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Small Molecule Inhibitors of Integrin α2β1

Description:

Integrin, Thrombosis, Hemostasis, Cancer Metastasis, Wound Healing, Viral Infection, Small Molecule 

 

Inventor

William F. DeGrado, Joel S. Bennett

 

Problem

There is a need for new therapeutics that prevent cardiovascular diseases with minimal effects on normal blood clotting.  Integrin α2β1 is a good therapeutic  target since it can lead to cardiovascular diseases including stroke or myocardial infarction when overexpressed, but does not severely impair normal bleeding when under-expressed. Integrin α2β1 has been implicated in several other disease states including cancer metastasis, wound healing, viral infections (such as rotaviruses), and glomerular injury. Therefore, novel inhibitors of integrin α2β1 could have potential benefits in preventing cardiovascular disease, as well as in several other therapeutic applications.

 

 

Solution

Drs. DeGrado and Bennett led the development of novel small molecule inhibitors of integrin α2β1, based on a prolyl-2,3-diaminopropionic acid (DAP) scaffold.  These compounds have been shown to inhibit human platelet adhesion and arterial thrombosis in a mouse model with IC50 values in the nanomolar range.

  

Advantages

• Inhibition of integrin α2β1

• IC50 values in nanomolar range

 

 

Applications

• Cardiovascular diseases

• Cancer metastasis

• Wound healing

• Viral infections

• Glomerular injury

 

 

Stage of Development

Primary human cells and mouse model

 

Intellectual Property

8,987,306

8,258,159

7,910,609

 

 

Reference Media

Miller MW et al. Proc Natl Acad Sci USA, 2009 106(3): 719-24.

Choi S et al. J Med Chem, 2007 50(22): 5457-62.

Borza CM et al. J Am Soc Nephrol, 2012 23(6): 1027-38.

 

Desired partnerships

• License

Co-development

 

 

Dockets # U4878 and R3789 


Patent Information:
For Information, Contact:
Jeffrey James
TLO
University of Pennsylvania
215-746-7041
jeffja@upenn.edu
Inventors:
William Degrado
Joel Bennett
Keywords: