Results 191 to 200 of about 291,222 (247)

Struktureller Mechanismus eines Aktivitäts‐Photoschalters am β2‐adrenergen Rezeptor

Angewandte Chemie, EarlyView.
Zeitaufgelöste Strukturen aus Messungen an Röntgen‐Freie‐Elektronen‐Lasern in Kombination mit zellulären Assays zeigen, wie der photoschaltbare β‐Blocker Photoazolol‐1 als Wirksamkeits‐Photoschalter der Funktion des β2‐adrenergen Rezeptor wirkt. Die lichtinduzierte Neupositionierung des Liganden verschiebt die Aktivität von inversem Agonistimus hin zu ...
Robin Stipp, Quentin Bertrand, Matilde Trabuco, Anna Duran‐Corbera, Maria Tindara Ignazzitto, Hannah Glover, Fabienne Stierli, Juanlo Catena, Melissa Carrillo, Sina Hartmann, Hans‐Peter Seidel, Matthias Mulder, Thomas Mason, Yasushi Kondo, Maximillian Wranik, Martin Appleby, Christoph Sager, Raymond Sierra, Gregory Gate, Pamela Schleissner, Xinxin Cheng, Tobias Weinert, Robert Cheng, Sandra Mous, John H. Beale, Michal Kepa, Amadeu Llebaria, Michael Hennig, Xavier Rovira, Joerg Standfuss   +29 more
wiley   +1 more source

Light‐Driven Competitive Selection in a Protein‐Catalyzed Dissipative Peptide Replication

Angewandte Chemie, EarlyView.
A structurally flexible protein catalyzes replication within a dissipative reaction network driven by UVA‐induced disulfide rearrangements. The protein accelerates templated autocatalytic cycles with replication emerging as the dominant pathway.
Éva Bartus, Edit Wéber, Attila Tököli, Ferenc Bogár, Momen R. F. Mohamed, Gábor Kecskeméti, Zoltán Szabó, Zoltán Kele, András Perczel, Márton Gadanecz, Zoltán Orgován, György M. Keserű, Tamás A. Martinek   +12 more
wiley   +1 more source

Parallels between the chloro and methoxy groups for potency optimization. [PDF]

RSC Med Chem
Chiodi D, Ishihara Y.
europepmc   +1 more source

Proteinvermittelte Kupfer‐Redoxregulation: Rolle von Disulfidbrücken und allosterischer Modulation

Angewandte Chemie, EarlyView.
Copper binding triggers structural changes that expose a reactive disulphide bridge, enabling intrinsic Cu(II) reduction in folded proteins. SAXS, XAS, and QM/MM simulations reveal how globular proteins such as HSA and SOD1 employ disulphide‐mediated dynamics to modulate site accessibility and control copper redox chemistry.
Rebecca Sternke‐Hoffmann, Chang Liu, Xue Wang, Hegne Pupart, Xun Sun, Jan Gui‐Hyon Dreiser, Peep Palumaa, Qinghua Liao, Matthias Krack, Jinghui Luo   +9 more
wiley   +1 more source

Crystal structure of carbon-nitrogen hydrolase from Helicobacter pylori G27. [PDF]

Acta Crystallogr F Struct Biol Commun
Srivastava A, Ayanlade JP, Suleiman L, Udell H, Abendroth J, Lorimer DJ, Edwards TE, Staker BL, Zigweid R, Subramanian S, Myler PJ, Chakafana G, Asojo OA.   +12 more
europepmc   +1 more source

Multicyclic D‐Stereospecific Hydrolase Dimer With High Sustained Activity

Angewandte Chemie, EarlyView.
Protein macrocyclization was applied to a thermally unstable D‐stereospecific hydrolase using in situ cyclization of proteins (INCYPRO). This site‐specific cross‐linking approach enhanced the resistance of the enzyme to heat and cosolvents.
Anissa Haim, Sandra Liebscher, Rasmus Klintrot, Lorenzo Vallino, Marcelo Masman, Andreas H. Simon, Marianne Hahn, Sven Hennig, Saskia Neubacher, Frank Bordusa, Tom N. Grossmann   +10 more
wiley   +1 more source

Crystal structure of Crocus vernus class IIIb chitinase: in silico ligand-binding studies and in vitro antifungal assay. [PDF]

Acta Crystallogr F Struct Biol Commun
Saeed A, Khaliq B, Iqbal S, Mehmood S, Betzel C, Akrem A.   +5 more
europepmc   +1 more source

Liganden der Lipidtasche induzieren allosterische Modulation der Proteindynamik im Bereich des aktiven Zentrums der Proteinkinase p38α

Angewandte Chemie, EarlyView.
Bei der Suche nach neuen allosterischen Stellen in der Serin/Threonin‐Kinase p38α deckt die NMR‐Spektroskopie eine dynamische Kopplung zwischen dem katalytischen Zentrum und der Lipidtasche auf. Die Ergebnisse offenbaren bewegungsbezogene Interdependenzen, die entfernte Regionen des Enzyms miteinander verbinden, was die Lipidtasche als ...
Sara Medina Gómez, Laurin T. Homberg, Mike Bührmann, Daniel Rauh, Rasmus Linser   +4 more
wiley   +1 more source

Fluorine‐18‐Labeled Nucleotide Analogs Targeting Ecto‐5'‐Nucleotidase (CD73) for Positron Emission Tomography Imaging of Solid Tumors

Angewandte Chemie, EarlyView.
Fluorine‐18‐labeled CD73 inhibitor [18F]PSB‐19427 enables noninvasive PET mapping of CD73 overexpression in triple‐negative breast (TNBC) and pancreatic cancer. For [18F]PSB‐19427, specific binding in human tumor tissues, favorable biodistribution with prolonged blood retention, robust tumor uptake, and superiority to [18F]FDG in a TNBC model ...
Clemens Dobelmann, Constanze C. Schmies, Georg Wilhelm Rolshoven, Mirko Scortichini, Stefan Wagner, Andreas Isaak, Riham M. Idris, Jennifer Dabel, Lucie Grey, Karolina Losenkova, Susanne Moschütz, Haneen Al Hroub, Antje Keim, Sandra Höppner, Jouko Sandholm, Pia Boström, Maija Hollmén, Norbert Sträter, Sven Hermann, Gennady G. Yegutkin, Kenneth A. Jacobson, Sonja Schelhaas, Christa E. Müller, Anna Junker   +23 more
wiley   +1 more source