Results 211 to 220 of about 308,029 (295)

Proteome‐Wide Target Identification Using Reactive Metallo‐Scaffolds (r‐mS): A Platform for Metallodrug Discovery

Angewandte Chemie, EarlyView.
Re‐envisioning the Ligandable Proteome: Reactive Metallo‐Scaffolds (r‐mS) combine non‐covalent protein engagement by a metallo‐scaffold with covalent cysteine capture through a tethered chloroacetamide warhead. Chemoproteomic profiling reveals unique enzyme engagement including ligases, kinases and methyltransferases, highlighting opportunities for ...
Jessica E. Waters, Harry Wilders, George S. Biggs, Mika Kintzel, Emma E. Cawood, Jonathan Bailey, Sarah Maslen, Yew Mun Yip, Mason Wakley, Ioannis G. Riziotis, Thomas W. Rees, Joanna Redmond, J. Mark Skehel, David House, Jacob Bush, Jeannine Hess   +15 more
wiley   +2 more sources

Unveiling the contribution of histidine-end-terminal pBAEs to endosomal escape using super-resCLEM imaging. [PDF]

Mater Today Bio
Navalón-López M, Andrian T, Albertazzi L, Borrós S, Fornaguera C, Pujals S.   +5 more
europepmc   +1 more source

Isosteric Engineering of Enzymes: Overcoming Activity–Stability Trade‐Offs by Site‐Selective CH → N Substitutions

Angewandte Chemie, EarlyView.
Coupling biosynthetic noncanonical amino acid production with genetic code expansion enables site‐specific incorporation of azatryptophans into PET‐degrading enzymes (PETases). By isosteric single‐atom editing of a conserved tryptophan, AzaPETases break the activity–stability trade‐off, delivering higher catalytic efficiency at elevated temperature and
Elwy H. Abdelkader, Haocheng Qianzhu, Gottfried Otting, Thomas Huber   +3 more
wiley   +2 more sources

Unraveling A4GALT Mechanism and Its Modulation With Adamantyl‐Galactosylceramide Analogues: Advancing Fabry Disease Therapeutic Strategies

Angewandte Chemie, EarlyView.
A 310‐helix‐mediated conformational switch promotes a front‐face SNi‐like catalysis by human A4GALT. Mechanism‐guided design identifies AdaGalCer as a selective modulator of globotriaosylceramide (Gb3) biosynthesis, opening a clear route toward new Fabry disease therapeutics.
Nicky de Koster, Òscar Vidal‐Gironès, Rowan de Graaf, Ken Kok, Lindsey T. Lelieveld, Jackelien Hoogervorst, Maria J. Ferraz, José Pablo Rivas‐Fernández, Rob F. Lammers, Herman S. Overkleeft, Johannes M. F. G. Aerts, Rolf G. Boot, Carme Rovira, Marta Artola   +13 more
wiley   +2 more sources

Cobalt(III)-Schiff Base Coordination to Nsp1, a SARS-CoV-2 Protein. [PDF]

Inorg Chem
Morales M, Yang MY, Goddard WA, Gray HB, Winkler JR.   +4 more
europepmc   +1 more source

Metal Oxides Catalyze Formation of Dehydroamino Acids by Phosphate β‐Elimination Under Physiological Conditions

Angewandte Chemie, EarlyView.
Dehydroamino acids (DHAA) are atypical electrophilic sites that lead to crosslinked proteins in Alzheimer's disease (AD) brains. No catalyst for their formation has been known in humans. We report that metal oxides catalyze β‐elimination of phosphoserine and phosphothreonine in model peptides at pH 7.5°C and 37°C, yielding DHAAs.
Samuel W. Markovich, Brian L. Frey, Mark Scalf, Lloyd M. Smith   +3 more
wiley   +2 more sources

The Pharmacology of the SLC15A4-TASL Complex, an Emerging Target for the Treatment of Lupus. [PDF]

Pharmacol Res Perspect
Wilkinson AL, Popat D, Sengmany K, Silva MC, Charlton SJ, Lay CS.   +5 more
europepmc   +1 more source

Osteoarthritis pain inversely correlates with histidine and glutamine following CSF and serum profiling. [PDF]

Arthritis Res Ther
Dunstan IK, Rasmussen LJH, Probert F, Olsen DA, Madsen JS, Eugen-Olsen J, Enggaard TP, Varnum C, Lambertsen KL, Anthony DC, Blichfeldt-Eckhardt MR.   +10 more
europepmc   +1 more source

Histidine in urine. 2 [PDF]

Biochemical Journal, 1941
openaire   +2 more sources

Formulation Development of a Multivalent Bioconjugate ExPEC Vaccine Candidate: Linking Early Design to Late-Stage Stability and Manufacturability. [PDF]

Vaccines (Basel)
Opacic M, Labovitiadi O, de Goede P, Capelle MAH.   +3 more
europepmc   +1 more source