Tag: Autophagy

AUTAC4 is a Mitochondria-Targeting Autophagy-Targeting Chimera (AUTAC)

A novel chimeric molecule, namely autophagy-targeting chimera (AUTAC), is the first degrader using the autophagy mechanism. AUTAC consists of a guanine tag and a specific binder of an intracellular target of interest. In addition, AUTAC can penetrate cell membranes, and degrade fragmented mitochondria as well as proteins. Mitochondria not...

AZD1208 is an Orally Bioavailable and Highly Selective PIM Kinases Inhibitor

Pim kinases, also known as serine/threonine kinases, have three highly homologous isoforms namely Pim-1, Pim-2, and Pim-3. And Pim-1, Pim-2, and Pim-3 are recurrent proviral integration locus in Moloney murine leukemia virus. The overexpression of Pim kinases occurs when viral inserts at this site. Pim kinases are overexpressed in...

LYN-1604 is a Potent ULK1 Activator

UNC-51 like kinase 1 (ULK1) is the mammalian homolog of ATG1. ULK1 is an autophagic initiator that may decide the subsequent cell fate. In the autophagic process, ULK1 is a component of the ULK complex that is essential for autophagy induction in different types of cancer. Additionally, characterization of ULK1 expression...

Dasatinib is an Orally Active Dual Bcr-Abl and Src Family Tyrosine Kinase Inhibitor

Src is an important member of the non-receptor protein tyrosine kinase. Furthermore, Src plays a key role in the regulation of many cells through the extracellular ligand binding to the receptor and the cell adhesion molecule activation in cell cycle-specific stage. Src can affect cell adhesion, motility, proliferation, and...

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...

PR-619 is a Broad-Range DUB Inhibitor

Ubiquitination is a post-translational modification where the polypeptide ubiquitin is attached to lysine residues of substrate proteins. This process is reversible, and ubiquitin removal is orchestrated by a large family of deubiquitinating enzymes (DUBs). DUBs fall into six subfamilies based on sequence and domain similarity. Ubiquitination and deubiquitination together...

NSC 33994 is a Selective JAK2 Inhibitor

Janus kinases (JAK) play a crucial role in cytokine-mediated signal transduction. Activated JAKs tyrosine autophosphorylate and phosphorylate specific tyrosine residues on the C-terminal end. This results in the recruitment and activation of the STAT proteins. Activated STATs subsequently translocate into the nucleus where they alter specific gene transcription patterns....