Tag: PARP

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...