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Št. zadetkov: 9
Sinteza in vredonotenje potencialnih zaviralcev N-acetilglukozaminil transferaze
Maša Sterle, Marko Anderluh, Matjaž Weiss
Magistrsko delo
Oznake: encim OGT;heksozaminska biosintezna pot;zaviralci OGT;kinolon-4-karboksamid;amidna vez;
O-beta-N-acetilglukozaminil transferaza (OGT) je encim, odgovoren za posttranslacijsko modifikacijo številnih proteinov, ki imajo poglavitno vlogo pri regulaciji različnih celičnih procesov. Povečana ali zmanjšana glikozilacija proteinov je udeležena v patologiji metabolnih in nevrodegenerativnih bo ...
Leto: 2019 Vir: Fakulteta za farmacijo (UL FFA)
Načrtovanje, sinteza in vrednotenje neplanarnih benzotiazolnih zaviralcev bakterijskih topoizomeraz z razširjenim spektrom delovanja
Maša Sterle, Anamarija Zega, Andrej Emanuel Cotman
Doktorska disertacija
Oznake: protibakterijske učinkovine;benzotiazol;dvojni inhibitor;DNA giraza;M. tuberkuloze;M. abscessus;netuberkulozne mikobakterije;asimetrična kataliza;DFT;fluor;hidrogeniranje;kinetična resolucija;rutenij;
Število življensko ogrožujočih okužb zaradi multirezistentnih po Gramu pozitivnih in po Gramu negativnih bakterij ter mikobakterij hitro narašča, zato je odkrivanje novih tarč in raz-voj novih učinkovin nujno. DNA giraza in topoizomeraza IV sta validirani tarči za razvoj protibakterijskih učinkovin, ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Hydrogen-bonding ability of Noyori–Ikariya catalysts enables stereoselective access to CF[sub]3-substituted syn-1,2-diols via dynamic kinetic resolution
Maša Sterle, Matej Huš, Matic Lozinšek, Anamarija Zega, Andrej Emanuel Cotman
Kratki znanstveni prispevek
Oznake: asymmetric catalysis;DFT;drug design;fluorine;hydrogenation;kinetic resolution;ruthenium;
Stereopure CF[sub]3-substituted syn-1,2-diols were prepared via the reductive dynamic kinetic resolution of the corresponding racemic α-hydroxyketones in HCO[sub]2H/Et[sub]3N. (Het)aryl, benzyl, vinyl, and alkyl ketones are tolerated, delivering products with ≥95% ee and ≥87:13 syn/anti. This method ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
New quinolinone O-GlcNAc transferase inhibitors based on fragment growth
Matjaž Weiss, Elena Maria Loi, Maša Sterle, Cyril Balsollier, Tihomir Tomašić, Roland J. Pieters, Martina Gobec, Marko Anderluh
Izvirni znanstveni članek
Oznake: O-GlcNAc;O-GlcNAc transferase;protein glycosylation;fragments growth;molecular docking;
O-GlcNAcylation is an important posttranslational and metabolic process in cells that must be carefully regulated. O-GlcNAc transferase (OGT) is ubiquitously present in cells and is the only enzyme that catalyzes the transfer of O-GlcNAc to proteins. OGT is a promising target in various pathologies ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Catalytic stereoconvergent synthesis of homochiral [beta]-CF[sub]3, [beta]-SCF[sub]3, and [beta]-OCF[sub]3 benzylic alcohols
Andrej Emanuel Cotman, Pavel A. Dub, Maša Sterle, Matic Lozinšek, Jaka Dernovšek, Živa Zajec, Anamarija Zega, Tihomir Tomašić, Dominique Cahard
Izvirni znanstveni članek
Oznake: adaptive crystals;asymmetric catalysis;density functional calculations;drug design;fluorine;hydrogenation;kinetic resolution;ruthenium;alcohols;catalysts;crystals;ketones;stereoselectivity;
We describe an efficient catalytic strategy for enantio- and diastereoselective synthesis of homochiral β-CF$_3$, β-SCF$_3$, and β-OCF$_3$ benzylic alcohols. The approach is based on dynamic kinetic resolution (DKR) with Noyori−Ikariya asymmetric transfer hydrogenation leading to simultaneous constr ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Discovery of K V 1.3 ion channel inhibitors
Špela Gubič, Louise Antonia Hendrickx, Žan Toplak, Maša Sterle, Steve Peigneur, Tihomir Tomašić, Luis A. Pardo, Jan Tytgat, Anamarija Zega, Lucija Peterlin-Mašič
Pregledni znanstveni članek
Oznake: KV1.3 channel;design of KV1.3 inhibitors;mitochondrial KV1.3;peptide inhibitors;small-molecule inhibitors;
The KV1.3 voltage gated potassium ion channel is involved in many physiological processes both at the plasma membrane and in the mitochondria, chiefly in the immune and nervous systems. Therapeutic targeting KV1.3 with specific peptides and small molecule inhibitors shows great potential for treatin ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Discovery and Hit-to-Lead Optimization of Benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas aeruginosa
Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Maša Sterle, Štefan Možina, Žiga Skok, Nace Zidar, Anamarija Zega, Janez Ilaš, Lucija Peterlin-Mašič, Tihomir Tomašić, Danijel Kikelj
Izvirni znanstveni članek
Oznake: antibacterial activity;bacteria;genetics;inhibitors;solubility;
We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant bacteria. Starting from DNA gyrase inhibitor 1, we identified compound 27, featuring a 10-fold improved aqueous solubility ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
New N-phenylpyrrolamide inhibitors of DNA gyrase with improved antibacterial activity
Andrej Emanuel Cotman, Federica Fulgheri, Martina Piga, Peter Peršolja, Davide Benedetto Tiz, Žiga Skok, Martina Durcik, Maša Sterle, Jaka Dernovšek, Anamarija Zega, Lucija Peterlin-Mašič, Janez Ilaš, Tihomir Tomašić, Danijel Kikelj, Nace Zidar
Izvirni znanstveni članek
Oznake: N-fenilpirolamidni inhibitorji;bakterijske DNA giraze;sinteza spojin;antibakterijsko delovanje;
This study presents the discovery of a new series of N-phenylpyrrolamide inhibitors of bacterial DNA gyrase with improved antibacterial activity. The most potent inhibitors had low nanomolar IC50 values against Escherichia coli DNA gyrase (IC50; 2–20 nM) and E. coli topoisomerase IV (22i, IC50 = 143 ...
Leto: 2024 Vir: Fakulteta za farmacijo (UL FFA)
Exploring the 5-substituted 2-aminobenzothiazole-based DNA gyrase B inhibitors active against ESKAPE pathogens
Maša Sterle, Martina Durcik, Clare E. M. Stevenson, Sara R. Henderson, Petra Eva Szili, Marton Czikkely, David M. Lawson, Danijel Kikelj, Nace Zidar, Lucija Peterlin-Mašič, Janez Ilaš, Tihomir Tomašić, Andrej Emanuel Cotman, Anamarija Zega
Izvirni znanstveni članek
Oznake: inhibitorji;organske kisline;proteini;bacteria;genetics;inhibitors;organic acids;peptides;proteins;
We present a new series of 2-aminobenzothiazole-based DNA gyrase B inhibitors with promising activity against ESKAPE bacterial pathogens. Based on the binding information extracted from the cocrystal structure of DNA gyrase B inhibitor A, in complex with Escherichia coli GyrB24, we expanded the chem ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 9
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