Retro-2 is a Selective Inhibitor of Retrograde Protein Trafficking

Viruses critically depend on host cellular factors to establish a productive infection. Retro-2 is an inhibitor of endosome-to-Golgi retrograde transport of the plant toxin ricin and bacterial Shiga toxin. However, the efficacy of Retro-2 also has been examined against enveloped viruses, such as filoviruses. As a result, Retro-2 is...

FAPI-46 is a Quinoline-Based Fibroblast Activation Protein (FAP)-Targeted Radiotracer

The proline-selective serine protease fibroblast activation protein (FAP) is a type II transmembrane glycoprotein. It is related to the dipeptidyl peptidases (DPPs) DPP2, DPP4, DPP8 and DPP9 and furthermore related to the endopeptidase prolyl oligopeptidase (PREP). FAP combines DPP and endopeptidase activities. FAP is not detectable in most healthy...

LDN193189 is a Selective BMP Type I Receptor Inhibitor

Fibrodysplasia ossificans progressiva (FOP) is a congenital disorder of progressive. It is widespread postnatal ossification of soft tissues and is without known effective treatments. A recent study identified heterozygous mutations in ACVR1, the gene encoding the BMP type I receptor ALK2, in all affected members from seven families. BMP...

Stafib-1 is the First Selective Inhibitor of the STAT5b SH2 Domain

The transcription factor STAT5A/B controls leukemic cell survival and disease progression. Especially, STAT5B as major STAT5 isoform driving BCR/ABL+ leukemia. Besides, STAT5B enables transformation by suppressing IFN-α/γ, thereby facilitating leukemogenesis. STAT5b might serve as an anticancer target in ductal pancreatic adenocarcinoma. Stafib-1 acts as the first selective inhibitor of...

PF-06260414 is an Orally Active and Nonsteroidal Selective Androgen Receptor Modulator

The Androgen receptor (AR) is a nuclear receptor. The Androgen receptor is a DNA binding transcription factor that regulates gene expression. Specifically, androgen-regulated genes are essential for the development and maintenance of male sexual phenotypes. Besides, androgen causes slow maturation of bone, but the more effective maturation comes from...

LC-2 is a First-in-Class PROTAC-Based KRAS G12C Degrader

KRAS gene is one of the most frequently mutated oncogenes in cancer. KRAS encodes a small, membrane-bound GTPase that relays signals from receptor tyrosine kinases (RTKs). It promotes cell proliferation, cell differentiation, or cell survival. In normal cells, KRAS functions as a molecular switch, cycling between an inactive, GDP-bound “off” state and...

DC_AC50 is a Dual inhibitor of Atox1 and CCS (Copper Chaperones)

Copper is a redox-active transition metal critical for most living organisms. At the same time, it serves as a catalytic cofactor for enzymes. Those enzymes play roles in antioxidant defense, iron homeostasis, cellular respiration, and a variety of biochemical processes. However, intracellular free copper may exhibit toxic side effects....