Bruton's tyrosine kinase as anti-cancer drug target

US11149092B2 · kind B2 · utility

Assignee

• The Research Foundation for The State University of New York · US

Inventors

• Douglas S. Conklin · Huntington Bay, US
• Cheryl L. Eifert · Watertown, US
• Antonis Kourtidis · St. Augustine, US
• Xianhui Wang · Albany, US
• Leila Kokabee · Albany, US

Key dates

• Filing date: May 1, 2017
• Grant date: Oct 19, 2021
• Expiry date: May 1, 2037

Classification

• Technology area (CPC G): Physics
• CPC primary: G01N2333/9121
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Receptor protein kinases (RPTKs) transmit extracellular signals across the plasma membrane to cytosolic proteins, stimulating formation of complexes that regulate key cellular functions. Over 5 half of the known tyrosine kinases are implicated in human cancers and are therefore highly promising drug targets. A large-scale loss-of-function analysis of tyrosine kinases using RNA interference in the clinically relevant Erb-B2 positive, BT474 breast cancer cell line showed that Bruton's tyrosine kinase (BTK), a cytosolic, non-receptor tyrosine kinase that has been extensively studied for its role in B cell development, is required, in altered form, for BT474 10 breast cancer survival. This alternative form contains an amino-terminal extension that is also present in tumorigenic breast cells at significantly higher levels than in normal breast cells.