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Interaction of desacetamidocolchicine, a fast binding analogue of colchicine with isotypically pure tubulin dimers alpha beta II, alpha beta III, and alpha beta IV.
TLDR
The observed pseudo-first-order rate constants increased in a nonlinear way with the drug concentration, indicating that the binding of DAAC to tubulin isoforms occur in two steps as is true for the binding for colchicine to Tubulin. Expand
Immobilizing and imaging microtubules by atomic force microscopy.
TLDR
Microtubules isolated from pig brains have been immobilized on an inorganic substrate for use in AFM studies and gold-coated tubules bound on silicon have been successfully imaged by STM, while images of uncertain origin were generated for tubules deposited on graphite. Expand
Interactions of a bicyclic analog of colchicine with beta-tubulin isoforms alphabeta(II), alphabeta(III) and alphabeta(IV).
TLDR
The results indicate that the B-ring plays a major role in determining the isoform differences, and the results might be of importance for designing tissue-specific analogs of colchicine for cancer chemotherapy. Expand
Evidence for an alternative pathway for colchicine binding to tubulin, based on the binding kinetics of the constituent rings.
TLDR
Stopped-flow kinetic studies reveal that fast TMA binding competes for the initial binding of colchicine, indicating that TMA also binds slowly in a second mode or site and the binding of TMA is practically thermoneutral. Expand
Kinetics of association and dissociation of two enantiomers, NSC 613863 (R)-(+) and NSC 613862 (S)-(-) (CI 980), to tubulin.
TLDR
The kinetics of binding of R- and S-enantiomers were studied by the fluorescence stopped-flow technique and the association rate constant of the S-isomer to the R-site was determined. Expand
Fluorescence stopped-flow study of the interaction of tubulin with the antimitotic drug MDL 27048.
TLDR
The kinetics of the binding of MDL 27048 to tubulin have been studied by fluorescence stopped flow and the reaction enthalpy change for the first binding equilibrium and the activation energies for the forward and reverse steps of the isomerization were determined from the temperature dependence. Expand
Abstract LB-210: KPT-8602 is a second-generation XPO1 inhibitor with improvedin vivotolerability that demonstrates potent acute lymphoblastic leukemia activity
TLDR
KPT-8062 is a second-generation XPO1 inhibitor with high specificity for its target and with potent anti-ALL activity, displaying better tolerability as compared to the first-generation SINE selinexor allowing it for daily dosing resulting in effective anti-all activity in in vivo PDX models. Expand