Literature DB >> 6115675

Stabilization of the colchicine-binding activity of tubulin by organic acids.

E Hamel, C M Lin.   

Abstract

A number of carboxylic acids and organic phosphates were found to be highly effective in stabilizing the colchicine-binding activity of calf brain tubulin. The most active were glutamate, glutarate, delta-aminovalerate, glucose 1-phosphate, glucose 6-phosphate, fructose 1,6-(bis)phosphate, creatine phosphate and 6-phosphogluconate Maximum effects occurred at high concentrations. Combinations of agents were also examined, and the most effective mixture for stabilizing tubulin found thus far was the combination of 1.0 M glutamate, 100 mM glucose 1-phosphate, 1 mM GTP and 0.5 mg/ml of albumin. No loss of activity occurred over 48 h at 37 degrees C with tubulin was present at a concentration of 100 microgram/ml.

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Year:  1981        PMID: 6115675     DOI: 10.1016/0304-4165(81)90231-2

Source DB:  PubMed          Journal:  Biochim Biophys Acta        ISSN: 0006-3002


  18 in total

1.  Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).

Authors:  Matthew T Macdonough; Tracy E Strecker; Ernest Hamel; John J Hall; David J Chaplin; Mary Lynn Trawick; Kevin G Pinney
Journal:  Bioorg Med Chem       Date:  2013-07-23       Impact factor: 3.641

2.  Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.

Authors:  Mallinath B Hadimani; Matthew T Macdonough; Anjan Ghatak; Tracy E Strecker; Ramona Lopez; Madhavi Sriram; Benson L Nguyen; John J Hall; Raymond J Kessler; Anupama R Shirali; Li Liu; Charles M Garner; George R Pettit; Ernest Hamel; David J Chaplin; Ralph P Mason; Mary Lynn Trawick; Kevin G Pinney
Journal:  J Nat Prod       Date:  2013-09-09       Impact factor: 4.050

3.  Synthesis and anti-breast cancer activity of novel indibulin related diarylpyrrole derivatives.

Authors:  Ebrahim Saeedian Moghadam; Ernest Hamel; Zahra Shahsavari; Mohsen Amini
Journal:  Daru       Date:  2019-03-20       Impact factor: 3.117

4.  Novel water-soluble substituted pyrrolo[3,2-d]pyrimidines: design, synthesis, and biological evaluation as antitubulin antitumor agents.

Authors:  Aleem Gangjee; Roheeth K Pavana; Wei Li; Ernest Hamel; Cara Westbrook; Susan L Mooberry
Journal:  Pharm Res       Date:  2012-07-20       Impact factor: 4.200

5.  Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.

Authors:  Roheeth Kumar Pavana; Shruti Choudhary; Anja Bastian; Michael A Ihnat; Ruoli Bai; Ernest Hamel; Aleem Gangjee
Journal:  Bioorg Med Chem       Date:  2016-11-15       Impact factor: 3.641

6.  Synthesis of dihydronaphthalene analogues inspired by combretastatin A-4 and their biological evaluation as anticancer agents.

Authors:  Casey J Maguire; Zhi Chen; Vani P Mocharla; Madhavi Sriram; Tracy E Strecker; Ernest Hamel; Heling Zhou; Ramona Lopez; Yifan Wang; Ralph P Mason; David J Chaplin; Mary Lynn Trawick; Kevin G Pinney
Journal:  Medchemcomm       Date:  2018-08-24       Impact factor: 3.597

7.  Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.

Authors:  Haichan Niu; Tracy E Strecker; Jeni L Gerberich; James W Campbell; Debabrata Saha; Deboprosad Mondal; Ernest Hamel; David J Chaplin; Ralph P Mason; Mary Lynn Trawick; Kevin G Pinney
Journal:  J Med Chem       Date:  2019-05-24       Impact factor: 7.446

8.  Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.

Authors:  Sultan Nacak Baytas; Nazan Inceler; Akin Yilmaz; Abdurrahman Olgac; Sevda Menevse; Erden Banoglu; Ernest Hamel; Roberta Bortolozzi; Giampietro Viola
Journal:  Bioorg Med Chem       Date:  2014-04-20       Impact factor: 3.641

9.  Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.

Authors:  Giovanni Marzaro; Antonio Coluccia; Alessandro Ferrarese; Paola Brun; Ignazio Castagliuolo; Maria Teresa Conconi; Giuseppe La Regina; Ruoli Bai; Romano Silvestri; Ernest Hamel; Adriana Chilin
Journal:  J Med Chem       Date:  2014-05-14       Impact factor: 7.446

10.  A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds.

Authors:  Emanuela Screpanti; Stefano Santaguida; Tam Nguyen; Romano Silvestri; Rick Gussio; Andrea Musacchio; Ernest Hamel; Peter De Wulf
Journal:  PLoS One       Date:  2010-07-15       Impact factor: 3.240

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