๐”– Bobbio Scriptorium
โœฆ   LIBER   โœฆ

Microtubule disassembly and inhibition of mitosis by a novel synthetic pharmacophore

โœ Scribed by Robin M. Scaife

Publisher
John Wiley and Sons
Year
2006
Tongue
English
Weight
532 KB
Volume
98
Category
Article
ISSN
0730-2312

No coin nor oath required. For personal study only.

โœฆ Synopsis

Microtubule drugs, which block cell cycle progression through mitosis, have seen widespread use in cancer chemotherapies. Although microtubules are subject to regulation by signal transduction mechanisms, their pharmacological modulation has so far relied on compounds that bind to the tubulin subunit. A new microtubule pharmacophore, diphenyleneiodonium, causing disassembly of the microtubule cytoskeleton is described here. Although this synthetic compound does not affect the assembly state of purified microtubules, it profoundly suppresses microtubule assembly in vivo, causes paclitaxel-stabilized microtubules to cluster around the centrosomes, and selectively disassembles dynamic microtubules. Similar to other microtubule drugs, this new pharmacophore blocks mitotic spindle assembly and mitotic cell division.

๐Ÿ“œ SIMILAR VOLUMES

Pharmacokinetic scaling of SJ-8029, a no
Pharmacokinetic scaling of SJ-8029, a novel anticancer agent possessing microtubule and topoisomerase inhibiting activities, by species-invariant time methods
โœ Beom S. Shin; Dong H. Kim; Chang Y. Cho; Si K. Park; Sun G. Chung; Eui H. Cho; S ๐Ÿ“‚ Article ๐Ÿ“… 2003 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 113 KB

## Abstract This study examined the pharmacokinetic disposition of SJโ€8029, a novel anticancer agent possessing microtubule and topoisomerase inhibiting activities, in mice, rats, rabbits and dogs after i.v. administration. The serum concentration__โ€__time curves of SJโ€8029 were best described by t

Effect of pharmacological agents on huma
Effect of pharmacological agents on human keratinocyte mitosis in vitro. II. Inhibition by catecholamines
โœ Robert A. Harper; B. Allen Flaxman ๐Ÿ“‚ Article ๐Ÿ“… 1975 ๐Ÿ› John Wiley and Sons ๐ŸŒ English โš– 531 KB

## Abstract Catecholamines produce mitotic inhibition in primary cell cultures of human keratinocytes probably via a block in the G~2~ part of the cell cycle. Epinephrine produced significant mitotic inhibition (49%) at a concentration as low as 4.5 ร— 10^โˆ’10^ M, while its analog, isoproterenol, pro

Recognition and inhibition of HIV integr
Recognition and inhibition of HIV integrase by a novel dinucleotide
โœ Michael Taktakishvili; Nouri Neamati; Yves Pommier; Vasu Nair ๐Ÿ“‚ Article ๐Ÿ“… 2000 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 140 KB

The viral enzyme, HIV integrase, is involved in the integration of viral DNA into host cell DNA. In the quest for a small nucleotide system with nuclease stability of the internucleotide phosphate bond and critical structural features for recognition and inhibition of HIV-1 integrase, we have discov