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An overview of pyridazin-3(2H)-one: a core for developing bioactive agents targeting cardiovascular diseases and cancer. 哒嗪-3(2H)-酮概述：开发针对心血管疾病和癌症的生物活性制剂的核心。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-08-06 DOI: 10.1080/17568919.2024.2379234
Zeinab S Abd-Rabo, Aya M Serry, Riham F George
{"title":"An overview of pyridazin-3(2<i>H</i>)-one: a core for developing bioactive agents targeting cardiovascular diseases and cancer.","authors":"Zeinab S Abd-Rabo, Aya M Serry, Riham F George","doi":"10.1080/17568919.2024.2379234","DOIUrl":"10.1080/17568919.2024.2379234","url":null,"abstract":"<p><p>Cardiovascular diseases (CVDs) and cancer are the top two leading causes of death globally. Vasodilators are commonly used to treat various CVDs. In cancer treatment, targeted anticancer agents have been developed to minimize side effects compared with traditional chemotherapy. Many hypertension patients are more prone to cancer, a case known as reverse cardio-oncology. This leads to the search for drugs with dual activity or repurposing strategy to discover new therapeutic uses for known drugs. Recently, medicinal chemists have shown great interest in synthesizing pyridazinone derivatives due to their significant biological activities in tackling these critical health challenges. This review will concentrate on pyridazin-3(2<i>H</i>)-one-containing compounds as vasodilators and anticancer agents, along with a brief overview of various methods for their synthesis.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1685-1703"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370926/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141893305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
In vitro anti-breast cancer study of hybrid cinnamic acid derivatives bearing 2-thiohydantoin moiety. 含有 2-硫代海因分子的混合肉桂酸衍生物的体外抗乳腺癌研究。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-07-01 DOI: 10.1080/17568919.2024.2366694
Dalal Nasser Binjawhar, Fawziah A Al-Salmi, Maha Ali Alghamdi, Ola A Abu Ali, Eman Fayad, Youstina William Rizzk, Nourhan M Ali, Ibrahim Mohey El-Deen, Elsayed H Eltamany
{"title":"<i>In vitro</i> anti-breast cancer study of hybrid cinnamic acid derivatives bearing 2-thiohydantoin moiety.","authors":"Dalal Nasser Binjawhar, Fawziah A Al-Salmi, Maha Ali Alghamdi, Ola A Abu Ali, Eman Fayad, Youstina William Rizzk, Nourhan M Ali, Ibrahim Mohey El-Deen, Elsayed H Eltamany","doi":"10.1080/17568919.2024.2366694","DOIUrl":"10.1080/17568919.2024.2366694","url":null,"abstract":"<p><p><b>Aim</b>: To synthesize new hybrid cinnamic acids (<b>10a</b>, <b>10b</b> and <b>11</b>) and ester derivatives (<b>7</b>, <b>8</b> and <b>9</b>) and investigate their anti-breast cancer activities.<b>Materials & methods:</b> Compounds <b>7-11</b> were evaluated (<i>in vitro</i>) for their cytotoxic activities against the MCF-7 cell line. A flow cytometry examination was performed. Protein levels of nuclear factor erythroid 2-related factor 2 (Nrf2), topoisomerase II and caspase-9 were measured by qRT-PCR. Molecular docking studies were conducted.<b>Results</b>: Several components were discovered to be active, mainly component <b>11</b>, which induced arrest in the cell cycle at phase S, greatly decreased the expression of Nrf2 and topoisomerase II; and upregulated the expression of caspase-9.<b>Conclusion:</b> The newly thiohydantoin-cinnamic acid hybrids can contribute to creating promising candidates for cancer drugs.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1665-1684"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370905/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467402","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Identification of novel benzothiazole-thiadiazole-based thiazolidinone derivative: in vitro and in silico approaches to develop promising anti-Alzheimer's agents. 鉴定新型苯并噻唑-噻二唑基噻唑烷酮衍生物：开发有前景的抗阿尔茨海默氏症药物的体外和硅学方法。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-06-28 DOI: 10.1080/17568919.2024.2366159
