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胰腺癌的分子研究:小分子抑制剂、其作用机制及其他

Molecular Research in Pancreatic Cancer: Small Molecule Inhibitors, Their Mechanistic Pathways and Beyond.

作者信息

Shetu Shaila A, James Nneoma, Rivera Gildardo, Bandyopadhyay Debasish

机构信息

Department of Chemistry, The University of Texas Rio Grande Valley, 1201 West University Drive, Edinburg, TX 78539, USA.

Laboratorio de Biotecnología Farmacéutica, Centro de Biotecnología Genómica, Instituto Politécnico Nacional, Reynosa 88710, Mexico.

出版信息

Curr Issues Mol Biol. 2023 Feb 27;45(3):1914-1949. doi: 10.3390/cimb45030124.

Abstract

Pancreatic enzymes assist metabolic digestion, and hormones like insulin and glucagon play a critical role in maintaining our blood sugar levels. A malignant pancreas is incapable of doing its regular functions, which results in a health catastrophe. To date, there is no effective biomarker to detect early-stage pancreatic cancer, which makes pancreatic cancer the cancer with the highest mortality rate of all cancer types. Primarily, mutations of the , , , and genes are responsible for pancreatic cancer, of which mutations of the gene are present in more than 80% of pancreatic cancer cases. Accordingly, there is a desperate need to develop effective inhibitors of the proteins that are responsible for the proliferation, propagation, regulation, invasion, angiogenesis, and metastasis of pancreatic cancer. This article discusses the effectiveness and mode of action at the molecular level of a wide range of small molecule inhibitors that include pharmaceutically privileged molecules, compounds under clinical trials, and commercial drugs. Both natural and synthetic small molecule inhibitors have been counted. Anti-pancreatic cancer activity and related benefits of using single and combined therapy have been discussed separately. This article sheds light on the scenario, constraints, and future aspects of various small molecule inhibitors for treating pancreatic cancer-the most dreadful cancer so far.

摘要

胰腺酶有助于新陈代谢消化,胰岛素和胰高血糖素等激素在维持我们的血糖水平方面发挥着关键作用。恶性胰腺无法履行其正常功能,这会导致健康灾难。迄今为止,尚无有效的生物标志物来检测早期胰腺癌,这使得胰腺癌成为所有癌症类型中死亡率最高的癌症。主要是 、 、 和 基因的突变导致胰腺癌,其中 基因的突变存在于超过80%的胰腺癌病例中。因此,迫切需要开发对负责胰腺癌增殖、传播、调节、侵袭、血管生成和转移的蛋白质有效的抑制剂。本文讨论了包括药学上有特权的分子、临床试验中的化合物和商业药物在内的多种小分子抑制剂在分子水平上的有效性和作用方式。天然和合成小分子抑制剂均已统计在内。分别讨论了使用单一疗法和联合疗法的抗胰腺癌活性及相关益处。本文揭示了用于治疗胰腺癌(迄今为止最可怕的癌症)的各种小分子抑制剂的情况、限制和未来方面。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/65cc/10047141/ae23ad3d0a4a/cimb-45-00124-g001.jpg

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