CAM833 is a Potent BRCA2-RAD51 Interaction Orthosteric Inhibitor
RAD51, an essential eukaryotic DNA recombinase, promotes homologous pairing and strand exchange during homologous recombination (HR) and the recombinational repair of double-strand breaks. RAD51 protein is recruited onto the DNA break by BRCA2 and forms homopolymeric filaments that invade the homologous chromatid and use it as a template for...
Simmiparib is An Orally Active PARP1/2 Inhibitor
Poly (ADP-ribose) polymerase (PARP), a family of proteins, is involved in various cellular processes such as DNA repair and programmed cell death. PARP is present in the cell nucleus. It consists of a DNA-binding domain, a caspase-cleaved domain, an auto-modification domain, and a catalytic domain. In particular, the protein...
DC-S239 is a Selective SET7 Inhibitor With Anti-Cancer Activity
SET7 is a protein lysine methyltransferase (PKMT), which methylates a plethora of proteins and regulates diverse biological processes. Meanwhile, SET7 plays a significant role in transcriptional regulation, cell cycle control, differentiation, DNA repair, and DNMT1 stability. Specifically, researches show that SET7 is closely associated with various diseases. Particularly, SET7...
Actinomycin D Inhibits DNA Repair and Induces Autophagy
Actinomycin D is isolated from Streptomyces species, containing a phenoxazine chromophore and two cyclic pentapeptide lactone rings. Besides, Actinomycin D can inhibit DNA repair, DNA-directed RNA synthesis, or DNA synthesis via binding to double-stranded DNA and the phenoxazine chromophore inserting DNA bases. Therefore, it acts as a DNA intercalator and...
D-I03 is a Selective RAD52 Inhibitor
DNA repair is very important for the maintenance of genome integrity in all organisms. Different exogenous agents or genotoxic products of metabolism cause multiple DNA repair systems evolved to eliminate a broad variety of DNA lesions. In normal cells, the specificities of different DNA repair mechanisms overlap to assure...
Niraparib is an Orally Active PARP Inhibitor
Poly (ADP-ribose) polymerases (PARPs) are a family of related enzymes. PARP shares the ability to catalyze the transfer of ADP-ribose to target proteins. PARP plays an important role in various cellular processes, including modulation of chromatin structure, transcription, replication, recombination, and DNA repair. Niraparib (MK-4827) is a potent PARP...
AOH1160, an Orally Active PCNA Inhibitor, Exhibits Efferctive Anti-cancer Activity with Low Toxicity
Proliferating cell nuclear antigen (PCNA) is an auxiliary protein of DNA polymerase delta. PCNA plays an essential role in regulating DNA synthesis and repair and is indispensable to cancer cell growth and survival. In this study, Long Gu, et al identified a potent PCNA inhibitor AOH1160 by targeting a...