Shoaib Khan, Rafaqat Hussain, Tayyiaba Iqbal, Yousaf Khan, Urooj Jamal, Hany W Darwish, Muhammad Adnan
{"title":"Identification of novel benzothiazole-thiadiazole-based thiazolidinone derivative: <i>in vitro</i> and <i>in silico</i> approaches to develop promising anti-Alzheimer's agents.","authors":"Shoaib Khan, Rafaqat Hussain, Tayyiaba Iqbal, Yousaf Khan, Urooj Jamal, Hany W Darwish, Muhammad Adnan","doi":"10.1080/17568919.2024.2366159","DOIUrl":"10.1080/17568919.2024.2366159","url":null,"abstract":"<p><p><b>Aim:</b> The present study describes benzothiazole derived thiazolidinone based thiadiazole derivatives (<b>1-16</b>) as anti-Alzheimer agents.<b>Materials & methods:</b> Synthesis of benzothiazole derived thiazolidinone based thiadiazole derivatives was achieved using the benzothiazole bearing 2-amine moiety. These synthesized compounds were confirmed via spectroscopic techniques (<sup>1</sup>H NMR, <sup>13</sup>C NMR and HREI-MS). These compounds were biologically evaluated for their anti-Alzheimer potential. Binding interactions with proteins and drug likeness of the analogs were explored through molecular docking and ADMET analysis, respectively. In the novel series, compound-<b>3</b> emerged as the most potent inhibitor when compared with other derivatives of the series.<b>Conclusion:</b> The present study provides potent anti-Alzheimer's agents that can be further optimized to discover novel anti-Alzheimer's drugs.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1601-1613"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370920/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467404","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Barbiturate-sulfonate hybrids as potent cholinesterase inhibitors: design, synthesis and molecular modeling studies. 作为强效胆碱酯酶抑制剂的巴比妥酸-磺酸盐杂化物：设计、合成和分子模型研究。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-07-16 DOI: 10.1080/17568919.2024.2366158
Asmaa F Kassem, Mohamed A Omar, Ahmed Temirak, Riham A El-Shiekh, Aladdin M Srour
{"title":"Barbiturate-sulfonate hybrids as potent cholinesterase inhibitors: design, synthesis and molecular modeling studies.","authors":"Asmaa F Kassem, Mohamed A Omar, Ahmed Temirak, Riham A El-Shiekh, Aladdin M Srour","doi":"10.1080/17568919.2024.2366158","DOIUrl":"10.1080/17568919.2024.2366158","url":null,"abstract":"<p><p><b>Aim:</b> Design and synthesis of a series of 5-benzylidene(thio)barbiturates <b>3a-r</b>.<b>Methodology:</b> Evaluation of the inhibitory activity of the new chemical entities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using Donepezil as the standard reference.<b>Results & Conclusion:</b> Compound <b>3r</b> emerged as the most potent AChE inhibitor (IC<sub>50</sub> = 9.12 μM), while compound <b>3q</b> exhibited the highest inhibitory activity against BChE (IC<sub>50</sub> = 19.43 μM). Toxicological bioassays confirmed the absence of cytotoxicity for the most potent compounds at the tested doses. Molecular docking analysis demonstrated that the tested derivatives effectively bind to the active sites of both enzymes. Overall, this study sheds light on the potential of barbiturate-sulfonate conjugates as promising drug candidates.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1615-1631"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370902/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141619704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Medicinal chemistry aspects of fat mass and obesity associated protein: structure, function and inhibitors. 脂肪量和肥胖相关蛋白的药物化学方面：结构、功能和抑制剂。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-17 Epub Date: 2024-08-05 DOI: 10.1080/17568919.2024.2380245
Changyu Ren, Zhi Cao, Yang Liu, Rui Wang, Congcong Lin, Zishu Wang
