Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transport vesicles, division of organelles, cytokinesis, and pathogen resistance. Dynamins are involved in scission (cleavage of the vesicle from the parent membrane) of nascent vesicles from parent membranes in eukaryotic cells. Dynamins interact directly with the lipid bilayer at the necks of clathrin-coated pits to sever and release coated vesicles. Dynamins contain five domains, including GTPase domain, middle domain, PH domain, GTPase effector domain (GED), and proline rich domain (PRD), while the dynamin-related proteins (DRPs) lack one or more of these domains or have additional domains. Dynamins and DRPs participate in a wide variety of cellular processes, including budding mitochondrial fission (mammalian Dlp1 and Saccharomyces cerevisiae Dnm1) and fusion (mammalian OPA1, S.cerevisiae Mgm1 and Schizosaccharomycespombe Msp1), vacuolar fission (S. cerevisiae Vps1), interferon-induced anti-viral protection (fish Mx proteins), plant cell cytokinesis and membrane fission (Arabidopsis thalianaDRP proteins), as well as pathogen resistance
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Ciliobrevin D is a cell-permeable, reversible, specific inhibitor of cytoplasmic dynein, blocks dynein-dependent microtubule gliding and ATPase activity while sparing kinesin dependent cellular trafficking; selectively affects retrograde transport, inhibits the bidirectional transport of organelles along sensory axons and impairs NGF-mediated regulation of growth cones and axon branches, disrupts spindle pole focusing and kinetochore-microtubule attachment at 10-40 uM
Dynein2-IN-37 (Ciliobrevin analog 37) is a potent, selective cytoplasmic dynein 2 ATPase activity antagonist with IC50 of 11 uM, shows weak inhibition for dynein 2 (IC50=280 uM); directly targets the heavy chains of both dynein isoforms and explore the structure-activity landscape of these inhibitors in vitro and in cells; inhibits retrograde ciliary GLI2 transport more strongly than ciliobrevin A, effectively disrupts Hedgehog signaling, intraflagellar transport, and ciliogenesis.
Dynarrestin is a novel inhibitor of cytoplasmic Dyneins 1 and 2, acts reversibly to inhibit cytoplasmic dynein 1-dependent microtubule binding and motility in vitro without affecting ATP hydrolysis; rapidly and reversibly inhibits endosome movement in living cells and perturbs mitosis by inducing spindle misorientation and pseudoprometaphase delay; reversibly inhibits cytoplasmic dynein 2-dependent intraflagellar transport (IFT) of the cargo IFT88 and flux of Smo within cilia without interfering with ciliogenesis and suppresses Hh-dependent proliferation of neuronal precursors and tumor cells.
Dynole 34-2 is a potent dynamin GTPase inhibitor with IC50 of 6.9 and 14.2 uM for full-length dynI and dynII GTPase activity, respectively; induces cytokinesis failure at the point of abscission, consistent with inhibition of dynamin while not affecting other cell cycle stages in cancer cells; disrupt midbody localization of calcineurin but not phospho-dynII and γ-tubulin, inhibits growth in a range of cancer cell lines with IC50 of 4.0 to 36.7 uM in MTT assays; Dynole 34-2 is a novel antimitotic compound acting specifically at the abscission stage.
Pyrimidyn 7(Pyrimidyn7) is a potent, dual-action dynamin GTPase activity inhibitor with IC50 of 1.1 uM/1.8 uM for dynamin I/dynamin II respectively, competitively inhibits both GTP and phospholipid interactions with dynamin; reversibly inhibits CME of both transferrin and EGF in a number of non-neuronal cell lines as well as inhibiting synaptic vesicle endocytosis (SVE) in nerve terminals; blocks clathrin-mediated endocytosis (CME).
Bis-T-23 (Ryngo 1-23)is a small molecule that stimulates actin-dependent dynamin oligomerization and promotes dynamin GTPase activity, increases actin polymerization in injured podocytes; ameliorates or prevents proteinuria and diminishes mesangial matrix expansion in diverse genetic and chronic models of glomerular disease in rodents, improves renal health in diverse models of both transient kidney disease and CKD.
DRP1 inhibitor 4
DRP1 inhibitor 4 is a selective, small molecule inhibitor of the mammalian mitochondrial division dynamin, DRP1 with IC50 of 1.0 uM, shows no activity against OPA1 and DYN1 (IC50>100 uM).
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