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Investigating the C2 modulation of the imidazo[1,2-a]pyrazine-based hit compound CTN1122: synthesis, in vitro antileishmanial activity, cytotoxicity and casein kinase 1 inhibition.
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-17 DOI: 10.1002/cmdc.202400862
Lhana Tisseur, Sandrine Cojean, Khadidiatou Gassama, Cédric Logé, Fabrice Pagniez, Christian Cavé, Guillaume Bernadat, Philippe M Loiseau, Stéphane Bach, Jérôme Thiéfaine, Carine Picot, Christophe Tomasoni, Olivier Leclercq, Blandine Baratte, Thomas Robert, Patrice Le Pape, Najma Rachidi, Marc-Antoine Bazin, Pascal/ Marchand
{"title":"Investigating the C2 modulation of the imidazo[1,2-a]pyrazine-based hit compound CTN1122: synthesis, in vitro antileishmanial activity, cytotoxicity and casein kinase 1 inhibition.","authors":"Lhana Tisseur, Sandrine Cojean, Khadidiatou Gassama, Cédric Logé, Fabrice Pagniez, Christian Cavé, Guillaume Bernadat, Philippe M Loiseau, Stéphane Bach, Jérôme Thiéfaine, Carine Picot, Christophe Tomasoni, Olivier Leclercq, Blandine Baratte, Thomas Robert, Patrice Le Pape, Najma Rachidi, Marc-Antoine Bazin, Pascal/ Marchand","doi":"10.1002/cmdc.202400862","DOIUrl":"https://doi.org/10.1002/cmdc.202400862","url":null,"abstract":"<p><p>Our research group previously discovered CTN1122, an imidazo[1,2-a]pyrazine compound with promising antileishmanial activity against intramacrophage amastigotes of Leishmania major and L. donovani strains. CTN1122 effectively targets Leishmania casein kinase 1 (L-CK1.2) and exhibits a favorable safety profile. To further explore its chemical space, we developed a convergent strategy to modify the C2 position of the imidazo[1,2-a]pyrazine core using Suzuki-Miyaura coupling of the corresponding triflate intermediate. Among 15 newly synthesized analogs, seven derivatives featuring variously substituted phenyl rings at C2 demonstrated L-CK1.2 inhibition within micromolar to submicromolar ranges and antileishmanial activity in vitro with low cytotoxicity in macrophages. Compounds 7d and 7l were particularly potent, with IC50 values of 1.25 µM and 0.92 µM against L. major, and 1.44 µM and 2.34 µM against L. donovani, respectively. They showed IC50 L-CK1.2 = 0.3 μM and 0.57 µM with enhanced selectivity indices (SI = 3.8 and 1.6) over the human CK1ε ortholog. Additionally, four C2 analogs and two C5 isomers exhibited notable antiparasitic effects without strongly inhibiting L-CK1.2, indicating a possible alternative mechanism of action. Compound 7k displayed the highest general activity, with IC50 values of 0.31 µM on L. major and 0.27 µM on L. donovani, coupled with favorable selectivity indexes.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400862"},"PeriodicalIF":3.6,"publicationDate":"2024-12-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142833264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Diastereoselective Cascade Double Michael Addition to Access Bridged Coumarins, Oxindoles and Spirooxindoles: A Sustainable Strategy for Synthesis of Anticancer Molecules.
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-16 DOI: 10.1002/cmdc.202400946
Kiranmai Nayani, Shravani Battula, Haripriya Bhumannagari, S S S S Sudha Ambadipudi, Sai Balaji Andugulapati
{"title":"Diastereoselective Cascade Double Michael Addition to Access Bridged Coumarins, Oxindoles and Spirooxindoles: A Sustainable Strategy for Synthesis of Anticancer Molecules.","authors":"Kiranmai Nayani, Shravani Battula, Haripriya Bhumannagari, S S S S Sudha Ambadipudi, Sai Balaji Andugulapati","doi":"10.1002/cmdc.202400946","DOIUrl":"https://doi.org/10.1002/cmdc.202400946","url":null,"abstract":"<p><p>An efficient and concise synthesis of highly functionalized bridged coumarins has been developed through a diastereoselective double Michael addition reaction of p-quinols with various 4-hydroxy coumarins under catalyst-free conditions in H2O-DMSO (8:2). The method has been applied to oxindoles for the synthesis of a variety of bridged-oxindoles and bridged-spiroxindoles in presence of a DABCO base using H2O-EtOH (8:2) as solvent medium. The strategy is simple, highly atom economical as there is no by-product and environmentally benign (E-factor = 0.1-0.9). The synthesized compounds were screened against triple-negative breast cancers and found that bridged coumarin (3a) and oxindole (5d) compounds exhibit potent anti-cancer activity at 6.6 and 8.8 µM (IC50) concentrations respectively. Further analysis revealed that 3a and 5d caused elevated early and total apoptosis by arresting the MDA-MB-468 cells in G2/M phase of the cell cycle. Overall, our results demonstrate that bridged coumarin (3a) and oxindole (5d) compounds-based approach attenuates the cancer progression and may pave a path for the translational outcome.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400946"},"PeriodicalIF":3.6,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142833262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Synthesis of 1,2,3-Triazole-Methyl-Menadione Derivatives: Evaluation of Electrochemical and Antiparasitic Properties against two Blood-Dwelling Parasites.
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-16 DOI: 10.1002/cmdc.202400731
Baptiste Dupouy, Tanja Karpstein, Cécile Häberli, Monica Cal, Matthias Rottmann, Pascal Maeser, Jennifer Keiser, Mourad Elhabiri, Elisabeth Davioud-Charvet
{"title":"Synthesis of 1,2,3-Triazole-Methyl-Menadione Derivatives: Evaluation of Electrochemical and Antiparasitic Properties against two Blood-Dwelling Parasites.","authors":"Baptiste Dupouy, Tanja Karpstein, Cécile Häberli, Monica Cal, Matthias Rottmann, Pascal Maeser, Jennifer Keiser, Mourad Elhabiri, Elisabeth Davioud-Charvet","doi":"10.1002/cmdc.202400731","DOIUrl":"https://doi.org/10.1002/cmdc.202400731","url":null,"abstract":"<p><p>This study explores the synthesis and evaluation of novel 1,2,3-triazole-methyl-1,4-naphthoquinone hybrids, focusing on their electrochemical properties and antiparasitic efficacies against two human blood-dwelling parasites Plasmodium falciparum and Schistosoma mansoni. Using copper-catalyzed azide-alkyne cycloaddition (CuAAC), a well-established tool in click chemistry, two synthetic routes were assessed to develop a- and b-[triazole-methyl]-menadione derivatives. By optimizing the CuAAC reaction conditions, yields were significantly improved, reaching up to 94% for key intermediates and resulting in the formation of a library of approximately 30 compounds. Biological evaluation of the compounds in antiparasitic drug assays demonstrated notable antischistosomal potencies, while no significant activity was observed for the same series against P. falciparum parasites. Electrochemical and 'benzylic' oxidation studies confirmed that the active 'benzoyl' metabolite responsible for the antiplasmodial activity of plasmodione cannot be generated. These findings highlight the potential of triazole-linked menadione hybrids as promising early candidates for antischistosomal drug development, and provides insights into structure-activity relationships crucial for future therapeutic strategies.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400731"},"PeriodicalIF":3.6,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826827","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Insight into Stabilization of G-Quadruplex in c-MYC Region with Phenanthroimidazoisoindol-Acrylates and their Binding Behaviour towards Human Serum Albumin.
