Results 181 to 190 of about 45,916 (341)
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
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
New Aryl-1,3-thiazole-4-carbohydrazides, Their 1,3,4-Oxadiazole-2- thione, 1,2,4-Triazole, Isatin-3-ylidene and Carboxamide Derivatives. Synthesis and Anti-HIV Activity [PDF]
Mehwash Zia +3 more
openalex +1 more source
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
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]
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
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
Piezogravimetric investigation of heterocyclic compounds as potential inhibitors against copper corrosion in acidic media [PDF]
Nyikos, Lajos +2 more
core +1 more source
QSAR study of anti-prion activity of 2-aminothiazoles [PDF]
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]
W J, Robbins, F, Kavanagh
openaire +2 more sources

