Results 181 to 190 of about 45,916 (341)

Gezielte Modulation des spliceosomalen Proteins USP39 durch allosterische Liganden und PROTAC‐induzierte Degradation

open access: yesAngewandte Chemie, Volume 138, Issue 5, 28 January 2026.
Proteolysis‐targeting Chimeras (PROTACs) ermöglichen die gezielte Degradation bislang als „undruggable“ geltende Proteine über das zelluläre Ubiquitin–Proteasom‐System. In dieser Studie identifizieren Schäfer et al. thiazolbasierte niedermolekulare Liganden, die allosterisch an die Zinkfinger‐Domäne der Ubiquitin‐spezifischen Protease 39 (USP39) binden
Daniel Schäfer   +11 more
wiley   +1 more source

Targeting the Spliceosomal Protein USP39 Through Allosteric Ligands and PROTAC‐Induced Degradation

open access: yesAngewandte Chemie International Edition, Volume 65, Issue 5, 28 January 2026.
Proteolysis‐targeting chimeras (PROTACs) enable degradation of proteins previously considered undruggable by harnessing the cellular ubiquitin–proteasome system. In this study, Schäfer et al. identify thiazole‐based small molecules that allosterically bind the zinc finger domain of ubiquitin‐specific protease 39 (USP39), a non‐enzymatic scaffold ...
Daniel Schäfer   +11 more
wiley   +1 more source

Pseudotetraivprolide aus Pseudomonas entomophila liefern Einblicke in die Biosynthese von Detoxin/Rimosamid‐ähnlichen Anti‐Antibiotika

open access: yesAngewandte Chemie, Volume 138, Issue 4, 22 January 2026.
Pseudotetraivprolid ist ein neuer Akteur unter den Detoxin/Rimosamid‐ähnlichen Naturstoffen. Die Biosynthese erfordert FabD aus dem Primärstoffwechsel und einen PipDFG‐Komplex für die Acetylierung im letzten Schritt – wodurch schließlich die anti‐antibiotische Wirkung entsteht.
Edna Bode   +13 more
wiley   +1 more source

Water Networks as Hydrophobic Recognition Motifs in Proteins

open access: yesAngewandte Chemie, Volume 138, Issue 2, 9 January 2026.
Hydrophobic groups can strengthen confined water networks, promoting order that propagates through the protein structure and drives recognition, creating a paradoxical hydrophobic binding hot spot. Polar groups are rejected because they disrupt the network, destabilizing the protein structure.
Serena G. Piticchio   +12 more
wiley   +2 more sources

The Trials and Tribulations of Structure Assisted Design of KCa Channel Activators. [PDF]

open access: yes, 2019
Calcium-activated K+ channels constitute attractive targets for the treatment of neurological and cardiovascular diseases. To explain why certain 2-aminobenzothiazole/oxazole-type KCa activators (SKAs) are KCa3.1 selective we previously generated ...
Brown, Brandon M   +6 more
core  

Pseudotetraivprolides from Pseudomonas entomophila Provide Insights into the Biosynthesis of Detoxin/Rimosamide‐Like Anti‐Antibiotics

open access: yesAngewandte Chemie International Edition, Volume 65, Issue 4, 22 January 2026.
Pseudotetraivprolide is a new player among the Detoxin/Rimosamide‐like natural products! Its biosynthesis requires FabD from primary metabolism and a PipDFG complex for final‐step acetylation – unlocking its anti‐antibotic activity. Abstract Novel variants of known natural product (NP) classes can provide valuable insights into their biosynthesis ...
Edna Bode   +13 more
wiley   +1 more source

QSAR study of anti-prion activity of 2-aminothiazoles [PDF]

open access: yes, 2012
2-aminothiazoles is a class of compounds capable of treating life-threatening prion diseases. QSAR studies on a set of forty-seven 2-aminothiazole derivatives possessing anti-prion activity were performed using multivariate analysis, which comprised of ...
Isarankura-Na-Ayudhya, Chartchalerm   +4 more
core  

Thiazole Effect on Phycomyces [PDF]

open access: yesProceedings of the National Academy of Sciences, 1941
W J, Robbins, F, Kavanagh
openaire   +2 more sources

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