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-16 DOI: 10.1002/cmdc.202400705
Kamaldeep Paul, Rekha Thakur, Vijay Luxami
{"title":"Insight into Stabilization of G-Quadruplex in c-MYC Region with Phenanthroimidazoisoindol-Acrylates and their Binding Behaviour towards Human Serum Albumin.","authors":"Kamaldeep Paul, Rekha Thakur, Vijay Luxami","doi":"10.1002/cmdc.202400705","DOIUrl":"https://doi.org/10.1002/cmdc.202400705","url":null,"abstract":"<p><p>The interaction of G-quadruplex (non-canonical DNA) with suitable compounds for their stabilization at the promoter region of oncogenes has become a potential anticancer approach. We have studied the interaction of phenanthroimidazoisoindol-acrylates derivatives with c-MYC G-quadruplex. A series of 20 compounds were evaluated for their anticancer activity against human cancer cell lines, where compounds 3fa, 3ha, and 3ae have shown the broad-spectrum anticancer activities against most of the cancer cell lines and inactive towards normal cell lines. Various spectroscopic techniques have been used to study the interaction of these compounds. The studies reveal the strong binding of all three compounds with c-MYC G-quadruplex with significant selectivity over dsDNA, with binding constant of the order of 106 M-1. All three compounds bind effectively with HSA, which is a carrier protein, with binding constant of the order of 105 M-1. These results show that phenanthroimidazoisoindol-acrylate derivatives exhibit specificity towards G4 DNA, highlighting their potential as effective anticancer agents targeting the c-MYC G-quadruplex.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400705"},"PeriodicalIF":3.6,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142833263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Cover Feature: Phosphate-Containing Glycolipids: A Review on Synthesis and Bioactivity (ChemMedChem 24/2024)
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-16 DOI: 10.1002/cmdc.202482402
Luís Pinheiro, Marisa Freitas, Paula S. Branco
{"title":"Cover Feature: Phosphate-Containing Glycolipids: A Review on Synthesis and Bioactivity (ChemMedChem 24/2024)","authors":"Luís Pinheiro,&nbsp;Marisa Freitas,&nbsp;Paula S. Branco","doi":"10.1002/cmdc.202482402","DOIUrl":"https://doi.org/10.1002/cmdc.202482402","url":null,"abstract":"<p>Phosphate-containing Glycolipids are structures that are not as widely understood as glycolipids. They are divided into two classes: phosphoglycolipids and glycophospholipids – depending on the position of the phosphate. They are inspired by natural sources of various origins. Because of their lipidic portion they are often associated with biological membranes. Their bioactivities concern mainly anti-metastasis, platelet aggregation, inflammatory, antifungal, antibiotic and neurogenic activities. More details can be found in article 10.1002/cmdc.202400315 by Luís Pinheiro and co-workers. \u0000 <figure>\u0000 <div><picture>\u0000 <source></source></picture><p></p>\u0000 </div>\u0000 </figure>\u0000 </p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"19 24","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202482402","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142861129","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
Front Cover: Cholinesterase Inhibitory Activity and Molecular Docking Studies of Isocryptolepine-Triazole Adducts (ChemMedChem 24/2024)
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-16 DOI: 10.1002/cmdc.202482401
Jumreang Tummatorn, Ittipat Meewan, Nisachon Khunnawutmanotham, Nitirat Chimnoi, Nutchapong Suwanwong, Warabhorn Rodphon, Charnsak Thongsornkleeb, Jingyue Yang, Somsak Ruchirawat
