Expert Opinion on Therapeutic Patents最新文献_第6页

Lysine demethylase (KDM) inhibitors for the treatment of cancer: a patent review (2015-present). 用于治疗癌症的赖氨酸去甲基化酶（KDM）抑制剂：专利审查（2015-至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-01-01 Epub Date: 2025-12-11 DOI: 10.1080/13543776.2025.2600945

Federica Sarno, Mariarosaria Conte, Annamaria Muro, Carmela Dell'Aversana, Giulia Sgueglia, Vincenzo Carafa, Nunzio Del Gaudio, Angela Nebbioso, Lucia Altucci

{"title":"Lysine demethylase (KDM) inhibitors for the treatment of cancer: a patent review (2015-present).","authors":"Federica Sarno, Mariarosaria Conte, Annamaria Muro, Carmela Dell'Aversana, Giulia Sgueglia, Vincenzo Carafa, Nunzio Del Gaudio, Angela Nebbioso, Lucia Altucci","doi":"10.1080/13543776.2025.2600945","DOIUrl":"10.1080/13543776.2025.2600945","url":null,"abstract":"Introduction: Lysine demethylases (KDMs) are crucial epigenetic regulators that modulate gene expression via demethylation of histone and non-histone proteins, playing a pivotal role in cancer progression. Dysregulation of KDM activity, particularly in KDM1A, KDM4, KDM5, and KDM6, has been linked to several cancers, including leukemia and breast, lung, and prostate cancers, leading to the emergence of KDM inhibitors (KDMi) as promising therapeutic agents. These inhibitors target KDMs by mimicking cofactors, chelating metal ions, or competing with histone substrates to disrupt demethylation. Some of the most studied KDMi are those targeting KDM1A.Areas covered: In this review, we critically explore the complex roles of KDMs in cancer, provide a detailed overview of patents describing KDMi published from 2015 to the present, and assess European clinical trials investigating KDMi developed for cancer therapy.Expert opinion: Despite the promising potential of KDMi, their clinical development is hampered by significant challenges including safety concerns, suboptimal patient enrollment, and difficulties in optimizing dosing regimens and identifying reliable biomarkers. Future research must focus on refining dosing protocols, discovering predictive biomarkers, and developing effective combination therapies to maximize patient outcomes, ultimately realizing the full promise of KDMi in cancer treatment.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"65-89"},"PeriodicalIF":4.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713954","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Sirtuin modulators: a review of patents from 2020 to 2024. Sirtuin调节剂：2020年至2024年专利回顾。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-01-01 Epub Date: 2025-11-06 DOI: 10.1080/13543776.2025.2585821

Emanuele Fabbrizi, Francesco Fiorentino, Antonello Mai, Dante Rotili

{"title":"Sirtuin modulators: a review of patents from 2020 to 2024.","authors":"Emanuele Fabbrizi, Francesco Fiorentino, Antonello Mai, Dante Rotili","doi":"10.1080/13543776.2025.2585821","DOIUrl":"10.1080/13543776.2025.2585821","url":null,"abstract":"Introduction: Sirtuins have gained significant prominence in scientific research due to their involvement in a wide array of biological processes, including DNA repair, genome stability, transcription modulation, and signal transduction. Dysregulation of their function has been implicated in various pathologies, including cancer, where sirtuins exhibit context-dependent effects. Consequently, the development of sirtuin inhibitors and activators remains an exceptionally important field of research, focusing on the design of selective modulators targeting individual sirtuin isoforms.Areas covered: This review includes the patents regarding sirtuin modulators released from 2020 to 2024 and provides a concise overview of the most relevant modulators developed so far. Relevant patents were systematically identified through comprehensive searches in PubMed (https://pubmed.ncbi.nlm.nih.gov), Google Patents (https://patents.google.com), and Espacenet (https://worldwide.espacenet.com).Expert opinion: Sirtuin modulators are pivotal in addressing aging, metabolism, cancer, and neurodegeneration. Sirtuins regulate key cellular processes like DNA repair, genome stability, and mitochondrial function. Activators show promise in mitigating many age-related diseases such as type 2 diabetes and neurodegeneration. Inhibitors demonstrate efficacy in oncology and neurodegenerative conditions. Advances in PROTAC technology enable selective degradation of specific isoforms, enhancing therapeutic precision. With progress in drug design and high-throughput screening, sirtuin modulators hold immense potential to revolutionize treatments for complex medical challenges.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-23"},"PeriodicalIF":4.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145437900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Patent landscape in hydroxamic acid-based HDAC inhibitors (2020-2024): structure-activity relationships and mechanistic insights. 羟肟酸类HDAC抑制剂的专利前景（2020-2024）：结构-活性关系和机制见解。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-01-01 Epub Date: 2025-11-27 DOI: 10.1080/13543776.2025.2591483

