Protein Kinase Targets in Breast Cancer

Abstract

With 1.67 million new cases and 522,000 deaths in the year 2012, breast cancer is the most common type of diagnosed malignancy and the second leading cause of cancer death in women around the world. Despite the success of screening programs and the development of adjuvant therapies, a significant percentage of breast cancer patients will suffer a metastatic disease that, to this day, remains incurable and justifies the research of new therapies to improve their life expectancy. Among the new therapies that have been developed in recent years, the emergence of targeted therapies has been a milestone in the fight against cancer. Over the past decade, many studies have shown a causal role of protein kinase dysregulations or mutations in different human diseases, including cancer. Along these lines, cancer research has demonstrated a key role of many protein kinases during human tumorigenesis and cancer progression, turning these molecules into valid candidates for new targeted therapies. The subsequent discovery and introduction in 2001 of the kinase inhibitor imatinib, as a targeted treatment for chronic myelogenous leukemia, revolutionized cancer genetic pathways research, and lead to the development of multiple small-molecule kinase inhibitors against various malignancies, including breast cancer. In this review, we analyze studies published to date about novel small-molecule kinase inhibitors and evaluate if they would be useful to develop new treatment strategies for breast cancer patients.

Bioinformatics Analysis of Global Proteomic and Phosphoproteomic Data Sets Revealed Activation of NEK2 and AURKA in Cancers

“…Carboxamide 11 is one of the best known selective inhibitors of NEK2 [38]. NEK2 has been reported to have a role in the progression of several malignancies, importantly in breast cancer, therefore devising the potential of an anticancer therapy [36,39,40]. AURKA is yet another essential target for a better clinical outcome in cancer treatment.…”

Paclitaxel’s Mechanistic and Clinical Effects on Breast Cancer

“…Epirubicin, similar to other anthracyclines, acts as an intercalating agent with DNA and thus interferes with transcription, resulting in suppression of RNA synthesis [46,47]. Kinase inhibitors Palbociclib and Ribociclib are both cyclin-dependent inhibitors suppressing cyclin dependent kinase (CDK) 4/6 activity to elicit the inhibition of proliferation [48]. 5-Fluorouracil, Capecitabine, and Gemcitabine are nucleoside inhibitors associated with the silencing of transcription and translation in BC [49].…”

Molecular targets of curcumin in breast cancer (Review)

“…Breast cancer is the most common cancer in women worldwide; it accounts for ~25% of all female malignancies and its prevalence is higher in developed countries (1). Breast cancer is the second leading cause of cancer-associated mortality among women in the world (1,2).…”

“…Breast cancer is the most common cancer in women worldwide; it accounts for ~25% of all female malignancies and its prevalence is higher in developed countries (1). Breast cancer is the second leading cause of cancer-associated mortality among women in the world (1,2). Current therapeutic strategies for breast cancer, which include surgery, chemotherapy and radiotherapy, may lack efficacy due to a high risk of relapse, poor patient response and the emergence of drug resistance (3).…”