{"title":"Front Cover: Cholinesterase Inhibitory Activity and Molecular Docking Studies of Isocryptolepine-Triazole Adducts (ChemMedChem 24/2024)","authors":"Jumreang Tummatorn,&nbsp;Ittipat Meewan,&nbsp;Nisachon Khunnawutmanotham,&nbsp;Nitirat Chimnoi,&nbsp;Nutchapong Suwanwong,&nbsp;Warabhorn Rodphon,&nbsp;Charnsak Thongsornkleeb,&nbsp;Jingyue Yang,&nbsp;Somsak Ruchirawat","doi":"10.1002/cmdc.202482401","DOIUrl":"https://doi.org/10.1002/cmdc.202482401","url":null,"abstract":"<p>This illustration depicts the molecular interactions of isocryptolepine-triazole hybrids with Acetylcholinesterase (AChE) in the brain related to Alzheimer′s disease. Central to the image is AChE, an enzyme involved in neurotransmitter regulation. Surrounding AChE are potential new compounds designed to inhibit its activity, thereby enhancing cholinergic signaling and potentially alleviating symptoms of Alzheimer′s. The visual emphasizes the innovative research aimed at developing effective therapeutics for this progressive neurodegenerative disorder. More details can be found in article 10.1002/cmdc.202400447 by Jumreang Tummatorn, Nutchapong Suwanwong, and co-workers.<figure>\u0000 <div><picture>\u0000 <source></source></picture><p></p>\u0000 </div>\u0000 </figure>\u0000 </p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":"19 24","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/cmdc.202482401","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142861116","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
The Evaluation of Glyceryl C3-Azolyl-Thiogalactosides as Galectin-1 and Galectin-3 Ligands. 评估甘油 C3-叠氮基硫代半乳糖苷作为 Galectin-1 和 Galectin-3 配体的作用。
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-14 DOI: 10.1002/cmdc.202400826
Vít Prouza, Jakub Zýka, Jaroslav Kozák, Alžbeta Magdolenová, Radek Pohl, Kamil Parkan
{"title":"The Evaluation of Glyceryl C3-Azolyl-Thiogalactosides as Galectin-1 and Galectin-3 Ligands.","authors":"Vít Prouza, Jakub Zýka, Jaroslav Kozák, Alžbeta Magdolenová, Radek Pohl, Kamil Parkan","doi":"10.1002/cmdc.202400826","DOIUrl":"https://doi.org/10.1002/cmdc.202400826","url":null,"abstract":"<p><p>Galectins are a family of galactoside-binding proteins involved in various pathophysiological processes, which makes them attractive targets for drug discovery. The derivatization of d-galactose at C3 and C1 positions has been shown to increase the affinity of synthetic galectin antagonists. In this study, two small libraries of d-galactose derivatives have been designed and synthesized. The first series involved the development of novel aromatic 3-azolyl-3-deoxy-d-galactopyranoses. The second series consisted of epimeric analogs of glyceryl β-S-d-galactopyranosides, which were also derivatized. Binding-affinity evaluations for galectin-1 and galectin-3 have revealed that galactose analogs from both series have potential for further optimization. Notably, a combination of modifications at the C3 position of the galactose ring and on the aglycone has led to the identification of promising galectin inhibitors, specifically the compounds 29R and 32S.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400826"},"PeriodicalIF":3.6,"publicationDate":"2024-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142823454","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
A Yeast-Based Assay for Inhibitors of l-Lactate Transport Utilizing Fluorescent Biosensors. 基于酵母的利用荧光生物传感器检测乳酸转运抑制剂的方法
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-13 DOI: 10.1002/cmdc.202400918
Finn Tiedjens, Maike Menzel, Pauline Stahnke, Hanna Grotewold, Cane Uzun, Derya Yildirim, Eric Beitz
{"title":"A Yeast-Based Assay for Inhibitors of l-Lactate Transport Utilizing Fluorescent Biosensors.","authors":"Finn Tiedjens, Maike Menzel, Pauline Stahnke, Hanna Grotewold, Cane Uzun, Derya Yildirim, Eric Beitz","doi":"10.1002/cmdc.202400918","DOIUrl":"https://doi.org/10.1002/cmdc.202400918","url":null,"abstract":"<p><p>Inhibitors of ʟ-lactate transport are in development as a novel mode of action in antitumor therapy and malaria. Previously, we used radiolabeled ʟ-lactate to assay transport via the human monocarboxylate transporter 1, MCT1, and the structurally unrelated malaria parasite's transporter, PfFNT. We encountered a sensitivity limit at IC50 around 100 nM possibly resulting from the required high cell number per sample. Here, we describe a sensitive background-free high-throughput assay in yeast based on fluorescent iLACCO biosensors. We used iLACCO for co-expression and fusions with the transporter protein. Uptake of ʟ-lactate produced strong intensiometric fluorescent responses that could be monitored in cell suspensions using a fluorometer and in individual cells by fluorescence microscopy. The signal decreased dose-dependently in the presence of specific MCT1 and PfFNT inhibitors. Re-evaluation of 36 PfFNT inhibitors yielded IC50 values below 100 nM now matching previous data on Ki compound affinity to isolated transporter protein.