TY  - JOUR
A1  - Cataldi, Eleonora
A1  - Raschig, Martina
A1  - Gutmann, Marcus
A1  - Geppert, Patrick T.
A1  - Ruopp, Matthias
A1  - Schock, Marvin
A1  - Gerwe, Hubert
A1  - Bertermann, Rüdiger
A1  - Meinel, Lorenz
A1  - Finze, Maik
A1  - Nowak‐Król, Agnieszka
A1  - Decker, Michael
A1  - Lühmann, Tessa
T1  - Amber Light Control of Peptide Secondary Structure by a Perfluoroaromatic Azobenzene Photoswitch
JF  - ChemBioChem
N2  - The incorporation of photoswitches into the molecular structure of peptides and proteins enables their dynamic photocontrol in complex biological systems. Here, a perfluorinated azobenzene derivative triggered by amber light was site‐specifically conjugated to cysteines in a helical peptide by perfluoroarylation chemistry. In response to the photoisomerization (trans→cis) of the conjugated azobenzene with amber light, the secondary structure of the peptide was modulated from a disorganized into an amphiphilic helical structure.
KW  - amber light
KW  - decafluoroazobezene
KW  - peptide stapling
KW  - photocontrol
KW  - perfluoroarylation
Y1  - 2023
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-312480
VL  - 24
IS  - 5
ER  - 
TY  - JOUR
A1  - Raschig, Martina
A1  - Ramírez‐Zavala, Bernardo
A1  - Wiest, Johannes
A1  - Saedtler, Marco
A1  - Gutmann, Marcus
A1  - Holzgrabe, Ulrike
A1  - Morschhäuser, Joachim
A1  - Meinel, Lorenz
T1  - Azobenzene derivatives with activity against drug‐resistant Candida albicans and Candida auris
JF  - Archiv der Pharmazie
N2  - Increasing resistance against antimycotic drugs challenges anti‐infective therapies today and contributes to the mortality of infections by drug‐resistant Candida species and strains. Therefore, novel antifungal agents are needed. A promising approach in developing new drugs is using naturally occurring molecules as lead structures. In this work, 4,4'‐dihydroxyazobenzene, a compound structurally related to antifungal stilbene derivatives and present in Agaricus xanthodermus (yellow stainer), served as a starting point for the synthesis of five azobenzene derivatives. These compounds prevented the growth of both fluconazole‐susceptible and fluconazole‐resistant Candida albicans and Candida auris strains. Further in vivo studies are required to confirm the potential therapeutic value of these compounds.
KW  - antifungal drug
KW  - azobenzenes
KW  - Candida auris
KW  - Candida albicans
Y1  - 2023
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-312295
VL  - 356
IS  - 2
ER  - 
TY  - JOUR
A1  - Schlauersbach, Jonas
A1  - Hanio, Simon
A1  - Raschig, Martina
A1  - Lenz, Bettina
A1  - Scherf-Cavel, Oliver
A1  - Meinel, Lorenz
T1  - Bile and excipient interactions directing drug pharmacokinetics in rats
JF  - European Journal of Pharmaceutics and Biopharmaceutics
N2  - Bile solubilization plays a major role in the absorption of poorly water-soluble drugs. Excipients used in oral drug formulations impact bile-colloidal properties and their molecular interactions. Polymer-induced changes of bile colloids, e.g., by Eudragit E, reduced the flux of the bile interacting drug Perphenazine whereas bile non-interacting Metoprolol was not impacted. This study corroborates these in vitro findings in rats. Eudragit E significantly reduced systemic availability of Perphenazine but not Metoprolol compared to the oral administrations without polymer. This study confirms the necessity to carefully select polymers for bile interacting drugs whereas non-bile interacting drugs are more robust in terms of excipient choice for formulation. The perspective of bile interaction may introduce interesting biopharmaceutical leverage for better performing oral formulations of tomorrow.
KW  - in vitro-in vivo correlation
KW  - pharmacokinetics
KW  - bile
KW  - excipient
KW  - rat study
Y1  - 2022
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-296969
VL  - 178
ET  - accepted version
ER  -