The goal of this application is to study in vivo efficacy of CT102, a newly discovered inhibitor of the OLIG2 transcription factor in animal models of glioblastoma (GBM), a highly underserved area of pharmacotherapy. In this proposal, the experienced drug discovery group at Curtana Pharmaceuticals Inc. will conduct a pre-clinical evaluation of selectivity and in vivo distribution of CT102 to determine protocols for efficacy studies in orthotopic models of GBM. CT102 will be studied at UCSD to confirm potency of newly synthesized materials, assess activity in an orthotopic model of GBM and conduct in vitro and in vivo profiling to evaluate CT102 as a sensitizer to chemo- or radiotherapy. A successful outcome may result in a potential small molecule therapeutic for GBM.
Public Health Relevance Statement: Public Health Relevance: The objective is to evaluate the efficacy of an inhibitor of the transcription factor, OLIG2 in pre-clinical animal models of glioblastoma, a disease which is a significant cause of mortality where survival is limited.
Project Terms: Adjuvant; Affect; analog; Animal Model; Area; base; Blood - brain barrier anatomy; Brain; Cancer Center; CDK2 gene; CDK4 gene; Cells; Chemosensitization; chemotherapy; Data; Disease; Drug Discovery Groups; Drug Formulations; EGF gene; Evaluation; experience; Feasibility Studies; Fund Raising; Glioblastoma; Goals; Heat-Shock Proteins 90; In Vitro; in vitro activity; in vitro Model; in vivo; in vivo Model; inhibitor/antagonist; Literature; Medical; Modeling; Molecular; Mortality Vital Statistics; Mus; novel; Outcome; Pathology; Pathway interactions; Patients; Penetration; Permeability; Pharmacologic Substance; Pharmacotherapy; Phase; Plasma; Platelet-Derived Growth Factor; pre-clinical; Protein Kinase; Proteins; Protocols documentation; public health relevance; Publishing; Radiation; Radiation therapy; Radio; Radiosensitization; Rationalization; research clinical testing; Route; Sampling; Series; Small Business Technology Transfer Research; small molecule; standard of care; stem; temozolomide; Testing; Therapeutic; transcription factor; Validation; Work
