eventually leading to autophagy induction.Biologically,HA-1141 suppresses growth and survival of cultured lung cancer cells and tumor growth in in vivo xenograft lung cancer models at a well-tolerated dose.Taken together,our study has identified a small molecule compound with the dual activities of ...
In summary, the molecule ABBV-467 is a highly potent and selective MCL-1 inhibitor that demonstrates robust inhibition of tumor growth in in vivo models of hematological malignancies. The macrocyclic compound exhibits a short half-life in humans, a design feature that we implemented as a means ...
(MUC16),mesothelinand others which promote peritoneal implantation should have been assessed. Someadhesion moleculessuch asintercellular adhesionmolecule (ICAM) might be influenced by metformin.Germeyer et al. (2011)have noticed that metformin increased and insulin decreased, but not beyond reasonable ...
The role of autophagy in cancer stem cells remains unclear. Accumulating evidence suggests that self-renewal, pluripotency and differen- tiation of stem cells depend on autophagy activity25. Autophagy is tightly regulated by the autophagy-related (ATG) genes and epigenetic machinery that involves post...
It has been reported that AIM may indirectly regulate inflammation or phagocytosis by binding the targets with toll-like receptors (TLRs) or scavenger receptors in pattern recognition receptors (PRRs) [4]. Meanwhile, with the synergistic effect of CD36, AIM can enhance autophagy and retard ...
Targeting Cullin-RING ligases by MLN4924 induces autophagy via modulating the HIF1-REDD1-TSC1-mTORC1-DEPTOR axis. MLN4924, a newly discovered small molecule inhibitor of NEDD8-activating enzyme (NAE), inactivates Cullin-RING E3 ubiquitin Ligases (CRLs) by blocking cullin neddylation. As a result...
natural logarithmic transformation of reactive hyperemia peripheral arterial tonometry index; ICAM-1, intercellular adhesion molecule 1; MCP-1, monocyte chemoattractant protein-1; VCAM-1, vascular cell adhesion protein 1; T1DM, type 1 diabetes mellitus; HUVEC, human umbilical vein end...
Recently, Carr et al.21 reported an intriguing action of bafilomycins on autophagy. They suggested that bafilomycin I (BFI), which has the conjugated D17,18, D19,20 diene moiety in the side chain part, stimulated autophagy, while other bafilomycins blocked autophagosomal degradation. As BFL ...
autophagy-related cell death in some malignant cells.11–14 Therefore, the development and use of small- molecule autophagic inducers is an emerging approach for treatment of cancers, especially where they have become apoptosis resistant.15 We have previously identified a small-molecule, saikosa- ...
Small Molecule Inhibitors of DNA Ligases The ultimate purpose of NHEJ is to facilitate DNA ligation, therefore DNA ligases are also considered attractive therapeutic targets. An in silico screen for small molecules that bound the catalytic domain of DNA ligase I yielded a number of potential DNA li...