ACS Medicinal Chemistry Letters最新文献_第10页

Discovery of Novel Pyrimidine Derivatives as Human Pin1 Covalent Inhibitors

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-20 DOI: 10.1021/acsmedchemlett.4c0047710.1021/acsmedchemlett.4c00477

Meizhen Tian, Xiaoyu Wang, Guodong Tang, Guonan Cui, Jie Zhou, Jing Jin* and Bailing Xu*,

引用次数: 0

Discovery of Novel Pyrimidine Derivatives as Human Pin1 Covalent Inhibitors. 新型嘧啶衍生物作为人Pin1共价抑制剂的发现。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-20 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00477

Meizhen Tian, Xiaoyu Wang, Guodong Tang, Guonan Cui, Jie Zhou, Jing Jin, Bailing Xu

引用次数: 0

Novel Ergoline Compounds as 5-HT2A Agonists for Treating Mood Disorders Such as Depressive Disorders and Bipolar Disorders

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-20 DOI: 10.1021/acsmedchemlett.4c0059310.1021/acsmedchemlett.4c00593

Ram W. Sabnis*,

引用次数: 0

Re-evaluation of Cyclic Peptide Binding to Neurotensin Receptor 1 by Shifting the Peptide Register during Synthesis

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-19 DOI: 10.1021/acsmedchemlett.4c0054210.1021/acsmedchemlett.4c00542

Lazarus Andrew de Zhang, Mengjie Liu, Daniel J. Scott* and David K. Chalmers*,

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引用次数: 0

Re-evaluation of Cyclic Peptide Binding to Neurotensin Receptor 1 by Shifting the Peptide Register during Synthesis. 在合成过程中，通过改变肽区来重新评估环肽与神经紧张素受体1的结合。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-19 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00542

Lazarus Andrew de Zhang, Mengjie Liu, Daniel J Scott, David K Chalmers

引用次数: 0

Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach. 基于结构的新型TLR7/8激动剂有效载荷设计实现免疫调节偶联方法。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-19 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00463

Yam B Poudel, Julian C Lo, Derek J Norris, Matthew Cox, Liqi He, Walter L Johnson, Murugaiah A M Subbaiah, Santigopal Mondal, Soodamani Thangavel, Lakshumanan Subramani, Maheswara Reddy, Suraksha Jain, Dahlia R Weiss, Prasanna Sivaprakasam, David Critton, Dawn Mulligan, Chunshan Xie, Payal Dhar, Yvonne Li, Emanuela Sega, Sayumi Yamazoe, Ashvinikumar V Gavai, Arvind Mathur, Christoph W Zapf, Eugene P Chekler

引用次数: 0

Advances in Psychoactive Alkaloid Delivery, Ergoline Analogues, and Serotonin Receptor Modulation for Enhanced Therapeutic Outcomes. 精神活性生物碱递送、麦角碱类似物和血清素受体调节提高治疗效果的研究进展。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-18 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00586

Robert B Kargbo

引用次数: 0

Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-18 DOI: 10.1021/acsmedchemlett.4c0046310.1021/acsmedchemlett.4c00463

Yam B. Poudel, Julian C. Lo, Derek J. Norris, Matthew Cox, Liqi He, Walter L. Johnson, Murugaiah A. M. Subbaiah, Santigopal Mondal, Soodamani Thangavel, Lakshumanan Subramani, Maheswara Reddy, Suraksha Jain, Dahlia R. Weiss, Prasanna Sivaprakasam, David Critton, Dawn Mulligan, Chunshan Xie, Payal Dhar, Yvonne Li, Emanuela Sega, Sayumi Yamazoe, Ashvinikumar V. Gavai, Arvind Mathur, Christoph W. Zapf and Eugene P. Chekler*,

{"title":"Structure-Based Design of Novel TLR7/8 Agonist Payloads Enabling an Immunomodulatory Conjugate Approach","authors":"Yam B. Poudel, Julian C. Lo, Derek J. Norris, Matthew Cox, Liqi He, Walter L. Johnson, Murugaiah A. M. Subbaiah, Santigopal Mondal, Soodamani Thangavel, Lakshumanan Subramani, Maheswara Reddy, Suraksha Jain, Dahlia R. Weiss, Prasanna Sivaprakasam, David Critton, Dawn Mulligan, Chunshan Xie, Payal Dhar, Yvonne Li, Emanuela Sega, Sayumi Yamazoe, Ashvinikumar V. Gavai, Arvind Mathur, Christoph W. Zapf and Eugene P. Chekler*, ","doi":"10.1021/acsmedchemlett.4c0046310.1021/acsmedchemlett.4c00463","DOIUrl":"https://doi.org/10.1021/acsmedchemlett.4c00463https://doi.org/10.1021/acsmedchemlett.4c00463","url":null,"abstract":"Dual activation of the TLR7 and TLR8 pathways leads to the production of type I interferon and proinflammatory cytokines, resulting in efficient antigen presentation by dendritic cells to promote T-cell priming and antitumor immunity. We developed a novel series of TLR7/8 dual agonists with varying ratios of TLR7 and TLR8 activity for use as payloads for an antibody–drug conjugate approach. The agonist-induced production of several cytokines in human whole blood confirmed their functional activity. Structure–activity relationship studies guided by structure-based drug design are described.","PeriodicalId":20,"journal":{"name":"ACS Medicinal Chemistry Letters","volume":"16 1","pages":"80–88 80–88"},"PeriodicalIF":3.5,"publicationDate":"2024-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143085008","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

Targeted Therapeutics in Oncology and Neurology: Advances in Kinase Inhibition and Biomarkers for Brain Injury. 肿瘤和神经学的靶向治疗：脑损伤的激酶抑制和生物标志物研究进展。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-18 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00585

Robert B Kargbo

引用次数: 0

Advancements in Neurotechnology: Pioneering Brain Monitoring and Stimulation for Enhanced Treatment and Understanding. 神经技术的进步：开创性的大脑监测和刺激，以加强治疗和理解。

IF 3.5 3区医学

ACS Medicinal Chemistry Letters Pub Date : 2024-12-18 eCollection Date: 2025-01-09 DOI: 10.1021/acsmedchemlett.4c00584

Robert B Kargbo

引用次数: 0