State Key Laboratories of Chemical Resources Engineering Beijing University of Chemical Technology, Beijing 100029, China.
Department of Biochemistry, Computational Medicinal Chemistry Laboratory, UCSS, Abdul Wali Khan University, Mardan, Pakistan.
Curr Pharm Des. 2022;28(28):2343-2348. doi: 10.2174/1381612828666220728101812.
Breast cancer is a common malignancy in women and is a diverse disease. In women, 287,850 and in males 2710 cases are reported in 2022 by WHO. Triple-negative breast cancer (TNBC), a subtype of breast cancer that lacks expression of the estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2), accounted for 10-20% of all new cases discovered in the United States in 2017. Because calcium integrin-binding protein1 lacks a suitable pocket that could be used to create a chemical inhibitor, and because the breast cancer-causing protein is nearly identical to its necessary wild-type counterpart, it was thought to be druggable. The structure and function of the newly discovered calcium integrinbinding protein1 have been improved, paving the way for the designing of several therapeutic candidates. Currently, no FDA-approved drugs are available for CIB1-driven cancer. CIB1 has proven to challenge drug target due to several factors, including the fact that the CIB1 protein is highly resistant to small inhibitors. This study aimed to present various ways for targeting calcium integrin-binding protein1, which is an important target that could be useful to scientists.
乳腺癌是女性常见的恶性肿瘤，是一种多样化的疾病。2022 年，世卫组织报告称，女性中有 287850 例，男性中有 2710 例。三阴性乳腺癌（TNBC）是一种缺乏雌激素受体（ER）、孕激素受体（PR）和人表皮生长因子受体 2（HER2）表达的乳腺癌亚型，在美国 2017 年发现的所有新病例中占 10-20%。由于钙整合素结合蛋白 1 缺乏一个合适的口袋，无法用来制造化学抑制剂，而且导致乳腺癌的蛋白质与它必需的野生型对应物几乎完全相同，因此人们认为它是可成药的。新发现的钙整合素结合蛋白 1 的结构和功能得到了改善，为设计几种治疗候选药物铺平了道路。目前，尚无 FDA 批准的药物可用于 CIB1 驱动的癌症。由于多种因素，包括 CIB1 蛋白对小分子抑制剂具有高度抗性，CIB1 已被证明是药物靶点的挑战。本研究旨在提出针对钙整合素结合蛋白 1 的各种方法，这是一个重要的靶点，对科学家可能有用。
