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Updated: May 16, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Mini-review: bmx kinase inhibitors for cancer therapy
John S Jarboe1, Shilpa Dutta, Sadanandan E Velu
1Department of Radiation Oncology, The University of Alabama at Birmingham, 619 19th St. South, HSROC 2232C, Birmingham, AL 35249, USA.
Abstract:
Kinase inhibitors are among the fastest growing class of anti-cancer therapies. One family of kinases that has recently gained attention as a target for treating malignant disorders is the Tec kinase family. Evidence has been published that one member of this family; the Bmx kinase, may play a role in the pathogenesis of glioblastoma, prostate, breast and lung cancer. Bmx has also shown potential as an anti-vascular therapy in combination with radiation or as a sensitizer to chemotherapeutic agents. Therefore, several companies such as Pharmacyclics, Avila Therapeutics, Merck and Co., Metaproteomics, IRM, and Moerae Matrix have developed compounds or peptides that function as Bmx kinase inhibitors. These companies have subsequently been issued patents for these inhibitors. Additionally, it has been shown that current clinical stage EGFR inhibitors can irreversibly inhibit Bmx, suggesting these compounds might be rapidly moved to clinical trials for other malignancies. This review will discuss current patents issued since 2009 that contain data specifically on inhibition of the Bmx kinase, and will also discuss the scientific literature that suggests their potential application as therapeutics in the treatment of the aforementioned malignancies.
Insights
Bmx kinase inhibitors show promise for treating glioblastoma, prostate, breast, and lung cancers. Recent patents and literature highlight their therapeutic potential, including combination therapies and repurposing of EGFR inhibitors.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Kinase inhibitors are a rapidly expanding class of anti-cancer drugs.
- The Tec kinase family, particularly Bmx kinase, is emerging as a therapeutic target for various cancers.
- Bmx kinase involvement is implicated in glioblastoma, prostate, breast, and lung cancer pathogenesis.
Purpose of the Study:
- To review patents issued since 2009 detailing Bmx kinase inhibition.
- To discuss scientific literature on the therapeutic potential of Bmx kinase inhibitors.
- To explore Bmx kinase as a target for anti-cancer therapies, including anti-vascular and chemosensitizing applications.
Main Methods:
- Patent literature review focusing on Bmx kinase inhibitors.
- Scientific literature analysis of Bmx kinase's role in cancer.
- Examination of existing EGFR inhibitors for potential Bmx kinase inhibition.
Main Results:
- Several companies have patented Bmx kinase inhibitors.
- Bmx kinase inhibition shows potential in preclinical cancer models.
- Existing EGFR inhibitors may offer a route for rapid clinical development against Bmx-related malignancies.
Conclusions:
- Bmx kinase is a validated therapeutic target for multiple cancers.
- Patented inhibitors and repurposed EGFR inhibitors represent promising avenues for Bmx-targeted cancer therapy.
- Further research into Bmx kinase inhibitors could lead to novel anti-cancer treatments.
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