Department of Molecular Medicine (DMM), Dow College of Biotechnology (DCoB), Dow University of Health Sciences (DUHS), Karachi, Pakistan.
DOW-DOGANA Advanced Molecular Genetics and Genomics Disease Research and Treatment Center (AMGGDRTC), Dow University of Health Sciences (DUHS), Karachi, Pakistan.
PLoS One. 2024 Apr 18;19(4):e0298747. doi: 10.1371/journal.pone.0298747. eCollection 2024.
Human kinases play essential and diverse roles in the cellular activities of maintaining homeostasis and growth. Genetic mutations in the genes encoding the kinases (or phosphotransferases) have been linked with various types of cancers. In this study, we cataloged mutations in 500 kinases genes in >65,000 individuals of global populations from the Human Genetic Diversity Project (HGDP) and ExAC databases, and assessed their potentially deleterious impact by using the in silico tools SIFT, Polyphen2, and CADD. The analysis highlighted 35 deleterious non-synonymous SNVs in the ExAC and 5 SNVs in the HGDP project. Notably, a higher number of deleterious mutations was observed in the Non-Finnish Europeans (26 SNVs), followed by the Africans (14 SNVs), East Asians (13 SNVs), and South Asians (12 SNVs). The gene set enrichment analysis highlighted NTRK1 and FGFR3 being most significantly enriched among the kinases. The gene expression analysis revealed over-expression of NTRK1 in liver cancer, whereas, FGFR3 was found over-expressed in lung, breast, and liver cancers compared to their expression in the respective normal tissues. Also, 13 potential drugs were identified that target the NTRK1 protein, whereas 6 potential drugs for the FGFR3 target were identified. Taken together, the study provides a framework for exploring the predisposing germline mutations in kinases to suggest the underlying pathogenic mechanisms in cancers. The potential drugs are also suggested for personalized cancer management.
人类激酶在维持体内平衡和生长的细胞活动中发挥着重要而多样的作用。编码激酶(或磷酸转移酶)的基因突变与各种类型的癌症有关。在这项研究中,我们对来自人类遗传多样性计划(HGDP)和 ExAC 数据库的全球超过 65000 个人的 500 个激酶基因中的突变进行了编目,并使用 SIFT、Polyphen2 和 CADD 等计算工具评估了它们潜在的有害影响。分析突出了 ExAC 中的 35 个有害非同义 SNV 和 HGDP 项目中的 5 个 SNV。值得注意的是,在非芬兰裔欧洲人中观察到更多的有害突变(26 个 SNV),其次是非洲人(14 个 SNV)、东亚人(13 个 SNV)和南亚人(12 个 SNV)。基因集富集分析突出了 NTRK1 和 FGFR3 在激酶中最为显著富集。基因表达分析显示 NTRK1 在肝癌中过度表达,而 FGFR3 在肺癌、乳腺癌和肝癌中的表达高于相应的正常组织。此外,还鉴定出了 13 种针对 NTRK1 蛋白的潜在药物,而针对 FGFR3 靶点的潜在药物有 6 种。总之,该研究为探索激酶中的种系易感性突变提供了一个框架,以提示癌症中的潜在发病机制。还建议使用潜在药物进行个性化癌症管理。