129086-10-8Relevant academic research and scientific papers
Site-specific protein PEGylation catalyzed by endo-β-N-acetylglucosaminidase
Goto, Kohtaro,Kurogochi, Masaki,Takashima, Shou,Mori, Masako,Matsuda, Akio,Mizuno, Mamoru
, (2020)
We demonstrated a novel site-specific method of protein PEGylation that is catalyzed by endo-β-N-acetylglucosaminidase (ENGase) with PEGylated oxazoline (1) as a donor. PEGylation via transglycosylation using 1 proceeded smoothly to GlcNAc compounds such as p-nitrophenyl N-acetylglucosaminide and RNase B derivatives.
IRAK DEGRADERS AND USES THEREOF
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, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
ALANINE-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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, (2017/02/09)
The description relates to inhibitors of Apoptosis Proteins (TAPs) binding compounds, including Afunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the IAP E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
A convenient synthetic route to differentially functionalized long chain polyethylene glycols
Burns,Field,Hashimoto,Petteys,Ridley,Samankumara Sandanayake
, p. 2337 - 2347 (2007/10/03)
A convenient and efficient synthetic route to differentially functionalized polyethylene glycols (PEGs) starting from cheap commercially available materials is reported. Selectively protected triethylene glycol or tetraethylene glycol have been reacted with a second PEG bearing both a protecting group and a leaving group.
Lack of effect of the length of oligoglycine- and oligo(ethylene glycol)-derived para-substituents on the affinity of benzenesulfonamides for carbonic anhydrase II in solution
Jain, Ahamindra,Huang, Shaw G.,Whitesides, George M.
, p. 5057 - 5062 (2007/10/02)
Using 1H NMR spectroscopy, values of T2 have been determined for the methylene protons of the oligoglycine moieties of para-substituted benzenesulfonamides having structures H2NO2SC6H4CO(Gly)(n)OH (n = 1-6) bound at the active site of bovine carbonic anhydrase II (CA, EC 4.2.1.1). These values have been correlated with measurements of dissociation constants of these complexes, in order to infer motion of these ligands when bound to the enzyme. Motion of glycines 1-3 (those closest to the aryl ring) is hindered by their proximity to the protein; motion of glycines 4-6 is relatively unhindered. Despite the restriction to motion inferred for glycines 1-3, the values of K(d) for the six compounds (n = 1-6, 1-6) are indistinguishable within experimental uncertainty (± 20%): K(d) in μM (n) 0.30 (1); 0.26 (2); 0.33 (3); 0.37 (4); 0.37 (5); 0.34 (6). There is, therefore, an unexpected compensation of the loss in conformational entropy on binding by another contributor to the free energy.
A Novel Procedure for the Synthesis of Ether-Bridged Perfluoro Non-Ionic Surfactants
Selve, C.,Achilefu, S.,Mansuy, L.
, p. 799 - 807 (2007/10/02)
An efficient procedure is described for the synthesis of perfluoro non-ionic surfactants of the type RF-CH2(OC2H4)pOH which involves the use of the principle of solid-liquid phase transfer methodology to simplify the Williamson ether synthesis usually employed in previous procedures.