Ekta Shirbhate, Vaibhav Singh, Vidya Prabha, Chandrabose Karthikeyan, Amit K Tiwari, Ravichandran Veerasamy, Haya Khader Ahmad Yasin, Harish Rajak

{"title":"Patent landscape in hydroxamic acid-based HDAC inhibitors (2020-2024): structure-activity relationships and mechanistic insights.","authors":"Ekta Shirbhate, Vaibhav Singh, Vidya Prabha, Chandrabose Karthikeyan, Amit K Tiwari, Ravichandran Veerasamy, Haya Khader Ahmad Yasin, Harish Rajak","doi":"10.1080/13543776.2025.2591483","DOIUrl":"10.1080/13543776.2025.2591483","url":null,"abstract":"Introduction: The hydroxamic acid-based histone deacetylase (HDAC) inhibitors play a crucial role as anticancer chemotherapeutics. It controls cellular pathways and epigenetically modifies gene expression, making them important for tackling the complicated character of cancer etiology.Areas covered: The action of current HDAC inhibitors on different target proteins and multiple-cancer cell lines are studied. The study underlines a comprehensive summary of different compounds published as patents from 2020 to 2024 and retrieved from Google patents, paying special attention to their structural differences and possible applications in cancer treatment. It stands out in today's scenario by providing structure-activity relationships (SAR) and mechanistic insights for heterocyclic scaffold-like pyrimidine, quinazoline, oxadiazole, thiadiazole, thiazole, piperazine, pyridine, indole and chromane rings used in the design of HDAC inhibitor.Expert opinion: Results reveal significant development in the synthesis of selective HDAC inhibitors with IC50 values in the nano and micromolar range, exceeding conventional inhibitors as vorinostat. Dual-targeting approaches have also evolved as sensible substitutes using molecules that improve treatment efficacy while reducing side effects. Thorough investigation on SAR across various heterocyclic scaffolds benefits future drug development projects, aimed at improving selectivity and minimizing side effects in cancer treatment.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"41-63"},"PeriodicalIF":4.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145539745","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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 patent review of topoisomerase 1 inhibitors (2021-present). 拓扑异构酶1抑制剂专利回顾（2021年至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-01-01 Epub Date: 2025-11-19 DOI: 10.1080/13543776.2025.2579073

Maria Fuertes, Endika Martín-Encinas, Asier Selas, Concepcion Alonso

{"title":"A patent review of topoisomerase 1 inhibitors (2021-present).","authors":"Maria Fuertes, Endika Martín-Encinas, Asier Selas, Concepcion Alonso","doi":"10.1080/13543776.2025.2579073","DOIUrl":"10.1080/13543776.2025.2579073","url":null,"abstract":"Introduction: Among the different topoisomerases, essential enzymes that play an important role in DNA processes such as replication and transcription, type I enzymes are targets of particular clinical importance for anticancer and antiparasitic drugs. Bearing this in mind, in the last 5 years specific inhibitors, both poison and suppressor types, have been patented for this target.Areas covered: This review covers the patent literature on topoisomerase 1 inhibitors and their application published between late 2020-present.Expert opinion: TOP1 inhibitors are being used in combination with synergistic therapies within a multimodal approach, including targeted therapies, adaptive immunotherapy, and the blockade of DNA repair mechanisms. Advances in drug delivery systems, especially antibody-drug conjugates (ADCs), are revolutionizing chemotherapy by enabling localized and tumor-specific drug release. In addition to traditional inhibitors like irinotecan and topotecan, new agents such as deruxtecan and govitecan have been approved, expanding therapeutic options. Moreover, small new molecules with more promising clinical potential are being developed.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"25-40"},"PeriodicalIF":4.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145512393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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 patent review of Mpro protease inhibitors for the treatment of COVID-19 infections (2020 - present). Mpro蛋白酶抑制剂治疗COVID-19感染的专利审查（2020年至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2026-01-01 Epub Date: 2025-12-08 DOI: 10.1080/13543776.2025.2588773

