Browsing Prof. Bablu Bhattacharya by Title
Now showing items 1-13 of 13
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Antagonists of Hsp16.3, a low-molecular-weight mycobacterial chaperone and virulence factor, derived from phage-displayed peptide libraries
(AMER SOC MICROBIOLOGY, 2005-11)The persistence of Mycobacterium tuberculosis is a major cause of concern in tuberculosis (TB) therapy. In the persistent mode the pathogen can resist drug therapy, allowing the possibility of reactivation of the disease. ... -
Anti-mitotic activity of colchicine and the structural basis for its interaction with tubulin
(JOHN WILEY & SONS, 2008-01)In this review, an attempt has been made to throw light on the mechanism of action of colchicine and its different analogs as anti-cancer agents. Colchicine interacts with tubulin and perturbs the assembly dynamics of ... -
Antimicrotubular drugs binding to vinca domain of tubulin
(KLUWER ACADEMIC PUBL, 2003-11)Studies on vinca domain binding drugs were done in great details by a number of workers as it is recognized as a potential target for anticancer drug development. Their structures, properties, mode of action, success and ... -
Antimitotic sulfonamides inhibit microtubule assembly dynamics and cancer cell proliferation
(AMER CHEMICAL SOC, 2006-08-01)Several sulfonamides have antitumor activities and are currently undergoing clinical evaluation for the treatment of cancer. In this study, we have elucidated the antiproliferative mechanism of action of five indole ... -
The B-ring substituent at C-7 of colchicine and the alpha-C-terminus of tubulin communicate through the "tail-body" interaction
(WILEY-LISS, 2004-11-15)The carboxy terminals of alphabeta-tubulins are flexible regions rich in acidic amino acid residues that play an inhibitory role in the polymerization of tubulin to microtubules. We have shown that the binding of colchicine ... -
Binding of Indanocine to the Colchicine Site on Tubulin Promotes Fluorescence, and Its Binding Parameters Resemble Those of the Colchicine Analogue AC
(AMER CHEMICAL SOC, 2009-02-24)Indanocine, a synthetic indanone, has shown potential antiproliferative activity against several tumor types. It is different from many other microtubule-disrupting drugs, because it displays toxicity toward multidrug ... -
Deuterium oxide stabilizes conformation of tubulin: A biophysical and biochemical study
(KOREAN SOCIETY BIOCHEMISTRY & MOLECULAR BIOLOGY, 2008-01-31)The present study was aimed to elucidate the mechanism of stabilization of tubulin by deuterium oxide (D2O). Rate of decrease of tryptophan fluorescence during aging of tubulin at 4 degrees C and 37 degrees C was significantly ... -
Fluorescence Spectroscopic Methods to Analyze Drug–Tubulin Interactions
(ELSEVIER ACADEMIC PRESS, 2010)Fluorescence spectroscopy has been extensively used to characterize ligand binding to tubulin and microtubules. The inherent advantages of fluorescence spectroscopic methods lie in their ease, sensitivity to local environmental ... -
Genistein Arrests Cell Cycle Progression of A549 Cells at the G2/M Phase and Depolymerizes Interphase Microtubules through Binding to a Unique Site of Tubulin
(AMER CHEMICAL SOC, 2010-03-02)Genistein (40,5,7-trihydroxyisoflavone), an isoflavone, is a major constituent of soyfoods. It has potential antiproliferative activity against several tumor types. We have examined the effect of genistein on cellular ... -
The natural naphthoquinone plumbagin exhibits antiproliferative activity and disrupts the microtubule network through tubulin binding
(AMER CHEMICAL SOC, 2008-07-29)Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone), a naphthoquinone isolated from the roots of Plumbaginaceae plants, has potential antiproliferative activity against several tumor types. We have examined the effects of ... -
-NH-dansyl isocolchicine exhibits a significantly improved tubulin-binding affinity and microtubule inhibition in comparison to isocolchicine by binding tubulin through its A and B rings
(AMER CHEMICAL SOC, 2005-03-08)Structure-activity relationship studies have established that the A and C rings of colchicine comprise the minimum structural feature necessary for high affinity drug-tubulin binding. Thus, colchicine acts as a bifunctional ... -
Oxalone and lactone moieties of podophyllotoxin exhibit properties of both the B and C rings of colchicine in its binding with tubulin
(AMER CHEMICAL SOC, 2006-05-23)Thermodynamics of podophyllotoxin binding to tubulin and its multiple points of attachment with tubulin has been studied in detail using isothermal titration calorimetry. The calorimetric enthalpy of the association of ... -
Sulfonamide drugs binding to the colchicine site of tubulin: Thermodynamic analysis of the drug-tubulin interactions by isothermal titration calorimetry
(AMER CHEMICAL SOC, 2005-01-27)The discovery of several sulfonamide drugs paved the way toward the synthesis of 6 (N-12-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide: E7010) and 7 (N-(3fluoro-4-methoxyphenyl)pentafluorobenzenesulfonamide, ...