Disease relevance of NSC376450

• The combined effect of the microtubule inhibitor tubulozole and gamma-irradiation has been investigated in vivo in subcutaneous MO4 fibrosarcomas and Lewis Lung carcinomas [1].

High impact information on NSC376450

• Effects of tubulozole on the microtubule system of cells in culture and in vivo [2].
• Inhibitors of protein biosynthesis, however, did not show synergistic activity with tubulozole [3].
• 2. Functional studies demonstrated that vincristine, tubulozole, podophyllotoxin, and demecolcine inhibited nAChR-stimulated catecholamine release noncompetitively and in a concentration-dependent manner, with IC50 values of 3 (1-10), 5 (2-10), 8 (4-15), and 19 (9-39) microM, respectively [4].
• We have used the synthetic microtubule inhibitor Tubulozole C in order to study the role of the microtubule system in human lymphocyte activation [5].
• For the cis and trans stereoisomers of the synthetic anti-microtubule compound tubulozole, at micromolar concentrations, tubulozole-C is cytotoxic to mammalian cells whereas tubulozole-T is not [6].

Biological context of NSC376450

• Light and electron microscopic investigations on mammalian cells in vitro and in vivo showed that tubulozole-C (R 46 846), the cis-isomer of tubulozole, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells [2].
• Effect of tubulozole, a new synthetic microtubule inhibitor, on the induction of casein gene expression by prolactin [7].
• New structural analogues of Tubulozole induce apoptosis, [Ca2+]i modifications and cytoskeletal disorganization in glial (GL15) and neuronal-like (PC12) cell lines [8].

Anatomical context of NSC376450

• The anti-microtubule agent tubulozole is found to disrupt, rapidly and transiently, the AFT, inhibiting flagella formation, cell elongation and the arrangement of microtubules and microfilaments [9].
• 1. Four hour treatments of adrenal chromaffin cells with colchicine (10, 100 microM and 1 mM), tubulozole (10 microM) or podophyllotoxin (100 microM) decreases alpha-tubulin mRNA content [10].

Associations of NSC376450 with other chemical compounds

• Erbulozole (R55 104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities [11].

Gene context of NSC376450

• Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules [12].
• The Kidney Invasion Test: an assay allowing macroscopic quantification of malignant invasion in vivo. Comparison between the microtubule inhibitor tubulozole and the podophyllotoxin congener etoposide (VP-16-213) [13].

Analytical, diagnostic and therapeutic context of NSC376450

• The interactive effect is maintained in a clinically relevant dose fractionation schedule whereby 8 fractions of 2 Gy each were pretreated 6 hr before with 80 mg/kg tubulozole [1].
• Analysis of labelled parasite proteins by two-dimensional gel electrophoresis showed that while it inhibited synthesis of most proteins to the same degree, tubulozole T super-inhibited the synthesis of certain proteins [12].
• Eighty mg/kg R 55 104, given orally 6 h before or 3 h after radiotherapy, displays a prominent interactive effect with 10 Gy gamma irradiation in subcutaneous murine tumors which is similar to 160 mg/kg tubulozole administered 6 h before 10 Gy [14].

References