Shanghai Institute of Materia Medica of the Chinese Academy of Sciences has disclosed phthalazinone or quinazolinone derivatives acting as poly(ADP-ribose) polymerase (PARP) inhibitors reported to be useful for the treatment of cancer.
Researchers have developed and tested a taurultam-derived oxathiazine compound, GP-2250, for the potential treatment of ovarian cancer. Taurolidine, a substance derived from the amino acid taurine, has been shown to have antiproliferative and antineoplastic activity in vitro and in vivo against various cancer types. GP-2250 was tested in vitro in several ovarian cancer cell lines, as well as in vivo as a monotherapy and in combination with standard-of-care drugs and PARP inhibitors.
Researchers from the Johns Hopkins University School of Medicine have hypothesized that LP-184 could synergize with the PARP inhibitor rucaparib, which avoids DNA repairing in tumor cells, for the treatment of atypical teratoid rhabdoid tumor.
Researchers from Federation University Australia and affiliated organizations have reported data from a study that aimed to assess the therapeutic efficacy of the poly (ADP-ribose) polymerase (PARP) inhibitor olaparib in a large animal model of pulmonary fibrosis.
Achieving proof of concept and a substantial clinical benefit with its PARP inhibitor stenoparib in advanced recurrent ovarian cancer, Allarity Therapeutics Inc. stopped a phase II trial and is preparing for a registrational study for what is now the company’s only internal drug candidate.
Ariceum Therapeutics GmbH has received approval from the U.K.'s Medicines and Healthcare products Regulatory Agency (MHRA) to conduct a phase I trial (CITADEL-123) of 123I-ATT-001, its iodine-123 labeled PARP inhibitor, in patients with recurrent glioblastoma. The study is expected to begin in the U.K. in June of 2024.
Researchers have identified NIMA-related kinase 1 (NEK1) as a potential therapeutic target driving tumor growth. It was identified using Turbine Ltd.’s Simulated Cell platform when they simulated perturbations in the DNA damage response pathways. NEK1 is involved in DNA damage response, cell cycle and mitosis.
Gilead Sciences Inc. has identified protein mono-ADP-ribosyltransferase TIPARP (PARP-7; ARTD14) inhibitors reported to be useful for the treatment of cancer.
Wigen Biomedicine Technology (Shanghai) Co. Ltd. has synthesized compounds acting as poly(ADP-ribose) polymerase (PARP; ARTD) inhibitors, preferably PARP-1, reported to be useful for the treatment of cancer.
To identify candidate therapeutic targets for cancers with SF3B1 hotspot mutations, drug-sensitivity screening of an in-house library of 80 small-molecule inhibitors resulted in the identification of a series of candidate SF3B1 mutant (SF3B1[MUT]) synthetic lethal drugs that led to significant reduction of survival in SF3B1(K700E) cells.
