Related Experiment Video
Updated: Aug 10, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
Src inhibitors: genomics to therapeutics
T Sawyer1, B Boyce, D Dalgarno
1ARIAD Pharmaceuticals, Cambridge, MA 02139, USA.
Abstract:
Following the milestone discoveries that identified Src as the first known protein tyrosine kinase and as a prototype oncogene, as well as Src transgenic studies to validate it as a promising therapeutic target for osteoporosis, intense efforts are being made to create Src inhibitor drugs. Drug discovery strategies focused on both the non-catalytic and catalytic domains of Src have successfully resulted in promising Src inhibitor lead compounds with potential therapeutic applications for osteoporosis, cancer, and other diseases. Some noteworthy examples of Src inhibitors are described, and their chemical diversity, structure-based design, and biological activities in vitro and in vivo are illustrated. The potency, selectivity, and in vivo efficacy of key Src inhibitors are being investigated in molecular, cellular and animal models. Consequently, Src inhibitor drug development is imminent, and current studies are well-poised to achieve the ultimate milestone of a Src inhibitor therapeutic.
Insights
Developing Src inhibitor drugs shows promise for treating osteoporosis and cancer. Research highlights diverse chemical compounds and their effectiveness in preclinical models, paving the way for new therapeutics.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Src is a key protein tyrosine kinase and oncogene.
- Src is a validated therapeutic target for osteoporosis and cancer.
- Intensive efforts are underway to develop Src inhibitor drugs.
Purpose of the Study:
- To review the progress in developing Src inhibitor drugs.
- To highlight chemical diversity and structure-based design of Src inhibitors.
- To illustrate the in vitro and in vivo biological activities of Src inhibitors.
Main Methods:
- Review of existing literature on Src inhibitors.
- Analysis of chemical structures and design strategies.
- Evaluation of in vitro and in vivo data on potency, selectivity, and efficacy.
Main Results:
- Promising Src inhibitor lead compounds have been identified.
- Inhibitors target both catalytic and non-catalytic domains of Src.
- Key inhibitors demonstrate potent, selective, and effective activity in preclinical models.
Conclusions:
- Src inhibitor drug development is nearing clinical application.
- Current research is well-positioned for therapeutic breakthroughs.
- Src inhibitors offer potential treatments for osteoporosis, cancer, and other diseases.
More Related Videos
08:59Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down
Published on: December 11, 2017
03:08Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization
Published on: October 3, 2025
Related Concept Videos
Genomics
Genetic Screens
Forward genetic screens
Forward or “classical” genetic screens involve creating random mutations in an organism’s DNA using radiation, mutagens, or insertion of additional bases, which result in visible changes...
Pharmacogenetics and Pharmacogenomics: Overview
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Pharmacogenomics: Identification of New Drug Targets