{"title":"Medicinal chemistry aspects of fat mass and obesity associated protein: structure, function and inhibitors.","authors":"Changyu Ren, Zhi Cao, Yang Liu, Rui Wang, Congcong Lin, Zishu Wang","doi":"10.1080/17568919.2024.2380245","DOIUrl":"10.1080/17568919.2024.2380245","url":null,"abstract":"<p><p>Adiposity and obesity-related proteins (FTO), the earliest identified mRNA <i>N</i><sup>6</sup>-methyladenosine (m<sup>6</sup>A) demethylases, are known to play crucial roles in several biological processes. Therefore, FTO is a promising target for anticancer treatment. Understanding the biological functions and regulatory mechanisms of FTO targets can serve as guidelines for drug development. Despite significant efforts to develop FTO inhibitors, no specific small-molecule inhibitors have entered clinical trials so far. In this manuscript, we review the relationship between FTO and various cancers, the small-molecule inhibitors developed against FTO targets from the perspective of medicinal chemistry and other fields, and describe their structural optimization process and structure-activity relationship, providing clues for their future development direction.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1705-1726"},"PeriodicalIF":3.2,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370915/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141888966","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents. 硫脲官能化氨基丁亚胺衍生物作为抗利什曼病药。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-02 Epub Date: 2024-07-02 DOI: 10.1080/17568919.2024.2359362
Muhammad Sajid, Hina Siddiqui, Humaira Zafar, Sammer Yousuf, Michael D Threadgill, Muhammad Iqbal Choudhary
{"title":"Thiourea-functionalized aminoglutethimide derivatives as anti-leishmanial agents.","authors":"Muhammad Sajid, Hina Siddiqui, Humaira Zafar, Sammer Yousuf, Michael D Threadgill, Muhammad Iqbal Choudhary","doi":"10.1080/17568919.2024.2359362","DOIUrl":"10.1080/17568919.2024.2359362","url":null,"abstract":"<p><p><b>Aim:</b> We aim to develop new anti-leishmanial agents against <i>Leishmania major</i> and <i>Leishmania tropica</i>.<b>Materials & methods:</b> A total of 23 thiourea derivatives of (±)-aminoglutethimide were synthesized and evaluated for <i>in vitro</i> activity against promastigotes of <i>L. major</i> and <i>L. tropica</i>.<b>Results & conclusion:</b> The <i>N</i>-benzoyl analogue <b>7p</b> was found potent (IC<sub>50</sub> = 12.7 μM) against <i>L. major</i> and non toxic to normal cells. The docking studies, indicates that these inhibitors may target folate and glycolytic pathways of the parasite. The <i>N</i>-hexyl compound <b>7v</b> was found strongly active against both species, and lacked cytotoxicity against normal cells, whereas compound <b>7r</b>, with a 3,5-bis-(tri-fluoro-methyl)phenyl unit, was active against <i>Leishmania</i>, but was cytotoxic in nature. Compound <b>7v</b> was thus identified as a hit for further studies.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1485-1497"},"PeriodicalIF":3.2,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370960/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141491535","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Synthesis of novel hybrids of 1,2,3-triazoles-hydrazone: targeting cholinesterases and Alzheimer's related genes. 合成新型 1,2,3-三唑-腙混合物：靶向胆碱酯酶和阿尔茨海默氏症相关基因。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-02 Epub Date: 2024-06-12 DOI: 10.1080/17568919.2024.2359894
Diba Shareghi-Boroujeni, Aida Iraji, Mahintaj Dara, Mohammad Hashem Hashempur, Shahrokh Zare, Roshanak Hariri, Tahmineh Akbarzadeh, Mina Saeedi
{"title":"Synthesis of novel hybrids of 1,2,3-triazoles-hydrazone: targeting cholinesterases and Alzheimer's related genes.","authors":"Diba Shareghi-Boroujeni, Aida Iraji, Mahintaj Dara, Mohammad Hashem Hashempur, Shahrokh Zare, Roshanak Hariri, Tahmineh Akbarzadeh, Mina Saeedi","doi":"10.1080/17568919.2024.2359894","DOIUrl":"10.1080/17568919.2024.2359894","url":null,"abstract":"<p><p><b>Aim:</b> A new series of 1,2,3-triazole-hydrazone derivatives were developed to evaluate their anti-Alzheimer's activity. <b>Materials & methods:</b> All compounds were screened toward cholinesterases via the modified Ellman's method. The toxicity assay on SH-SY5Y cells was performed using the MTT assay, and the expression levels of <i>GSK-3α</i>, <i>GSK-3β</i>, <i>DYRK1</i> and <i>CDK5</i> were assessed in the presence of compounds <b>6m</b> and <b>6p</b>.<b>Results:6m</b> and <b>6p</b>; acting as mixed-type inhibitors, exhibited promising acetylcholinesterase and butyrylcholinesterase inhibitory activity, respectively. <b>6m</b> demonstrated no toxicity under tested concentrations on the SH-SY5Y cells and positively impacted neurodegenerative pathways. Notably, <b>6m</b> displayed a significant downregulation in mRNA levels of <i>GSK-3α</i>, <i>GSK-3β</i> and <i>CDK5</i>.<b>Conclusion:</b> The target compounds could be considered in developing anti-Alzheimer's disease agents.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1519-1535"},"PeriodicalIF":3.2,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370907/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141305754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
NMR analysis, cytotoxic activity and theoretical study of a complex between SRPIN340 and p-sulfonic acid calix[6]arene. SRPIN340 与对磺酸钙[6]炔复合物的核磁共振分析、细胞毒性活性和理论研究。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-02 Epub Date: 2024-07-01 DOI: 10.1080/17568919.2024.2366690
Lívia Cristina de Souza Viol, Natália Aparecida Liberto Silva, Cristiane Isaac Cerceau, Marcus Vinícius de Andrade Barros, Raoni Pais Siqueira, Victor Hugo Sousa Gonçalves, Gustavo Costa Bressan, Sergio Antonio Fernandes, Elson Santiago Alvarenga, Róbson Ricardo Teixeira
{"title":"NMR analysis, cytotoxic activity and theoretical study of a complex between SRPIN340 and <i>p</i>-sulfonic acid calix[6]arene.","authors":"Lívia Cristina de Souza Viol, Natália Aparecida Liberto Silva, Cristiane Isaac Cerceau, Marcus Vinícius de Andrade Barros, Raoni Pais Siqueira, Victor Hugo Sousa Gonçalves, Gustavo Costa Bressan, Sergio Antonio Fernandes, Elson Santiago Alvarenga, Róbson Ricardo Teixeira","doi":"10.1080/17568919.2024.2366690","DOIUrl":"10.1080/17568919.2024.2366690","url":null,"abstract":"<p><p><b>Aim:</b> This study aimed to enhance the aqueous dissolution of SRPK inhibitor <i>N</i>-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide (SRPIN340).<b>Materials & Methods:</b> A complex with <i>p</i>-sulfonic calix[6]arene (Host) and SRPIN340 (Guest) was prepared, studied via <sup>1</sup>H nuclear magnetic resonance (NMR) and theoretical calculations and biologically evaluated on cancer cell lines.<b>Results & conclusion:</b> The 1:1 host (H)/guest (G) complex significantly enhanced the aqueous dissolution of SRPIN340, achieving 64.8% water solubility as determined by <sup>1</sup>H NMR quantification analysis. The H/G complex reduced cell viability by 75% for HL60, ∼50% for Nalm6 and Jurkat, and ∼30% for B16F10 cells. It exhibited greater cytotoxicity than free SRPIN340 against Jurkat and B16F10 cells. Theoretical studies indicated hydrogen bond stabilization of the complex, suggesting broader applicability of SRPIN340 across diverse biological systems.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1537-1550"},"PeriodicalIF":3.2,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370924/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467405","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
A novel chromone-based as a potential inhibitor of ULK1 that modulates autophagy and induces apoptosis in colon cancer. 一种基于色酮的新型 ULK1 潜在抑制剂，可调节自噬并诱导结肠癌细胞凋亡。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-02 Epub Date: 2024-07-01 DOI: 10.1080/17568919.2024.2363668
