Next Article in Journal
Engineering Solutions for Mitigation of Chimeric Antigen Receptor T-Cell Dysfunction
Previous Article in Journal
Sex Hormones and Hormone Therapy during COVID-19 Pandemic: Implications for Patients with Cancer
Previous Article in Special Issue
Src Family Tyrosine Kinases in Intestinal Homeostasis, Regeneration and Tumorigenesis
Review

Three-Dimensional Interactions Analysis of the Anticancer Target c-Src Kinase with Its Inhibitors

Department of Pharmacy, University of Pisa, 56126 Pisa, Italy
*
Author to whom correspondence should be addressed.
Cancers 2020, 12(8), 2327; https://doi.org/10.3390/cancers12082327
Received: 13 July 2020 / Revised: 7 August 2020 / Accepted: 16 August 2020 / Published: 18 August 2020
(This article belongs to the Special Issue The Role of Src Kinase Family in Cancer)
Src family kinases (SFKs) constitute the biggest family of non-receptor tyrosine kinases considered as therapeutic targets for cancer therapy. An aberrant expression and/or activation of the proto-oncogene c-Src kinase, which is the oldest and most studied member of the family, has long been demonstrated to play a major role in the development, growth, progression and metastasis of numerous human cancers, including colon, breast, gastric, pancreatic, lung and brain carcinomas. For these reasons, the pharmacological inhibition of c-Src activity represents an effective anticancer strategy and a few compounds targeting c-Src, together with other kinases, have been approved as drugs for cancer therapy, while others are currently undergoing preclinical studies. Nevertheless, the development of potent and selective inhibitors of c-Src aimed at properly exploiting this biological target for the treatment of cancer still represents a growing field of study. In this review, the co-crystal structures of c-Src kinase in complex with inhibitors discovered in the past two decades have been described, highlighting the key ligand–protein interactions necessary to obtain high potency and the features to be exploited for addressing selectivity and drug resistance issues, thus providing useful information for the design of new and potent c-Src kinase inhibitors. View Full-Text
Keywords: c-Src kinase; ligand–protein interaction c-Src kinase; ligand–protein interaction
Show Figures

Figure 1

MDPI and ACS Style

Jha, V.; Macchia, M.; Tuccinardi, T.; Poli, G. Three-Dimensional Interactions Analysis of the Anticancer Target c-Src Kinase with Its Inhibitors. Cancers 2020, 12, 2327. https://doi.org/10.3390/cancers12082327

AMA Style

Jha V, Macchia M, Tuccinardi T, Poli G. Three-Dimensional Interactions Analysis of the Anticancer Target c-Src Kinase with Its Inhibitors. Cancers. 2020; 12(8):2327. https://doi.org/10.3390/cancers12082327

Chicago/Turabian Style

Jha, Vibhu, Marco Macchia, Tiziano Tuccinardi, and Giulio Poli. 2020. "Three-Dimensional Interactions Analysis of the Anticancer Target c-Src Kinase with Its Inhibitors" Cancers 12, no. 8: 2327. https://doi.org/10.3390/cancers12082327

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop