Traf2- and Nck-interacting kinase inhibitors: a patent review (2008-2024).

IF 4.6 2区医学 Q1 CHEMISTRY, MEDICINAL

Expert Opinion on Therapeutic Patents Pub Date : 2025-10-01 Epub Date: 2025-08-20 DOI:10.1080/13543776.2025.2548585

Luoheng Qin, Vladimir Aladinskiy, David Gennert, Xin Cheng, Jinxin Liu, Tingting Liu, Feng Ren, Alex Zhavoronkov

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引用次数: 0

Abstract

Introduction: Traf2- and Nck-interacting kinase (TNIK) is a crucial player in various intracellular signaling pathways, including Wnt/β-catenin, cytoskeleton organization, and immune activation. It phosphorylates several key target genes and is widely expressed in different organ systems, such as neural, gastrointestinal, lung, liver, and kidney tissues. TNIK has been implicated in multiple different disease areas, including oncology, neurological diseases, and fibrosis.

Area covered: This review provides an update of small molecule TNIK inhibitors in patents published from 2008 to 2024.

Expert opinion: Despite over 10 patents disclosing multiple scaffolds since 2008, only one inhibitor, INS018_055, has advanced to clinical trials to treat idiopathic pulmonary fibrosis. For the oncology indications, this is largely due to complexities in the relationship between TNIK and oncogenic pathways. Additionally, key characteristics of the molecules, such as kinase selectivity, physicochemical properties, and pharmacokinetic profiles, have played significant roles in determining whether the molecules are drug-like enough to advance to clinical trials.

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Traf2和nck相互作用激酶抑制剂：专利审查（2008 - 2024）。

Traf2和nck相互作用激酶（TNIK）在多种细胞内信号通路中起着至关重要的作用，包括Wnt/β-catenin，细胞骨架组织和免疫激活。它磷酸化几个关键靶基因，并广泛表达于不同的器官系统，如神经、胃肠、肺、肝和肾组织。TNIK涉及多种不同的疾病领域，包括肿瘤、神经系统疾病和纤维化。涵盖领域：本综述提供了2008年至2024年发表的专利中小分子TNIK抑制剂的最新情况。专家意见：尽管自2008年以来有超过10项专利披露了多种支架，但只有一种抑制剂INS018_055进入了治疗特发性肺纤维化的临床试验。对于肿瘤适应症，这主要是由于TNIK与致癌途径之间关系的复杂性。此外，分子的关键特征，如激酶选择性、物理化学性质和药代动力学特征，在决定分子是否具有足够的药物样性以进行临床试验方面发挥了重要作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Expert Opinion on Therapeutic Patents 医学-药学

CiteScore

12.10

自引率

1.50%

发文量

审稿时长

6-12 weeks

期刊介绍： Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.