Václav Mik, Laila S Benz, Jiří Voller, Theresia Dunzendorfer-Matt, Manfred S Weiss, Vladimír Kryštof

{"title":"A patent review of Mpro protease inhibitors for the treatment of COVID-19 infections (2020 - present).","authors":"Václav Mik, Laila S Benz, Jiří Voller, Theresia Dunzendorfer-Matt, Manfred S Weiss, Vladimír Kryštof","doi":"10.1080/13543776.2025.2588773","DOIUrl":"10.1080/13543776.2025.2588773","url":null,"abstract":"Introduction: The SARS-CoV-2 main protease (Mpro, also known as 3CLpro or nsp5) is essential for viral replication. As there are no close human homologs, it represents an attractive and specific target for antiviral therapy against COVID-19. Its well-defined active site and conserved substrate specificity have enabled structure-guided drug design with high precision.Areas covered: This review examines the patent landscape for small-molecule inhibitors of SARS-CoV-2 Mpro published between 2020 and early 2025. Compounds were grouped by scaffold type and mechanism of action, covering covalent and non-covalent inhibitors, orthosteric and allosteric binders and unique modalities such as PROTACs. Clinically advanced agents including nirmatrelvir, ensitrelvir, simnotrelvir, zevotrelvir and leritrelvir are highlighted alongside structurally novel leads and broad-spectrum candidates.Expert opinion: A number of Mpro inhibitors have progressed into preclinical and clinical stages, underscoring the rapid advancement in this field. The accumulation of structural knowledge, chemical diversity and mechanistic insight has laid a robust foundation for future antiviral development and may further enhance the utility of Mpro inhibitors against evolving coronaviruses.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"91-109"},"PeriodicalIF":4.6,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145676861","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Insights and trends in development of TEAD-YAP/TAZ inhibitors: a review of PCT patents (2022 to June 2025). eotp - 2025 - 0028。TEAD-YAP/TAZ抑制剂发展的洞察和趋势：PCT专利回顾（2022年至2025年6月）

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-12-01 Epub Date: 2025-11-07 DOI: 10.1080/13543776.2025.2574611

Te Fan, Zhong Yu, Aiping Xiao, Yan Zhang, Fei Xiang

{"title":"Insights and trends in development of TEAD-YAP/TAZ inhibitors: a review of PCT patents (2022 to June 2025).","authors":"Te Fan, Zhong Yu, Aiping Xiao, Yan Zhang, Fei Xiang","doi":"10.1080/13543776.2025.2574611","DOIUrl":"10.1080/13543776.2025.2574611","url":null,"abstract":"Introduction: The transcription enhancer associated domain (TEAD) family has been well documented for its roles in modulating cancer development, primarily through interactions with its two co-activators: yes-associated protein (YAP) and transcriptional coactivator with PDZ-binding motif (TAZ). Although TEAD was first reported more than two decades ago, no therapeutic compounds directly targeting this protein or its interaction with YAP/TAZ are currently available or in late-phase clinical development. This underscores the need for continued exploration of novel strategies for the molecular design of targeted therapies, to which updated patent reviews are expected to make a considerable contribution.Areas covered: This review evaluated the Patent Cooperation Treaty (PCT) patents claiming TEAD - YAP/TAZ inhibitors published between 1 January 2022 and 30 June 2025, and provides opinions on strategies for the development of TEAD - YAP/TAZ inhibitors.Expert opinion: Over the past 3 years, there has been a marked increase in the number of PCT patents claiming structurally diverse TEAD - YAP/TAZ inhibitors, including filings by potentially new players. This trend highlights the growing recognition of the TEAD - YAP/TAZ axis as an attractive strategy for the development of new drugs, particularly for anti-cancer therapeutics.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1209-1239"},"PeriodicalIF":4.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145279350","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Therapeutic applications of benzoxaborole compounds: a patent and literature analysis (2019-2024). 苯并恶咯罗勒化合物的治疗应用：专利和文献分析（2019-2024）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-12-01 Epub Date: 2025-10-25 DOI: 10.1080/13543776.2025.2576513

