Binding of Tubulin to Substituted Sepharose.
نویسندگان
چکیده
منابع مشابه
Molecular Modeling Studies on Vinblastine Binding Site of Tubulin for Antimitotic agents
Medicinal chemistry depends on many other disciplines ranging from organic chemistry andpharmacology to computational chemistry. Typically medicinal chemists use the moststraightforward ways to prepare compounds. The validation of any design project comes from thebiological testing.Studies of the binding site of vinblastine by a single cross—linking experiment identified it asbeing between resi...
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Isocolchicine is a structurally related isomer of colchicine altered in the methoxytropone C ring. In spite of virtual structural homology of colchicine and isocolchicine, isocolchicine is commonly believed to be inactive in binding to tubulin and inhibiting microtubule assembly. We have found that isocolchicine does indeed bind to the colchicine site on tubulin, as demonstrated by its ability ...
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Understanding the interactions of epothilones with β-tubulin is crucial for computer aided rational design of macrocyclic drugs based on epothilones and epothilone derivatives. Despite numerous structure-activity relationship investigations we still lack substantial knowledge about the binding mode of epothilones and their derivatives to β-tubulin. In this work, we reevaluated the electron crys...
متن کاملPromotion of fluorescence upon binding of colchicine to tubulin.
Colchicine, which does not fluoresce in aqueous media and organic solvents, exhibits marked fluorescence on combination with brain tubulin, with a corrected excitation maximum at 362 nm, an emission maximum at 435 nm, and a quantum yield of about 0.03. From fluorescence measurements it was found that rat brain tubulin binds 0.83 moles of colchicine per dimer (molecular weight 110,000) with an a...
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Tubulin possesses two distinct binding sites for vinblastine; one of high affinity (Ka = 6.2 X 106M” ) occupancy of which prevents polymerization of tubulin and a second, lower affinity site (K, = 8 X 104M”) occupancy of which correlates with the aggregating effects of the alkaloid on tubulin [l]. The recent report [2] that maytansine, a new antitumor agent of plant origin [3,4] , was a potent ...
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ژورنال
عنوان ژورنال: Acta Chemica Scandinavica
سال: 1976
ISSN: 0904-213X
DOI: 10.3891/acta.chem.scand.30b-0794