Compounds that Inhibit QSOX1 Enzymatic Activity

Description

Despite tremendous scientific progress and treatment advances, cancer continues to be the leading cause of death worldwide, with global burden by 2030 estimated to be 21.4 million new diagnoses and 13.2 million deaths (IARC). Because invasion and metastasis are arguably the most dangerous characteristics of cancer, therapeutics that suppress these characteristics could be very valuable.

Quiescin sulfhydryl oxidase1 (QSOX1) is an enzyme that is highly overexpressed in many tumor types but not in normal cells or tissue. Research has shown that QSOX1 over-expression plays an important role in tumorigenesis, cell invasion/migration and metastases. Suppression of QSOX1 protein expression leads to reduced tumor cell growth and invasion in vitro and in vivo. 

Researchers at Arizona State University have discovered that QSOX1 is a tractable anti-neoplastic drug target and have identified and characterized compounds which inhibit the enzymatic activity of QSOX1. These compounds slow the growth and invasion of pancreatic, renal and breast cancer cells in murine models of cancer, likely by disrupting the extracellular matrix and tumor-stroma interaction. Further, these compounds could sensitize tumors such that other therapeutic agents are more effective or could be used in lower doses.

Currently, no other small molecule inhibitors exist for QSOX1, making these “first-in-class”.  Since surgery would cure cancer if it did not metastasize, drugs that suppress extracellular matrix deposition and metastases represent a new class of anti-neoplastic agent. 

Potential Applications

•       Treatment or prognosis of tumors that over-express QSOX1 (non-limiting tumor types: pancreatic, lung, colon, breast and prostate tumors) 

o       Reduce/slow the increase in tumor mass 

o       Diminish tumor cell viability 

o       Suppress metastasis 

o       Limit/prevent/inhibit worsening/reduce recurrence of symptom development 

o       Increase survival time

Benefits and Advantages

•       Less expensive than biologics

•       Can be modified to increase bioavailability

•       Suppresses metastatic tumor growth

For more information about the inventor(s) and their research, please see
Dr. Laeke's directory webpage 

Case ID:
M15-214LC
Published:
08-16-2016
Last Updated:
05-21-2018

Patent Information

App Type:
Provisional
Serial No.:
62/218,732
Patent No.:
File Date:
09-15-2015
Issue Date:
10-15-2018
Expire Date:
09-15-2016

For More Information, Contact