Simone Giovannuzzi, Alessio Nocentini, Claudiu T Supuran, Jean-Yves Winum

{"title":"Therapeutic applications of benzoxaborole compounds: a patent and literature analysis (2019-2024).","authors":"Simone Giovannuzzi, Alessio Nocentini, Claudiu T Supuran, Jean-Yves Winum","doi":"10.1080/13543776.2025.2576513","DOIUrl":"10.1080/13543776.2025.2576513","url":null,"abstract":"Introduction: Benzoxaborole is a boron-based heterocyclic scaffold with remarkable potential in medicinal chemistry. Its unique chemical structure and compatibility with biological systems have enabled the development of innovative drug candidates. Benzoxaborole derivatives exhibit diverse biological activities, including antibacterial, antifungal, antiparasitic, antiviral, anticancer, and anti-inflammatory effects, making them valuable in addressing various medical challenges.Areas covered: This manuscript reviews the medicinal chemistry literature and patent landscape from 2019 to 2024, focusing on the therapeutic potential of benzoxaborole-based compounds.Expert opinion: Benzoxaboroles are gaining recognition as a versatile and innovative class of therapeutics with strong potential in infectious diseases, oncology, and inflammatory conditions. Their unique boron-containing scaffold enables diverse biological interactions and favorable pharmacokinetic properties. While clinical data are still emerging, early results and robust patent activity suggest significant therapeutic value. Advances in synthetic methods, targeted delivery, and computational design are accelerating their development. With continued focused research and strategic clinical validation, benzoxaboroles are well-positioned to address pressing medical challenges, particularly antimicrobial resistance, and could become an integral part of future treatment paradigms across multiple therapeutic areas.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1241-1261"},"PeriodicalIF":4.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145307345","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Medicinal chemistry perspective of ERK1/2 inhibitors in cancer treatment: an updated patent review (2019-present). ERK1/2抑制剂在癌症治疗中的药物化学前景：更新的专利审查（2019年至今）

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-12-01 Epub Date: 2025-10-14 DOI: 10.1080/13543776.2025.2575028

Ankit Kumar Singh, Ajad Chauhan, Vineet Prajapati, Adarsh Kumar, Harshwardhan Singh, Amita Verma, Pradeep Kumar

{"title":"Medicinal chemistry perspective of ERK1/2 inhibitors in cancer treatment: an updated patent review (2019-present).","authors":"Ankit Kumar Singh, Ajad Chauhan, Vineet Prajapati, Adarsh Kumar, Harshwardhan Singh, Amita Verma, Pradeep Kumar","doi":"10.1080/13543776.2025.2575028","DOIUrl":"10.1080/13543776.2025.2575028","url":null,"abstract":"Introduction: The mitogen-activated protein kinase (MAPK) pathway also known as the RAS/RAF/MEK/ERK pathway is a vital intracellular signaling cascade that regulates apoptosis, differentiation, proliferation, and signal transduction.Area covered: This review focuses on the critical role of ERK1/2 in the MAPK pathway and its implication in various cancers. It presents a detailed analysis of ERK1/2 inhibitors currently undergoing clinical evaluation, along with recently patented ERK1/2 inhibitors. The data were compiled by systematically searching databases including SciFinder, PubMed, Scopus, Google Scholar, and Google Patents using the keyword 'ERK' for the period 2019 to the present.Expert opinion: Since 2019, several heterocyclic ERK1/2 inhibitors have shown promise in overcoming resistance within the MAPK cascade. However, detailed investigations into mutant versus wild-type ERK1/2 binding dynamics remain sparse, and the development of non-traditional approaches like PROTAC-mediated ERK degradation is still in its nascent stage. To successfully transition ERK1/2 inhibitors from bench to bedside, several strategic directions must be prioritized. First, overcoming resistance remains a critical challenge. Future ERK inhibitors must effectively target downstream components. Second, there is a pressing need to move beyond traditional ATP-competitive inhibitors. In addition, the pharmacological properties of ERK-targeting agents to enhance clinical efficacy and safety.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1185-1207"},"PeriodicalIF":4.6,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145286015","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

