Rok Frlan

Dr. Rok Frlan

The Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia
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Research Focus & Metrics

Academic Career Length

22Years (2005-Present)

(Calculated once Scilit publication data is synced: current year − year of first publication + 1)

Representative Publications

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1 August 2006 in Current Medicinal Chemistry
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SGStanislav Gobec
Stanislav Gobec
Rok FrlanRok Frlan
Rok Frlan
Cathepsin B is an abundant and ubiquitously expressed cysteine peptidase of the papain family. It is involved in many physiological processes, such as remodeling of the extracellular matrix (wound healing), apoptosis, and activation of thyroxine and renin. In addition to its physiological roles, cathepsin B is important in many pathological processes, such as inflammation, parasite infection and cancer, where it is highly up-regulated. In cancer patients, elevated cathepsin B activity correlates to poor therapy outcome. Therefore, it is not surprising that the use of cathepsin B inhibitors reduces both tumor cell motility and invasiveness in vitro. This review summarizes recent developments in cathepsin B inhibition. To date, numerous protein inhibitors of cathepsin B have been described, some of which are of endogenous origin and function as regulators of cathepsin B activity in the cell, such as the cystatins. In addition, some exogenous protein inhibitors of cathepsin B have been isolated from various natural sources, and the use of X-ray crystal structures of cathepsin B complexed with such protein inhibitors has resulted in the design and synthesis of many new small-molecular-weight compounds as inhibitors of cathepsin B. These synthetic compounds generally contain an electrophilic functionality that reacts with cathepsin B. In the present review, these inhibitors are divided according to their mechanisms of action, as reversible and irreversible, and then further subdivided into groups for their full descriptions.

29 June 2006 in Synthesis
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DKDanijel Kikelj
Danijel Kikelj
Rok FrlanRok Frlan
Rok Frlan
Diaryl ethers form an important class of organic compounds, both in life sciences and in the polymer industry. In general, diaryl ethers can be synthesized by means of copper-catalyzed Ullmann diaryl ether coupling, palladium-catalysed Buchwald-Hartwig reaction, nucleophilic aromatic substitution, arylboronic acid diaryl ether coupling, oxidative coupling, and nucleophilic aromatic addition to metal-arene complexes. This review covers the progress in diaryl ether synthesis since 1999, with literature coverage through September 2005.

1 January 2021 in European Journal of Medicinal Chemistry
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BJBadr Jismy
Badr Jismy
AQAbdelkarim El Qami
Abdelkarim El Qami
APAnja Pišlar
Anja Pišlar
Rok FrlanRok Frlan
Rok Frlan
JKJanko Kos
Janko Kos
MAMohamed Abarbri
Mohamed Abarbri

11 January 2008 in Molecules
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Rok FrlanRok Frlan
Rok Frlan
AKAndreja Kovač
Andreja Kovač
DBDidier Blanot
Didier Blanot
SGStanislav Gobec
Stanislav Gobec
SPSlavko Pečar
Slavko Pečar
Aleš ObrezaAleš Obreza
Aleš Obreza
A series of novel N-benzylidenesulfonohydrazide compounds were designedand synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) andUDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved inthe biosynthesis of bacterial cell-walls. Some compounds possessed inhibitory activityagainst both enzymes with IC50 values as low as 30 μM. In addition, a new, one-potsynthesis of amidobenzaldehydes is reported.

5 April 2024 in Antibiotics
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TŽTjaša Žagar
Tjaša Žagar
Rok FrlanRok Frlan
Rok Frlan
NGNina Kočevar Glavač
Nina Kočevar Glavač
The use of green extraction methods that meet the criteria of sustainable and environmentally friendly technologies has been increasing in recent decades due to their many benefits. In this respect, extracts obtained using subcritical water are also gaining increased attention because of their potential antioxidant and antimicrobial properties. Their antimicrobial activity is mainly due to the presence of various polyphenolic compounds. Although the exact mechanism of the antibacterial action of polyphenolic compounds has not yet been fully investigated and described, polyphenols are known to affect the bacterial cell at several cellular levels; among other things, they cause changes and ruptures in the cell membranes of the bacterial cell, affect the inactivation of bacterial enzymes and damage bacterial DNA. The difference in the strength of the antimicrobial activity of the extracts is most likely a result of differences in their lipophilicity and in the number and position of hydroxyl groups and double bonds in the chemical structure of polyphenols. By changing the extraction conditions, especially the temperature, during subcritical water extraction, we affect the solubility of the compounds we want to extract. In general, as the temperature increases, the solubility of polyphenolic compounds also increases, and the reduction of the surface tension of subcritical water at higher temperatures also enables faster dissolution of polyphenolic compounds. Different bacterial strains have different sensitivity to different extracts. However, extracts obtained with subcritical water extraction demonstrate strong antimicrobial activity compared to extracts obtained with conventional methods.

9 July 2015 in The Journal of Organic Chemistry
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Rok FrlanRok Frlan
Rok Frlan
Matej SovaMatej Sova
Matej Sova
SGStanislav Gobec
Stanislav Gobec
GSGaj Stavber
Gaj Stavber
ZČZdenko Časar
Zdenko Časar