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001-es BibID:	BIBFORM066145
Első szerző:	Herczeg Mihály (vegyész, biológia-kémia tanár)
Cím:	Inhibitory Effect of Multivalent Rhamnobiosides on Recombinant Horseshoe Crab Plasma Lectin Interactions with PAO1 / Herczeg Mihály, Mező Erika, Molnár Nikolett, Ng Sim-Kun, Lee Yuan-Chuan, Dah-Tsyr Chang Margaret, Borbás Anikó
Dátum:	2016
ISSN:	1861-4728
Megjegyzések:	To evaluate the molecular interaction of recombi-nant horseshoe crab plasma lectin (rHPL) withPseudomonasaeruginosaPAO1, multivalent rhamnobioside derivativeswere designed. Eight rhamnoclusters with three or foura(1?3)-rhamnobiosides attached to different central cores, suchas methyl gallate, pentaerythritol, andN-Boc Tris, througheither an ethylene glycol or a tetraethylene glycol linker,were assembled in two consecutive azide?alkyne cycloaddi-tion click reactions. The synthetic method embraced thepreparation of twoa(1?3)-rhamnobiosides with differentlinker arms and their conjugation, in stoichiometric or sub-stoichiometric amounts, to propargyl ether-functionalizedtri- or tetravalent scaffolds. A divalent derivative and twoself-assembling rhamnobiosides were also prepared. The dif-ferent architectures and valences of the rhamnoclusters pro-vided an opportunity to evaluate the impact of topologyand valency on the binding properties toward rHPL. Inhibito-ry ELISA data showed that all covalently linked rhamnoclus-ters could inhibitP. aeruginosaPAO1 recognition activity ofrHPL with high efficacy. Trivalent rhamnobiosides showeda stronger inhibitory effect onP. aeruginosaPAO1 binding,and the more flexible clusters on a pentaerythritol or a Triscore were superior to the less flexible methyl gallate-basedclusters. Interestingly, the length of the linker arms hada very low impact on the binding ability of the rhamnoclus-ters. Herein, the two trivalent derivatives on anN-Boc pro-tected Tris central core were the best inhibitors. The self-as-sembling amphiphilic rhamnobioside derivatives were foundto display no multivalent effect.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban carbohydrates click chemistry inhibitors lectin multivalency
Megjelenés:	Chemistry - An Asian Journal 11 : 23 (2016), p. 3398-3413. -
További szerzők:	Mező Erika (1986-) (vegyész) Molnár Nikolett (1992-) (gyógyszerész) Ng, Sim-Kun (1980-) (vegyész) Lee, Yuan-Chuan (1932-) (biokémikus) Dah-Tsyr Chang, Margaret (1956-) (vegyész) Borbás Anikó (1965-) (vegyész)
Pályázati támogatás:	K109208 OTKA PD115645 OTKA Ministry of Science and Technology MOST 105-2627M-007-003 to M.D.-T.C.) Egyéb
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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