An updated patent review of small molecule glucagon receptor antagonists (2020-2024). 小分子胰高血糖素受体拮抗剂专利更新综述（2020-2024）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-11-01 Epub Date: 2025-09-21 DOI: 10.1080/13543776.2025.2559928

Chunyang Wang, Liyang Lyu, Dongyang Liu, Yuanjia Hu

{"title":"An updated patent review of small molecule glucagon receptor antagonists (2020-2024).","authors":"Chunyang Wang, Liyang Lyu, Dongyang Liu, Yuanjia Hu","doi":"10.1080/13543776.2025.2559928","DOIUrl":"10.1080/13543776.2025.2559928","url":null,"abstract":"Introduction: The glucagon receptor (GCGR) plays a pivotal role in diabetes management. While small molecule GCGR antagonists (GCGRAs) offer several advantages, including glycemic control, oral bioavailability, and cost-effectiveness, their clinical development is hampered by safety concerns. Recent structural and mechanistic insights have elucidated ligand binding and biased signaling and informed the rational design of GCGRAs.Areas covered: This review presents an overview of small molecule GCGRAs between 2020 and 2024, drawing information from existing patents, peer-reviewed literature, and clinical data retrieved from the PubMed, Web of Science, SciFinder, and Derwent Innovation databases.Expert opinion: In this observation period, innovation ownership shifted from pharmaceutical companies to academic institutions, which are emerging as key applicants for novel chemotypes. Such a significant shift reflects a broader divergence in innovation strategies, with academia increasingly exploring new chemotypes supported by deep learning and virtual screening, while companies focus on maintaining and optimizing established scaffolds. Furthermore, advances in structural and mechanistic studies have clarified ligand binding and biased signaling, informing the rational design of high-specificity, high-affinity GCGRAs. However, clinical investigations are warranted to assess whether these compounds can overcome current developmental bottlenecks, restore glucose homeostasis, and address safety concerns.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1169-1183"},"PeriodicalIF":4.6,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145085228","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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 patent review of MLKL modulators (2023 - present). MLKL调制器专利回顾（2023年至今）。

IF 4.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-11-01 Epub Date: 2025-09-22 DOI: 10.1080/13543776.2025.2563877

Bo-Wen Wan, Cheng-Shi Jiang, Chunlin Zhuang

{"title":"A patent review of MLKL modulators (2023 - present).","authors":"Bo-Wen Wan, Cheng-Shi Jiang, Chunlin Zhuang","doi":"10.1080/13543776.2025.2563877","DOIUrl":"10.1080/13543776.2025.2563877","url":null,"abstract":"Introduction: Mixed-spectrum kinase structural domain-like protein (MLKL), which emerged as a pivotal regulator in biomedical research, plays a critical role in necroptotic pathways. Recent advancements have underscored the therapeutic potential of MLKL modulators.Areas covered: This review focuses on the patent literature covering MLKL-targeted molecules published from 2023 to July 2025. Patent and literature searching were performed using SciFinder, Espacenet, and PubMed databases.Expert opinion: Research on MLKL modulators has seen significant progress in recent years, with many preclinical studies documenting various modulators, but the development of MLKL modulators, particularly activators, remains in its early stages due to challenges in specificity, efficacy, and bioavailability. Advancing therapeutic strategies will require a deeper understanding of MLKL-driven pathologies, optimizing existing modulators, and discovering new ones. The notable increase in natural product-derived MLKL inhibitors highlights the potential of identifying and modifying natural products as an effective approach for developing novel inhibitors.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1155-1167"},"PeriodicalIF":4.6,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145079997","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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