Nur Farisya Shamsudin, Sze-Wei Leong, Andreas Koeberle, Utid Suriya, Thanyada Rungrotmongkol, Suet Lin Chia, Muhammad Taher, Muhammad Salahuddin Haris, Hussah Abdullah Alshwyeh, Areej A Alosaimi, Ahmed Mediani, Muna Abdulsalam Ilowefah, Deri Islami, Siti Munirah Mohd Faudzi, Mohd Fadhlizil Fasihi Mohd Aluwi, Lam Kok Wai, Kamal Rullah
{"title":"A novel chromone-based as a potential inhibitor of ULK1 that modulates autophagy and induces apoptosis in colon cancer.","authors":"Nur Farisya Shamsudin, Sze-Wei Leong, Andreas Koeberle, Utid Suriya, Thanyada Rungrotmongkol, Suet Lin Chia, Muhammad Taher, Muhammad Salahuddin Haris, Hussah Abdullah Alshwyeh, Areej A Alosaimi, Ahmed Mediani, Muna Abdulsalam Ilowefah, Deri Islami, Siti Munirah Mohd Faudzi, Mohd Fadhlizil Fasihi Mohd Aluwi, Lam Kok Wai, Kamal Rullah","doi":"10.1080/17568919.2024.2363668","DOIUrl":"10.1080/17568919.2024.2363668","url":null,"abstract":"<p><p><b>Aim:</b> Chromones are promising for anticancer drug development.<b>Methods & results:</b> 12 chromone-based compounds were synthesized and tested against cancer cell lines. Compound <b>8</b> showed the highest cytotoxicity (LC<sub>50</sub> 3.2 μM) against colorectal cancer cells, surpassing 5-fluorouracil (LC<sub>50</sub> 4.2 μM). It suppressed colony formation, induced cell cycle arrest and triggered apoptotic cell death, confirmed by staining and apoptosis markers. Cell death was accompanied by enhanced reactive oxygen species formation and modulation of the autophagic machinery (autophagy marker light chain 3B (LC3B); adenosine monophosphate-activated protein kinase (AMPK); protein kinase B (PKB); UNC-51-like kinase (ULK)-1; and ULK2). Molecular docking and dynamic simulations revealed that compound <b>8</b> directly binds to ULK1.<b>Conclusion:</b> Compound <b>8</b> is a promising lead for autophagy-modulating anti-colon cancer drugs.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1499-1517"},"PeriodicalIF":3.2,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370956/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467403","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Regulation of post-translational modification of PD-L1 and associated opportunities for novel small-molecule therapeutics. PD-L1 翻译后修饰的调控及新型小分子疗法的相关机遇。
IF 3.2 4区 医学
Future medicinal chemistry Pub Date : 2024-08-02 Epub Date: 2024-07-01 DOI: 10.1080/17568919.2024.2366146
Jinglin Tang, Han Liu, Jinze Li, Yibo Zhang, Suyang Yao, Kan Yang, Zhihao You, Xiaoqiang Qiao, Yali Song
{"title":"Regulation of post-translational modification of PD-L1 and associated opportunities for novel small-molecule therapeutics.","authors":"Jinglin Tang, Han Liu, Jinze Li, Yibo Zhang, Suyang Yao, Kan Yang, Zhihao You, Xiaoqiang Qiao, Yali Song","doi":"10.1080/17568919.2024.2366146","DOIUrl":"10.1080/17568919.2024.2366146","url":null,"abstract":"<p><p>PD-L1 is overexpressed on the surface of tumor cells and binds to PD-1, resulting in tumor immune escape. Therapeutic strategies to target the PD-1/PD-L1 pathway involve blocking the binding. Immune checkpoint inhibitors have limited efficacy against tumors because PD-L1 is also present in the cytoplasm. PD-L1 of post-translational modifications (PTMs) have uncovered numerous mechanisms contributing to carcinogenesis and have identified potential therapeutic targets. Therefore, small molecule inhibitors can block crucial carcinogenic signaling pathways, making them a potential therapeutic option. To better develop small molecule inhibitors, we have summarized the PTMs of PD-L1. This review discusses the regulatory mechanisms of small molecule inhibitors in carcinogenesis and explore their potential applications, proposing a novel approach for tumor immunotherapy based on PD-L1 PTM.</p>","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1583-1599"},"PeriodicalIF":3.2,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11370925/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141467406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
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