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Novel Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (TDP1) for Treatment of Solid Tumors

Abstract: Topoisomerase 1 (TOP1) is an essential enzyme that plays a critical role in DNA transcription and replication. TOP1 inhibitors are a known class of anti-cancer agents that work to interrupt DNA replication in cancer cells, causing cell death. Since the discovery of the TOP1 inhibitor camptothecin (CPT) from plant extracts more than 60 years...

Published: 5/22/2024 | Inventor(s): Xue Zhao, George Lountos, Evgeny Kiselev, David Waugh, Yves Pommier, Terrence Burke

Keywords(s): Burke, CANCER, solid tumor, Tdp1, TOP1, Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1, Zhao

Category(s): Application > Therapeutics, Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology

Peptide Mimetic Ligands of Polo-like Kinase 1 Polo Box Domain

Abstract: Polo-like kinase 1 (Plk1) is a critical protein involved in regulation of mitosis, and aberrant expression of this kinase is found in various cancer types. Inhibition of Plk1 is currently being pursued in pre-clinical drug development for novel anti-cancer therapeutics. Plk1 contains an allosteric domain, known as the polo-box domain (PBD),...

Published: 5/22/2024 | Inventor(s): Terrence Burke, Wen-Jian Qian, Kyung Lee, Jung-Eun Park, James Kelley

Keywords(s): Burke, CANCER, mitosis, Peptide Inhibitor, polo-box domain (PBD), Polo-like kinase 1 (Plk1), therapeutic

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology, Application > Therapeutics

Peptide Mimetic Ligands of Polo-like Kinase 1 Polo Box Domain (“Plk1 PBD Portfolio”)

Published: 5/22/2024 | Inventor(s): Terrence Burke, Jung-Eun Park, Wen-Jian Qian, Fa Liu, Kyung Lee

Keywords(s): Burke, CANCER, mitosis, Peptide Inhibitor, polo-box domain (PBD), Polo-like kinase 1 (Plk1), therapeutic

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology, Application > Therapeutics