Tag: PARP

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...

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...

FR 180204 is an ATP-competitive and Selective ERK Inhibitor

An extracellular signal-regulated kinase (ERK) is a serine/threonine-protein kinase of the mitogen-activated protein kinase superfamily. Selective inhibition of ERK represents a potential approach for the treatment of cancer and other diseases. Simultaneous targeting of multiple effectors such as RAF, MEK, and ERK offers the potential for enhanced efficacy while...

CSRM617 is a Transcription Factor ONECUT2 Inhibitor for Prostate Cancer

The transcription factor ONECUT2 (OC2) is a master regulator of androgen receptor networks in mCRPC (metastatic castration-resistant prostate cancer ). OC2 acts as a survival factor in mCRPC models. OC2 is a potential drug target in the metastatic phase of aggressive PC. CSRM617,  a well-tolerated novel small-molecule inhibitor of...

ML367 is an ATAD5 Stabilization Inhibitor

DNA damage is an abnormal chemical structure in DNA, it undergoes DNA repair. DNA repair is a process to identify and correct DNA damage. If the process fails, irreparable DNA damage may happen. Consequently, this may lead to malignant tumors. ATAD5 (ATPase family AAA domain-containing protein 5) is a...

NMS-P515 is an Orally Active and Stereospecific PARP-1 Inhibitor

Poly (ADP-ribose) polymerase-1 (PARP-1) plays an important role in signaling and repair of DNA single strand breaks. PARP-1 is a well-established target in cancer therapy, as testified by the number of marketed drugs applied in the treatment of breast and prostate cancer. A study from Gianluca Papeo discovered and...