作为结直肠癌治疗靶点的 PI3K 和 tankyrase 抑制剂。

IF 4.6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Therapeutic Targets Pub Date : 2024-03-01 Epub Date: 2024-03-21 DOI:10.1080/14728222.2024.2331015
Prasanna Anjaneyulu Yakkala, Fatima Naaz, Syed Shafi, Ahmed Kamal
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引用次数: 0

摘要

导言:永利相关整合(Wnt/β-catenin)和 PI3K 等通路在结直肠癌(CRC)的发展过程中发挥着重要作用,但它们在肿瘤发生过程中的作用却各不相同。尽管存在差异,但这些通路通过反馈机制相互作用,并在正常和病理情况下调控上游和下游过程中的共同效应因子。它们相互控制的能力是 CRC 选择性抑制剂的主要抵抗机制:本综述重点介绍了 CRC 中相互关联的 Wnt/β-catenin 和 PI3K 通路、最近的研究进展以及开发针对 Tankyrase 酶和 PI3K 的抑制剂的一些重要观点,此外还简要介绍了 PI3K 和 Tankyrases(TNKS)双重抑制剂的潜力:最近的研究主要集中在克服挑战上,特别是与针对 PI3K 和 Tankyrase 蛋白的双重抑制剂的耐药性和疗效有关的挑战。尽管存在这些挑战,但PI3K和Tankyr酶仍然是治疗实体瘤的有希望的治疗靶点。设计有效的抑制剂对于有效阻断这些蛋白信号通路至关重要。此外,还必须探索结合 PI3K 和 tankyrase 对其他信号通路进行双靶点抑制的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PI3K and tankyrase inhibitors as therapeutic targets in colorectal cancer.

Introduction: The pathways like Wingless-related integration (Wnt/β-catenin) and PI3K play an important role in colorectal cancer (CRC) development; however, their roles are distinct in the process of oncogenesis. Despite their differences, these pathways interact through feedback mechanisms and regulate the common effectors both in the upstream and the downstream processes in normal and pathological conditions. Their ability to reciprocally control each other is a primary resistance mechanism for the selective inhibitors in CRC.

Area covered: This review highlights the Wnt/β-catenin and PI3K pathways that are interrelated in CRC, recent advances and some key perspectives in developing inhibitors that could target the tankyrase enzyme and PI3K, apart from a brief description of the potential of dual inhibitors of PI3K and Tankyrases (TNKS).

Expert opinion: Recent research has focused on overcoming the challenges particularly relating to the resistance and efficacy of dual inhibitors targeting PI3K and tankyrase proteins. Despite these challenges, PI3K as well as tankyrases remain promising therapeutic targets for the treatment of solid tumors. The design of potent inhibitors is crucial to effectively block these protein signaling pathways. Moreover, it is essential to explore the potential of dual-target inhibition of other signaling pathways in conjunction with PI3K and tankyrase.

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来源期刊
CiteScore
8.90
自引率
1.70%
发文量
58
审稿时长
3 months
期刊介绍: The journal evaluates molecules, signalling pathways, receptors and other therapeutic targets and their potential as candidates for drug development. Articles in this journal focus on the molecular level and early preclinical studies. Articles should not include clinical information including specific drugs and clinical trials. The Editors welcome: Reviews covering novel disease targets at the molecular level and information on early preclinical studies and their implications for future drug development. Articles should not include clinical information including specific drugs and clinical trials. Original research papers reporting results of target selection and validation studies and basic mechanism of action studies for investigative and marketed drugs. The audience consists of scientists, managers and decision makers in the pharmaceutical industry, academic researchers working in the field of molecular medicine and others closely involved in R&D.
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