RUNX1 inhibition for treatment of proliferative vitreoretinopathy and conditions associated with epithelial to mesenchymal transition

A method for treating or reducing the severity of proliferative vitreoretinopathy (PVR) in a human subject comprising:

• diagnosing a PVR in a subject,
• wherein said diagnosing a PVR comprises the steps of:
• (a) providing an ocular test sample from said subject,
• (b) assaying the level of RUNX1 protein or mRNA in the test sample;
• and
• (c) diagnosing the subject as having aberrant PVR if the level of RUNX1 protein or mRNA is elevated in the test sample compared to a normal control;
• and
• administering to the subject a small molecule RUNX1 inhibitor that comprises the structure of Formula I:
• or a pharmaceutically acceptable salt or ester thereof, wherein
• each R1 is individually selected from halogen, alkyl, aryl, heteroaryl, or alkoxy,
• and R2 is selected from aryl or heteroaryl, and
• a is 0 to 4;
• Formula III:
• or a pharmaceutically acceptable salt or ester thereof, wherein
• each R1 is individually selected from halogen, alkyl, aryl, heteroaryl, or alkoxy,
• R2 is selected from aryl or heteroaryl;
• R3 is alkyl or aryl, and
• a is 0 to 4;
• or
• Formula V:
• or a pharmaceutically acceptable salt or ester thereof, wherein
• R1 is H3, NH2, or NHC (O) CH3, and
• X is CH2 or C(O).