin-binding affinity than [<sup>111</sup>In]-In-RGD-DA1 and [<sup>111</sup>In]-In-DOTA-c-(RGDfK), a counterpart without dual amino acid linkers and ALB. In biodistribution studies, [<sup>111</sup>In]-In-RGD-DA6 also showed higher tumor accumulation than [<sup>111</sup>In]-In-RGD-DA1 and [<sup>111</sup>In]-In-DOTA-c-(RGDfK). These results highlight the potential of [<sup>111</sup>In]-In-RGD-DA6 as an integrin α<sub>v</sub>β<sub>3</sub>-targeted radioligand with enhanced tumor accumulation.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 7","pages":"1346-1353"},"PeriodicalIF":3.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12257415/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144641195","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}
{"title":"Novel Heterocyclic Compounds as SMN2 Modulators for Treating Spinal Muscular Atrophy Via Modulation of SMN2 Splicing.","authors":"Ram W Sabnis","doi":"10.1021/acsmedchemlett.5c00364","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00364","url":null,"abstract":"<p><p>Provided herein are novel heterocyclic compounds as SMN2 modulators, pharmaceutical compositions, use of such compounds in treating spinal muscular atrophy (SMA) via modulation of SMN2 splicing, and processes for preparing such compounds.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 7","pages":"1262-1263"},"PeriodicalIF":3.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12257372/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144641212","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}
{"title":"The Importance of Correct New Drug Designations: New \"Novel Drug Entity\" Designations.","authors":"Sarah K Branch, Israel Agranat","doi":"10.1021/acsmedchemlett.5c00320","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.5c00320","url":null,"abstract":"<p><p>The Viewpoint addresses designations of novel drugs. The regulatory designation of new drugs is significant as it may confer exclusivity. The terminology for nonbiological drugs in the US is described. The Viewpoint recommends for approved novel drug compilations: novel molecular entity (nonbiological drug), novel biological entity, novel therapeutic entity for both designations.</p>","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 7","pages":"1217-1220"},"PeriodicalIF":3.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12257418/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144641227","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}