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WEE1 Kinase Inhibitors for the Treatment of Glioblastoma
Wee1 kinase participates in the G2-M checkpoint to prevent mitosis in the presence of DNA damage and therefore may play an important role in drug resistance to DNA alkylating agents, by allowing tumor cells to repair DNA damage prior to mitosis. Inhibition of the Wee1 kinase is known to potentiate the effect of chemotherapy in a variety of tumor...
Published: 11/30/2023
|
Inventor(s):
Philip Reigan
,
Christopher Matheson
Disease Areas
Oncology
Category(s):
Therapeutics
Inhibitors of Wee1 kinase for pediatric and adult cancers
The Wee1 kinase participates in the G2-M checkpoint to prevent mitosis in the presence of DNA damage and therefore may play an important role in drug resistance to DNA alkylating agents, by allowing tumor cells to repair DNA damage prior to mitosis. Inhibition of the Wee1 kinase is known to potentiate the effect of chemotherapy in a variety of tumor...
Published: 11/30/2023
|
Inventor(s):
Philip Reigan
,
Donald Backos
,
Christopher Matheson
,
Kimberly Casalvieri
Disease Areas
Oncology
Category(s):
Therapeutics
Small Molecule Inhibitors of STAT3 for the Treatment of AML
Signal transducer and activator of transcription-3 (STAT3) is involved in multiple cancer types and inflammatory diseases. STAT3 is particularly important in leukemic stem cell proliferation and AML progression, which makes it an attractive target for therapeutic inhibition. A team of investigators at the University of Colorado led by Dr. Reigan...
Published: 11/30/2023
|
Inventor(s):
Philip Reigan
,
Donald Backos
,
Christopher Matheson
,
Steffanie Furtek
Disease Areas
Oncology
Category(s):
Therapeutics
Oxindol-3-ylidene inhibitors of AMP-activated protein kinase (AMPK)
The oral tyrosine kinase inhibitor sunitinib, used in the clinic to treat advanced renal cell carcinoma and gastrointestinal stromal tumors, is a potent AMPK inhibitor. However, sunitinib has been associated with clinical cardiac toxicity through non-specific binding to the AMPKα2 isoform. Dr.
Philip Reigan
and a team of researchers have revealed...
Published: 11/30/2023
|
Inventor(s):
Philip Reigan
,
Donald Backos
,
Christopher Matheson
,
Craig Jordan
Disease Areas
Oncology
Category(s):
Therapeutics
Development of AMPK PROTAC degraders and their hypoxia-activated prodrugs
Dr.
Philip Reigan
and a team of researchers are developing novel oxindole-based inhibitors of 5' AMP-activated protein kinase (AMPK), a kinase with a critical function in metabolic regulation. An extension of developing AMPK inhibitors is to couple these inhibitors to a the cereblon (CRBN)-binding ligand, pomalidomide, as a PROteolysis TArgeting...
Published: 5/9/2023
|
Inventor(s):
Philip Reigan
Disease Areas
Oncology
Category(s):
Therapeutics
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