Abstract: A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
Abstract: A method of treating cancer in a subject in need thereof includes administering to the subject therapeutically effective amounts of a PP2A activator and a protein kinase inhibitor.
Type:
Grant
Filed:
June 23, 2016
Date of Patent:
August 18, 2020
Assignees:
CASE WESTERN RESERVE UNIVERSITY, ICHAN SCHOOL OF MEDICINE AT MOUNT SINAI
Inventors:
Narla Goutham, Michael Ohlmeyer, Daniel McQuaid
Abstract: Disclosed is an expression regulatory system for cell-specific transcription (expression) of a protein of interest, for example a cell cycle inducer that reactivates proliferation in adult or neonatal cardiomyocytes or insulin-producing beta cells. The expression regulatory system comprises a first nucleic acid that encodes a microRNA recognition element that specifically binds a target cell miR, and a translation suppressor protein; and a second nucleic acid that comprises a suppressor protein interaction motif that binds the translation suppressor protein, and a gene that encodes a protein of interest. When a cell of interest is co-transfected with the first and second nucleic acids of the system, the protein of interest expressed in a cell-specific fashion.
Type:
Application
Filed:
March 15, 2019
Publication date:
July 4, 2019
Applicant:
ICHAN SCHOOL OF MEDICINE AT MOUNT SINAI
Abstract: A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
Type:
Application
Filed:
September 8, 2016
Publication date:
September 6, 2018
Applicant:
Ichan School of Medicine at Mount Sinai