Articles with "selective orally" as a keyword



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BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor

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Published in 2022 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.2c01267

Abstract: Despite advances in the treatment of heart failure in recent years, options for patients are still limited and the disease is associated with considerable morbidity and mortality. Modulating cyclic guanosine monophosphate levels within the natriuretic… read more here.

Keywords: orally bioavailable; selective orally; 7081 potent; pde9a inhibitor ... See more keywords
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Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.

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Published in 2023 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c01718

Abstract: Cyclin-dependent kinase 8 (CDK8), as a kinase subunit of the Mediator complex, is involved in the regulation of RNA polymerase II-mediated transcription, thereby modulating multiple signaling pathways and multiple transcription factors involved in oncogenic control.… read more here.

Keywords: discovery potent; potent selective; chemistry; orally bioavailable ... See more keywords
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Abstract LB320: Discovery and characterization of QTX3034, a potent, selective, and orally bioavailable allosteric KRAS inhibitor

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Published in 2023 at "Cancer Research"

DOI: 10.1158/1538-7445.am2023-lb320

Abstract: The RAS family of proto-oncogenes are the most frequently mutated genes in cancer, in which mutations in KRAS account for approximately 25% of all human cancers. RAS oncogenes impair the ability of RAS to convert… read more here.

Keywords: qtx3034; kras inhibitor; orally bioavailable; qtx3034 potent ... See more keywords
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Abstract LB321: Discovery and characterization of QTX3046, a potent, selective, and orally bioavailable non-covalent KRASG12D inhibitor

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Published in 2023 at "Cancer Research"

DOI: 10.1158/1538-7445.am2023-lb321

Abstract: The RAS family of proto-oncogenes are the most frequently mutated genes in cancer, in which mutations in KRAS account for approximately 25% of all human cancers. RAS oncogenes impair the ability of RAS to convert… read more here.

Keywords: qtx3046 potent; bioavailable non; krasg12d; orally bioavailable ... See more keywords