Tag: PARP

Xentuzumab is a Monoclonal Antibody That Targets IGF Ligands IGF1 and IGF2

IGF, an insulin-like growth factor, regulates cell growth, proliferation, and survival. The IGF system is made up of IGF1, IGF2, insulin, and corresponding receptors. It transmits abnormal signals to cause a variety of cancers. One that stands out is castration-resistant prostate cancer. IGF can either up-regulate IGF-binding proteins or...

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...

Rucaparib is a PARP Inhibitor

PARP is a family of proteins involved in many cellular processes, such as DNA repair, genomic stability, and programmed cell death. At least 18 members of the PARP family are encoded by different genes and have homology in conserved catalytic domains. Specifically, PARPs play an important role in various...

DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP

Proteolysis targeting chimera (PROTAC) is a bifunctional small molecule. Interestingly, dual PROPACs are dual-targeted degradation molecules that combine the concepts of PROTAC and dual-targeting. Dual PROPACs degrade two completely different pathway targets while simultaneously taking advantage of both PROTAC and dual-target drugs. Thus, dual PROPACs not only achieve the...

BSJ-4-116 is a Highly Potent and Selective PROTAC Based CDK12 Degrader

CDKs are serine/threonine protein kinases. They play major roles in regulating many different aspects of mammalian cellular function, most notably cell cycle and transcription. CDK12 is an emerging therapeutic target due to its role in regulating the transcription of DNA-damage response (DDR) genes. For example, ovarian and triple-negative breast...

Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor

PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...

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...