Category: Prostate Cancer

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...

XL092 is a Potent Axl, Mer and C-Met kinase Inhibitor

Human Axl belongs to the TAM subfamily of receptor tyrosine kinases that includes Mer. TAM kinases contain two immunoglobulin-like domains and two fibronectin type III domains. Many cancer cells exhibit overexpressed Axl. And it is initially cloned from patients with chronic myelogenous leukemia. Axl has been associated with cancers...

Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor

Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...