Related Experiment Video

Updated: May 27, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

SRC kinase inhibitors: an update on patented compounds

S Schenone1, C Brullo, F Musumeci

  • 1Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Genova, Viale Benedetto XV, 3, I-16132 Genova, Italy. schensil@unige.it

Current Medicinal Chemistry
|November 5, 2011
PubMed

Insights

The cytoplasmic tyrosine kinase c-Src is crucial in cancer development. Inhibitors targeting c-Src show promise as cancer therapeutics, with ongoing research exploring selective and multitargeted compounds for improved efficacy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Cytoplasmic tyrosine kinase c-Src regulates cell functions like adhesion, invasion, proliferation, survival, and angiogenesis.
  • Overexpression or hyperactivation of c-Src is critical in tumor development, suggesting its oncogenic potential is linked to signaling pathway activation.
  • c-Src is a promising therapeutic target for cancer treatment due to its role in tumor progression.

Purpose of the Study:

  • To review c-Src inhibitors from patents (2006-2011).
  • To focus on chemical features, structure-activity relationships, and mechanisms of action of these inhibitors.
  • To highlight ongoing research and potential for novel cancer therapeutics.

Main Methods:

  • Patent literature review (2006-2011) focusing on c-Src inhibitors.
  • Analysis of chemical features and structure-activity relationships.
  • Categorization of inhibitors (Type I/II ATP-competitive, substrate-competitive).

Main Results:

  • Examples of various c-Src inhibitors identified in patents are presented.
  • Discussion includes chemical characteristics and, where available, structure-activity relationships and mechanisms of action.
  • Active research indicates potential for both c-Src selective and multitargeted inhibitors.

Conclusions:

  • c-Src inhibitors represent a promising therapeutic strategy for cancer treatment.
  • Ongoing research is actively developing selective and multitargeted compounds.
  • Clinical trial outcomes will determine the most effective therapeutic compounds in the near future.

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
MAPK Signaling Cascades01:07

MAPK Signaling Cascades

Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include: