RLA-5331 is an Iron Activator Containing Anti-androgen
Prostate cancer (PCa) is one of the most prevalent malignancies in the world. Depending on the grade of cancer, a variable percentage of these patients experience progression to castration-resistant prostate cancer (CRPC) within 10 years. However, CRPC can develop into metastatic castration-resistant prostate cancer (MCRPC). Research has shown that...
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...
ARD-69 is a Potent PROTAC Androgen Receptor Degrader
Androgen receptor (AR) is a ligand-dependent nuclear transcription factor and a member of the steroid hormone nuclear receptor family. In fact, AR has many biological functions and can control the expression of specific genes. AR can interact with its natural ligands 5α-Dihydrotestosterone (DHT) binds to testosterone. Importantly, AR signal...
KGP94 is a Selective Inhibitor of Cathepsin L for Cancer Research
Cathepsin L is a lysosomal cysteine protease. Particularly, it may play a key role in various biological and disease processes through intracellular and extracellular protein degradation. Obviously, cathepsin L is a ubiquitously expressed cysteine protease located in lysosomes under normal conditions. However, cancer cells secrete cathepsin L to help...
Rucaparib (AG014699) is an Orally Active PARP-1/2/3 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 presents 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 can...
Indoximod, An Immunometabolic Adjuvant, is an IDO Pathway Inhibitor
Indoleamine 2,3-dioxygenase (IDO) is an enzyme of interest in immuno-oncology. It has immunosuppressive effects that result from its role in tryptophan catabolism. IDO1 catalyzes the initial rate-limiting step in the degradation of the essential amino acid tryptophan along the kynurenine pathway. IDO inhibits a tryptophan sufficiency signal that stimulates...
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...