Tag: Autophagy

GPP78 is a Nampt Inhibitor and an Autophagy Inducer

Nicotinamide phosphoribosyltransferase (NAMPT) is an enzyme that catalyzes the synthesis of nicotinamide mononucleotide (NMN) from nicotinamide (NM) and PRPP. Therefore, NAMPT plays an important role in the cyclic biosynthetic pathway of nicotinamide adenine dinucleotide (NAD). Especially, NAMPT acts as an extracellular proinflammatory cytokine, able to induce cellular expression of...

CA-5f is a Late-Stage Macroautophagy (Autophagy) Inhibitor for NSCLC Treatment

Currently, discovery of small-molecule modulators of autophagy has become a popular therapy for cancer treatment. A study from Lu Zhang has discovered and identified a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion, CA-5f. Autophagy plays essential roles in various normal cellular processes, including cell proliferation, ageing, and to...

MRT67307 Blocks mTOR-Dependent Autophagy by Inhibiting ULK1 Kinase

Yesterday, I introduced a dual IKKε/TBK1 inhibitor MRT67307. Studies have showed that MRT67307 plays a significant role in innate immunology. Not only this, a study from Katy J. Petherick drew a conclusion that MRT67307 blocked mTOR-dependent autophagy by inhibiting ULK1 kinase. ULK1, is believed to be specific for autophagy....

S130, Targeting ATG4B, Inhibits Autophagy and Activates Apoptosis in Colorectal Colon Cancer

Autophagy is an evolutionarily conserved and stress-responsive catabolic process. Particularly, cellular components and damaged organelles are sequestered within autophagosomes for lysosomal degradation. Autophagy is a multi-step process. Autophagosome biogenesis requires 2 ubiquitin-like conjugation systems: the Atg12-Atg5 and the Atg8–phosphatidylethanolamine (PE) systems. Importantly, the cysteine protease ATG4B is a key...

SLLN-15 Activates Autophagy in Triple-Negative Breast Cancer (TNBC)

As more active compounds found in Triple-negative breast cancer (TNBC), this kind of malignant tumor has received more and more attention. Our previous article “IITZ-01 as a Potent Lysosomotropic Autophagy Inhibitor” described the good efficacy of IITZ-01 in TNBC. Today, I would like to introduce another novel small molecule...

IITZ-01 as a Potent Lysosomotropic Autophagy Inhibitor

Triple-negative breast cancer (TNBC) lacks the expression of estrogen receptor (ER) and progesterone receptor (PR). Moreover, human epidermal growth factor receptor overexpression is also absent. The morbidity of TNBC accounts for ~15% of all breast cancers patients. Unfortunately, compared with other breast cancer types, this type of breast cancer...