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400918"},"PeriodicalIF":3.6,"publicationDate":"2024-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821533","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Synthesis of New Enantiopure Aminoalcohol Fluorenes as Promising Antimalarial Compounds. 合成新的不反纯氨基醇芴作为有前途的抗疟化合物。
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-13 DOI: 10.1002/cmdc.202400790
Camille Tisnerat, Jérémy Schneider, Romain Mustière, Aurélie Herrero, René Momha, Céline Damiani, Patrice Agnamey, Anne Totet, Mathieu Marchivie, Jean Guillon, Alexandra Dassonville-Klimpt, Pascal Sonnet
{"title":"Synthesis of New Enantiopure Aminoalcohol Fluorenes as Promising Antimalarial Compounds.","authors":"Camille Tisnerat, Jérémy Schneider, Romain Mustière, Aurélie Herrero, René Momha, Céline Damiani, Patrice Agnamey, Anne Totet, Mathieu Marchivie, Jean Guillon, Alexandra Dassonville-Klimpt, Pascal Sonnet","doi":"10.1002/cmdc.202400790","DOIUrl":"https://doi.org/10.1002/cmdc.202400790","url":null,"abstract":"<p><p>Herein, we report the design, synthesis, and characterisation of a new library of enantiopure aminoalcohol fluorenes, as well as their in vitro evaluation for biological properties, including activity against two strains of P. falciparum (3D7 and W2) and cytotoxicity on the HepG2 cell line. All tested compounds exhibited good to excellent antimalarial potency with IC50 values ranging from 0.7 to 70.2 nM whatever the strain. Interestingly, most compounds showed equal or better antimalarial activity compared to the reference drugs lumefantrine, mefloquine and chloroquine. Despite moderate cytotoxicity in the micromolar range, all aminoalcohol fluorenes displayed an excellent selectivity index higher than 100 due to strong antimalarial activity. Furthermore, we report in silico analyses of physicochemical and pharmacokinetic properties for all compounds, highlighting the drug-likeness of compound 10 and its promising potential for further studies.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400790"},"PeriodicalIF":3.6,"publicationDate":"2024-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142816848","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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
Autophagy-mediated targeted protein degradation.
IF 3.6 4区 医学
ChemMedChem Pub Date : 2024-12-13 DOI: 10.1002/cmdc.202400866
Jinning Shao, Shangzhi Xie, Shurui Hong, Linghui Qian
{"title":"Autophagy-mediated targeted protein degradation.","authors":"Jinning Shao, Shangzhi Xie, Shurui Hong, Linghui Qian","doi":"10.1002/cmdc.202400866","DOIUrl":"https://doi.org/10.1002/cmdc.202400866","url":null,"abstract":"<p><p>Autophagy is an evolutionarily conserved turnover process in eukaryotes, mediating the delivery of various cellular components to lysosomes for degradation and facilitating the recycle of the breakdown products to maintain the homeostasis. By harnessing this powerful autophagy-lysosomal degradation system, strategies for targeted protein degradation (TPD) have been emerging to remove specific disease-related proteins (both intracellular and cell-surface proteins) for complete elimination of their functions, bringing new insights to drug discovery. Herein, we give a brief introduction on how autophagy works followed by a focus on available small-molecule and macromolecule-based strategies for TPD mediated by autophagy.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400866"},"PeriodicalIF":3.6,"publicationDate":"2024-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821534","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"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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