Tag: PARP

CMLD-2 is Inhibits HuR and Induces Apoptosis

Hu antigen R (HuR) is an RNA binding protein. Specifically, Its overexpression in human cancer is associated with aggressive disease, drug resistance, and poor prognosis. HuR is highly abundant in many types of cancer and promotes tumorigenesis through cancer-related mRNA interactions. Besides, HuR has related to the regulation of...

Senaparib is a Selective and Orally Active PARP1/2 Inhibitor

Poly(ADP-ribose) polymerase (PARP) is an important protein in DNA repair pathways especially the base excision repair. . PARP proteins compose of two ribose moieties and two phosphates per unit polymer. PARP inhibitors represent a successful example of precision medicine as the first drugs targeting DNA damage response to have...

AZ9482 is a Triple PARP1/2/6 Inhibitor

PARPs are implicated in a variety of cellular metabolic processes including DNA-damage repair and mitotic spindle formation. In particular, PARP1 is essential in repairing DNA single- and double-strand breaks. For example, PARP1 Inhibitor Olaparib is an effective synthetic lethal strategy in cancer. Recently, scientists reported a triple PARP1/2/6 inhibitor,...

BETd-260 is a Potent PROTAC BET Degrader

The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...

dTRIM24 is a Selective PROTAC Degrader of TRIM24

TRIM24 is a multidomain protein characterized as a co-regulator of transcription. Especially, dTRIM24 acts as a chemical probe of an emerging cancer dependency. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. TRIM24 has been posited as a dependency in numerous cancers,...

SC-43 is a Potent and Orally Active SHP-1 Agonist and STAT3 Phosphorylation Inhibitor

Cholangiocarcinoma (CCA) is the second most common hepatic malignancy after hepatocellular carcinoma (HCC). CCAs are epithelial malignancies that arise from cholangiocytes and are aggressive behavior and advanced clinical stage. STAT3 belongs to a family of transcription factors that relay cytokine receptor-generated signals into the nucleus. STAT3 is activated by...

NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity

Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...