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O-GlcNAcylation is an essential post-translational modification that occurs on nuclear and cytoplasmic proteins, regulating their function in response to cellular stress and altered nutrient availability. O-GlcNAc transferase (OGT) is the enzyme that catalyzes this reaction and represents a potential therapeutic target, whose biological role is still not fully understood. To support this research field, a series of cell-permeable, low-nanomolar OGT inhibitors were recently reported. In this study, we resynthesized the most potent OGT inhibitor of the library, OSMI-4, and we used it to investigate OGT inhibition in different human cell lines. The compound features an ethyl ester moiety that is supposed to be cleaved by carboxylesterases to generate its active metabolite. Our LC-HRMS analysis of the cell lysates shows that this is not always the case and that, even in the cell lines where hydrolysis does not occur, OGT activity is inhibited. Nasl. z nasl. zaslona. Opis vira z dne 11. 8. 2020. Št. članka: 3381. Abstract. Bibliografija: str. 9-10. European Union’s Horizon2020 program under the Marie Skłodowska-Curie, PhD4GlycoDrug COST actions, Innogly COST Actions, GLYCONanoPROBES

The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance, but also provide at least interim effective protection against emerging bacterial infections. Research into DNA gyrase and topoisomerase IV inhibitors has become a particular focus, with the description of a new class of bacterial topoisomerase type II inhibitors known as "novel bacterial topoisomerase inhibitors" NBTIs. Elucidation of the key structural modifications incorporated into these inhibitors and the impact these can have on their general physicochemical properties are detailed in this review. This defines novel bacterial topoisomerase inhibitors with promising antibacterial activities and potencies, which thus represent one potential example of the future "drugs for bad bugs", as identified by the World Health Organization. Bibliografija: str. 5672-5674. Abstract. ARRS ARRS

The Faculty of Pharmacy of the University of Ljubljana mission is to assure excellent education and research, as well as professional engagements. The Faculty fosters training of critically minded graduates capable of confronting current and future challenges. Societal impact is sought in collaborations with strategic partners from the fields of health institutions, regulatory agencies and education and research-related policy makers. The Faculty is committed to training and educating professionals responsive to the medication and health needs of the patient%s, as well as of leaders for regional and global competitive environments in the fields of pharmacy, pharmaceutical industry, clinical and laboratory biomedicine and cosmetology. Poslanstvo Fakultete za farmacijo Univerze v Ljubljani je kakovostno izobraževanje, raziskovalna odličnost in vpetost v stroko. Skrbimo za razvoj kritično mislečih diplomantov, sposobnih soočenj z izzivi stroke v sedanjosti in prihodnosti. Svoj doprinos družbi dolgoročno zagotavljamo v sodelovanju s strateškimi partnerji iz zdravstvenih zavodov, gospodarstva, regulatornih organov ter oblikovalcev in izvrševalcev politik izobraževanja in zdravstvene dejavnosti. Sledimo poslanstvu vzgoje, usposabljanja in izobraževanja strokovnjakov v skrbi za paciente in njihovo zdravje kot tudi strokovnjakov za delo v regionalnem in globalnem tekmovalnem okolju na področju farmacije, farmacevtske industrije, klinične kemije in laboratorijske biomedicine ter kozmetologije.

The article provides a systematic overview of drugs used in the treatment of wounds. Its purpose is not to give treatment guidelines for specific types of wounds, but rather to review mechanisms of drug action according to the individual phases of wound healing and to present current information on active ingredients that are currently registered or are available in the Republic of Slovenia. In this way, health professionals may select appropriate knowledgebased therapies in the process of wound care. V prispevku predstavljamo sistematičen pregled zdravilnih učinkovin, ki jih uporabljamo v oskrbi ran. Namen prispevka je pojasniti delovanje zdravilnih učinkovin na različne faze celjenja ran in predstaviti aktualne informacije o tistih, ki so trenutno registrirane v Republiki Sloveniji. S tem želimo zdravstvenim delavcem olajšati izbor najustreznejšega zdravljenja v oskrbi ran, ki naj ne temelji le na poznavanju smernic zdravljenja, temveč tudi na poznavanju mehanizmov delovanja uporabljenih zdravilnih učinkovin.

Permeability across blood-brain barrier is a necessity for achieving pharmacological effect in the central nervous system. Development of central nervous system agents requires optimization of drug permeability into brain additional to enhancement of other pharmacodynamic and pharmacokinetic parameters. Herein, in silico methods for prediction of blood-brain barrier permeability are reviewed. Futhermore, special attention is paid to the possibilty of active transport as a mechanism of transport as in addition to passive permeability, it can fundamentaly influence the permeability of central nervous system agent. Za dosego farmakološkega učinka v centralnem živčnem sistemu je nujen predpogoj, da učinkovina prehaja preko krvno-možganske pregrade. Pri razvoju učinkovin z delovanjem v centralnem živčevju moramo zato poleg farmakodinamskih in farmakokinetičnih parametrov optimizirati tudi prehajanje spojine v možgane. V preglednem članku so predstavljeni in silico načini napovedovanja prehajanja krvno-možganske pregrade. Poleg pasivnega prehajanja je potrebno upoštevati tudi možnost aktivnega prenosa, ki lahko bistveno vpliva na prehodnost učinkovine.