Microtubules are a component of the cytoskeleton, found throughout the cytoplasm. These tubular polymers of tubulin can grow as long as 50 micrometres, with an average length of 25 µm, and are highly dynamic. The outer diameter of a microtubule is about 24 nm while the inner diameter is about 12 nm. Microtubules are found in eukaryotic cells and are formed by the polymerization of a dimer of two globular proteins, alpha and beta tubulin. Tubulin is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the alpha-, beta-, gamma-, delta-, and epsilon-tubulins and a sixth family which is present only in kinetoplastid protozoa. The most common members of the tubulin family are α-tubulin and β-tubulin, the proteins that make up microtubules. Microtubules are very important in a number of cellular processes. They are involved in maintaining the structure of the cell.
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A novel combretastatin A-4 derivative and tubulin polymerization inhibitor that strongly stanches tumour blood flows and inhibits growth of tumours developing in various tissues and organ; a vascular-disrupting agent under clinical investigation combined with cisplatin/docetaxel or carboplatin/paclitaxel in patients with advanced solid tumors.
6-MOMIPP is a novel microtubule disruptor that targets the colchicine binding site on β-tubulin, induces mitotic arrest, caspase activation and loss of cell viability of U251 glioblastoma in vitro; demonstrates broad activity against the viability of multiple glioblastoma, melanoma and lung carcinoma cell lines; effectively inhibits growth of subcutaneous and intracerebral tumors without causing general toxicity in mice bearing human U251 glioblastoma xenografts .
CCB02 (CCB 02) is a specific small molecule inhibitor of CPAP-tubulin interaction with IC50 of 0.689 uM in AlphaScreen assay, selectively binds at the CPAP binding site of tubulin; does not inhibits a panel of cell cycle- and centrosome-related kinases; impairs proliferation of cells with centrosome amplification, activates extra centrosomes to nucleate enhanced numbers of microtubules prior to mitosis, causes cells to undergo centrosome de-clustering, prolonged multipolar mitosis, and cell death; demonstrates broad anti-invasive activity in various cancer models, including tyrosine kinase inhibitor (TKI)-resistant EGFR-mutant NSCLC.
ATM-3507 (ATM3507) is a small molecule inhibitor of Tpm3.1 tropomyosin isoform, disrupts Tpm3.1-containing microfilaments in SK-N-SH cells at 5 uM; shows cancer cell cytotoxicity comparable with the first-in-class tool compound TR100, also shows a strong synergistic effect when TR100 or ATM-3507 were combined with antimicrotubule agents in both in vitro and in vivo neuroblastoma models.
TR-100 (TR100) is a specific anti-tropomyosin compound that disrupts the actin cytoskeleton via targeting of Tpm3.1-containing actin filaments; perturbs Tpm3.1-regulated actin filament depolymerisation from the barbed end without affecting the capacity of Tpm3.1 to regulate barbed end actin elongation or bind F-actin; TR-100 (TR100) is effective in vitro and in vivo in reducing tumor cell growth in neuroblastoma and melanoma models.
Avanbulin (BAL27862, BAL-27862) is a novel microtubule-destabilizing agent that potently inhibits tubulin assembly at 37¡ãC with IC50 of 1.4 uM in tubulin-binding assays; potentli bindis to unassembled tubulin with a stoichiometry of 1 mol/mol tubulin and a dissociation constant of 244¡À30 nM, BAL27862 bound to tubulin independently of vinblastine, without the formation of tubulin oligomers; inhibits tumor cell proliferation through activation of the spindle assembly checkpoint, inhibits EB1-dependent migration and invasion and promotes differentiation of glioblastoma stem-like cells both in vitro and in vivo.
VERU-111 (VERU111) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities; inhibits cell viability of human melanoma cell lines (A375, M14, and RPMI7951) with IC50 of 5-10 nM.
MP-HJ-1b is a novel potent inhibitor of microtubule and tumor cell growth, binds the colchicine pocket at the intra-dimer interface, depolymerizes microtubules and affects spindle formation; shows activities against a panel of more than 1000 human cancer cell lines with a wide variety of tissue origins, also induces the spike-like conformation of microtubules in vitro and in vivo, which is different from typical microtubule modulators; exhibits an interesting property of general cytotoxicity instead of Ras-mutant-specific killing (A549 KRAS-G12S, IC50=0.04 uM); MPHJ-1b displayed favorable pharmacological properties for overcoming tumor MDR both in vitro and in vivo.
VERU-111 analogue 13f
VERU-111 analogue 13f is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities; inhibits cell viability of human melanoma cell lines (A375, M14, and RPMI7951) with IC50 of 1-3 nM; VERU-111 analogue 13f is significantly more potent than VERU-111, exhibits a strong inhibitory effect on tumor growth in vivo.
A taxol derivative with antitumor, antiproliferative properties.
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