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Recent advances in pharmacological diversification of Src family kinase inhibitors

Preeya Negi, Rameshwar S. Cheke, Vaishali M. Patil

2021Egyptian Journal of Medical Human Genetics21 citationsDOIOpen Access PDF

Abstract

Abstract Background Src kinase, a nonreceptor protein-tyrosine kinase is composed of 11 members (in human) and is involved in a wide variety of essential functions required to sustain cellular homeostasis and survival. Main body of the abstract Deregulated activity of Src family kinase is related to malignant transformation. In 2001, Food and Drug Administration approved imatinib for the treatment of chronic myeloid leukemia followed by approval of various other inhibitors from this category as effective therapeutics for cancer patients. In the past decade, Src family kinase has been investigated for the treatment of diverse pathologies in addition to cancer. In this regard, we provide a systematic evaluation of Src kinase regarding its mechanistic role in cancer and other diseases. Here we comment on preclinical and clinical success of Src kinase inhibitors in cancer followed by diabetes, hypertension, tuberculosis, and inflammation. Short conclusion Studies focusing on the diversified role of Src kinase as potential therapeutical target for the development of medicinally active agents might produce significant advances in the management of not only various types of cancer but also other diseases which are in demand for potent and safe therapeutics.

Topics & Concepts

Proto-oncogene tyrosine-protein kinase SrcTyrosine kinaseCancerMedicineKinaseSrc family kinaseImatinibCancer researchPharmacologyMyeloid leukemiaBiologyInternal medicineCell biologyReceptorCytokine Signaling Pathways and InteractionsCancer Mechanisms and TherapyPI3K/AKT/mTOR signaling in cancer
Recent advances in pharmacological diversification of Src family kinase inhibitors | Litcius