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Inhibition of Cdk Activity

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 Activity

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...

PI3K/mTOR/AKT Signaling Pathway

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast, mTORC2 consists of a rapamycin-insensitive companion...

Protein Kinases and Phosphatases

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 Phosphatases

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...

The JAK-STAT Signaling Pathway

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as SH2...

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Updated: May 15, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

Kinase dysfunction and kinase inhibitors.

Cheryl A London¹

¹Department of Veterinary Biosciences, College of Veterinary Medicine, The Ohio State University, Columbus, OH 43214, USA. cheryl.london@cvm.osu.edu

Veterinary Dermatology

|January 22, 2013

Summary

This summary is machine-generated.

Kinase inhibitors, drugs targeting cancer-driving proteins, show promise in both human and veterinary oncology. Their application in dogs and cats is a recent development with approved treatments available.

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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

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Area of Science:

Oncology
Molecular Biology
Pharmacology

Background:

Cancer cells exhibit dysregulated cell survival and proliferation due to molecular abnormalities.
Kinases, proteins that phosphorylate other proteins, are key regulators of critical cellular processes and are often implicated in cancer.
Targeting kinase function is a major strategy in cancer therapy, with small molecule inhibitors showing significant clinical efficacy.

Purpose of the Study:

To review the biology of protein kinase dysfunction in human and animal cancers.
To discuss the application of specific kinase inhibitors in veterinary cancer patients.
To highlight recent advances and approved kinase inhibitors for animal cancer treatment.

Main Methods:

Review of scientific literature on kinase biology and inhibitors in human and veterinary oncology.
Analysis of approved kinase inhibitors for cancer treatment in dogs.
Discussion of the role of protein kinases in cancer development and progression.

Main Results:

Kinase inhibitors have demonstrated significant clinical efficacy in human cancers.
Two kinase inhibitors, toceranib and masitinib, are approved for veterinary use in dogs.
The use of kinase inhibitors in veterinary medicine is an emerging field with potential for enhanced efficacy.

Conclusions:

Protein kinase dysfunction is a common feature of cancer in both humans and animals.
Kinase inhibitors represent a valuable therapeutic strategy for cancer treatment.
Further exploration of kinase inhibitors in combination regimens may enhance their biological activity in veterinary oncology.