Results 161 to 170 of about 268,204 (256)

Ac‐SDKP modulates apoptosis via HSP27 and the FAS/FASL and mitochondrial axes

Animal Models and Experimental Medicine, EarlyView.
Schematic diagram of Ac‐SDKP regulating the FAS/FASL and mitochondrial apoptosis pathways via HSP27. Ac‐SDKP inhibits HSP27 expression, activates the FAS/FASL pathway and Caspase‐3 signaling, increases Caspase‐8 and Caspase‐3 expression, and induces cell apoptosis.
Wenxin Guo, Jinyin Yan, Wenli Li, Jin Wang, Lu Liu, Chengmei Zhang, Wei Cao, Shanshan Yao, Haibo Gong, Yi He, Zihan Zhou, Siyan Chen, Li Feng, Haijing Deng   +13 more
wiley   +1 more source

Discovery of a Reversible Sub‐Picomolar Thrombin Inhibitor Using DCC

Angewandte Chemie, EarlyView.
An ultrapotent yet fully reversible trivalent thrombin inhibitor discovered through screening a large dynamic combinatorial library (DCL) of 125 000 members of self‐assembled fragments. The innovative approach leverages size‐exclusion‐based affinity selection, coupled with MALDI‐TOF mass spectrometry readout, enabling the full workflow to be completed ...
Millicent Dockerill, Richard J. Payne, Nicolas Winssinger   +2 more
wiley   +2 more sources

Metastasis suppressing properties of the cell-surface anchored serine protease prostasin: new functional and mechanistic insights from breast cancer. [PDF]

Oncogenesis
Lundgren JG, Flynn MG, Winkler AR, Rivera BN, Tanabe LM, Stemmer PM, Chen LM, Chai KX, List K.   +8 more
europepmc   +1 more source

Water, Alcohols, Amines, and Amides as Formal Hydrogen‐Atom‐Transfer Reagents Through Activation With Redox‐Active Lewis Acids

Angewandte Chemie, EarlyView.
Protic molecules containing strong O─H or N─H bonds typically resist hydrogen‐atom abstraction because of the high reactivity of the resulting heteroatom‐centered radicals. However, association of the protic molecules with redox‐active Lewis acids can provide powerful hydrogen‐atom donors or proton‐coupled‐electron‐transfer reagents.
Petra Vojáčková, Armido Studer
wiley   +2 more sources

Cytokine Milieu Relevant to Atopic Dermatitis Enhances Epidermal Trypsin-Like Serine Protease Activity, Which Is Pharmacologically Suppressed in Human Keratinocytes. [PDF]

J Dermatol
Onishi S, Yasutomi Y, Tsedendorj O, Morizane S.   +3 more
europepmc   +1 more source

Biophysical and Functional Characterization of a Thermally Stable Bifunctional Serine Protease Inhibitor from <i>Cleome viscosa</i> Seeds. [PDF]

Int J Mol Sci
Radhakrishnan M, Senthilvadivelu V, Nadendla EK, Sivashanmugan K, Krishnasamy G.   +4 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

Phosphorylation of EF-P aggravates Streptococcus suis-induced blood-brain barrier damage by enhancing serine protease production. [PDF]

Vet Res
Yin H, Tian Y, Zhou Z, Lang S, Li Y, Peng L, Li J, Fang R.   +7 more
europepmc   +1 more source

Evolution of Catalysis in the Serine Proteases

Cold Spring Harbor Symposia on Quantitative Biology, 1987
J N, Higaki, B W, Gibson, C S, Craik
openaire   +2 more sources

A Comprehensive 19F NMR Framework for Fragment‐Based Drug Discovery: The Validated Screening Library OpenFL600 and Efficient Affinity Ranking by CSAR

Angewandte Chemie, EarlyView.
NMR screening is a powerful method for hit detection in drug‐discovery. We designed and validated the OpenFL600 19F$^{19}{\rm F}$ NMR library to probe diverse targets, including RNA, GPCRs, kinases, and proteases. This library yields target‐specific ligands without generating promiscuous binders.
Simon H. Rüdisser, Gabriela Stadler, Giacomo Padroni, Daria Barbash, Marco M. Ruckstuhl, Nils Lorz, Christina Jordan, Sarah Skibinski, Timo T. Stühlinger, Sarah E. Kratzwald, Katharina M. Siess, Sven Brüschweiler, Gerald Platzer, Antoine Cléry, Robert Konrat, Frédéric H.‐.T. Allain, Alvar D. Gossert   +16 more
wiley   +2 more sources