Results 201 to 210 of about 39,817 (294)

Hijacking the MDM2 E3 Ligase with novel BRD4‐Targeting PROTACs in Pancreatic Cancer Cells

ChemBioChem, Accepted Article.
The phenotypic effect induced by a Proteolysis‐Targeting Chimera (PROTAC) can depend on several factors, including the E3 ligase recruited. For the discovery of a first‐in‐class PROTAC for a target of interest, the E3 ligases commonly hijacked remain the Von Hippel‐Lindau (VHL) and Cereblon (CRBN) since potent and accessible ligands are readily ...
Mihaela Ficu, Dan Niculescu-Duvaz, Mohammed Aljarah, Caroline Springer, Christopher S. Kershaw   +4 more
wiley   +1 more source

Asymmetric Synthesis of Noradamantane Scaffolds via Diphenylprolinol Silyl Ether-Mediated Domino Michael/Epimerization/Michael (or Aldol)/1,2-Addition Reactions. [PDF]

Angew Chem Int Ed Engl
Daskalakis K, Umekubo N, Indu S, Kawauchi G, Taniguchi T, Monde K, Hayashi Y.   +6 more
europepmc   +1 more source

Multifunctional Heterocyclic Scaffolds for Hybrid Lewis Acid/Lewis Base Catalysis of Carbon–Carbon Bond Formation [PDF]

, 2016
Benoit, Adam R., Dockendorff, Chris, Huff, Raechel, Lindeman, Sergey, Meyle, Elisia, Porter, Jacob D., Wiedenhoeft, Dennis, Wu, Yibiao, Yeung, Teresa H.W.   +8 more
core   +1 more source

Proline Amide Catalyzes Formation of Toxic Crotonaldehyde from Acetaldehyde Under Physiologically Relevant Conditions

ChemBioChem, EarlyView.
Crotonaldehyde‐derived DNA lesions are reported in patients after ethanol exposure, which implies that crotonaldehyde is produced after ethanol ingestion. Here, we show that proline amide, which mimics N‐terminal proline residues on human proteins, can catalyze crotonaldehyde formation from the ethanol metabolite acetaldehyde under physiologically ...
Liam A. Thomas, Vicki L. Emms, Dipti Vashi, Louise Fairall, John W. R. Schwabe, Richard J. Hopkinson   +5 more
wiley   +1 more source

Catalytic and Enantioselective Synthesis of Inherently Chiral Saddle-Shaped Compounds by [2 + 2 + 2] Cycloaddition of 1,8-Naphthylene-Based 1,10-Diynes with Alkynoates. [PDF]

Chemistry
Shibata T, Nakada M, Senda K, Ito M.
europepmc   +1 more source

Diversity of ThDP‐Dependent Enzymes Forming Chiral Tertiary Alcohols

ChemBioChem, EarlyView.
Chiral tertiary alcohols are widespread in nature and bioactive compounds; however, their asymmetric synthesis faces several challenges. This review outlines the toolbox of ThDP‐dependent enzymes able to produce tertiary alcohols through the formation of CC bond formation using ketones as acceptor substrates. Herein, the substrate scope, the diversity
Daniela Bjarnesen, Lucrezia Lanza, Francesco Presini, Pier Paolo Giovannini, Michael Müller   +4 more
wiley   +1 more source

<i>C</i> ₄-Symmetric Bowl-Shaped Diruthenium Tetracarboxylate Catalysts for Enantioselective C-H Functionalization Using Donor/Acceptor Carbenes. [PDF]

ACS Catal
Sailer JK, Bacsa J, Davies HML.
europepmc   +1 more source

Activity‐enhancing mutations in an LmrR‐based artificial metalloenzyme destabilize the protein scaffold and alter its conformational plasticity

ChemBioChem, Accepted Article.
Artificial metalloenzymes (ArM) hold great potential for the sustainable catalysis of complex new‐to‐nature reactions. To efficiently improve the catalytic efficacy of ArMs a rational approach is desirable, requiring detailed molecular insight into their conformational landscape.
Adil A. Safeer, Fabrizio Casilli, Wouter Beugelink, Gerard Roelfes, Marc Baldus, Hugo van Ingen   +5 more
wiley   +1 more source

Observation of the solvent enantio-isotope effect in asymmetric ring-opening of cyclic diaryliodoniums with selenocyanate. [PDF]

Chem Sci
Li Y, Tao C, Duan L, Gu Z.
europepmc   +1 more source

Mammalian Tolerance to Amino Acid Heterochirality

ChemBioChem, Accepted Article.
Organisms use amino acids predominantly in l‐configuration. On the other hand, a series of studies show that a variety of d‐amino acids also occur in mammals and amino acid homochirality is not complete. Mammals de novo synthesize most amino acids with l‐configuration, but serine and aspartate are converted from l‐ to d‐configuration by endogenous ...
Jumpei Sasabe, Sakiko Taniguchi, Kenichiro Adachi, Xuan Tran, Masataka Suzuki   +4 more
wiley   +1 more source