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Nizkomolekularni ligandi galektinov : strukturno podprta optimizacija afinitete In selektivnosti = Small-molecule galectin ligands : structure-based optimisation of affinity and selectivity : PhD dissertationvan Klaveren, SjorsV telesu so vse celične površine prekrite z glikani. Tudi na številne regulatorne komponente so vezani ogljikovi hidrati, ki pomagajo pri njihovem delovanju. Galektini so družina proteinov, ki se ... vežejo na določene glikane in oligosaharide ter jih navzkrižno povežejo, s čimer vplivajo na širok spekter celičnih procesov. Člani družine galektinov so strukturno podobni in so lahko vključeni v iste ali različne procese. V notranjosti celice so prisotni galektini, ki pomagajo pri odkrivanju izpostavljenih glikanov na poškodovanih znotrajceličnih veziklih, kar sproži avtofagijo, ki pomaga odstraniti poškodovane celice in bakterijske okužbe. Nekateri galektini imajo vlogo pri spodbujanju angiogeneze in limfangiogeneze, kar je povezano z obnovo poškodovanega tkiva in rastjo tumorjev. Študije so pokazale tudi vpletenost galektinov v avtoimunske in nevrodegenerativne bolezni. Raziskave v tej doktorski disertaciji so bile osredotočene na odkrivanje in razvoj selektivnih ligandov z visoko afiniteto za več galektinov, s posebnim poudarkom na galektinu-8. Sintetizirali smo več strukturno raznolikih knjižnic spojin, ki smo jih načrtovali na podlagi struktur znanih ligandov in struktur proteinov. Odkrili smo več novih zaviralcev galektinov-1, -3 in -8N ter postavili razmerja med strukturo in delovanjem. Izhodiščne spojine smo optimizirali do spojin s submikromolarnimi afinitetami in analogov s skoraj popolno selektivnostjo za galektin-8N glede na ostale testirane galektine. Takšne visoko selektivne spojine so uporabne za preučevanje biološke vloge galektina-8 in patologij, v katere je vključen. To lahko posledično vodi tudi do zaviralcev galektina-8N s farmacevtskim potencialom.Type of material - dissertation ; adult, seriousPublication and manufacture - Ljubljana : [S. van Klaveren], 2024Language - englishCOBISS.SI-ID - 191366403
Author
van Klaveren, Sjors
Other authors
Tomašič, Tihomir |
Nilsson, Ulf, farmacevt |
Walse, Björn |
Johnsson, Richard |
Minovski, Nikola |
Perdih, Andrej, farmacevt
Topics
Farmacevtska kemija |
Beljakovine |
galektini |
glikani |
kvaziharmonska analiza |
interna dinamika |
vodni transport |
SGLT1 |
vSGLT
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Library/institution |
City | Acronym | For loan | Other holdings |
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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DRS, in which the journal is indexed
Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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van Klaveren, Sjors | ![]() |
Tomašič, Tihomir | 28334 |
Nilsson, Ulf, farmacevt | ![]() |
Walse, Björn | ![]() |
Johnsson, Richard | ![]() |
Minovski, Nikola | 29497 |
Perdih, Andrej, farmacevt | 25493 |
Source: Personal bibliographies
and: SICRIS
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