Results 201 to 210 of about 47,089 (385)

Development of a Partial Proteolysis Targeting Chimera Library Based on Achiral Cereblon E3 Ligase Ligands and its Application for Bruton's Tyrosine Kinase Degraders

open access: yesChemMedChem, EarlyView.
A partial proteolysis targeting chimera (PROTAC) library bearing achiral phenyl dihydrouracil cereblon ligands is prepared. It is then applied to the rapid development of a full PROTAC library targeting Bruton's tyrosine kinase, which can be directly used for screening.
Chelsi M. Almodóvar‐Rivera   +5 more
wiley   +1 more source

Development of Keap1‐Nrf2 Protein–Protein Interaction Inhibitor Activating Intracellular Nrf2 Based on the Naphthalene‐2‐acetamide Scaffold, and its Anti‐Inflammatory Effects

open access: yesChemMedChem, EarlyView.
Pyrrolidine‐type naphthalene‐2‐acetamide compound 5i inhibits Kelch‐like ECH‐associated protein 1 (Keap1)‐nuclear factor erythroid 2‐related factor 2 (Nrf2) protein–protein interaction by binding to the Keap1‐DC domain; it subsequently activates intracellular Nrf2 and induces Nrf2‐target genes.
Daisuke Yasuda   +11 more
wiley   +1 more source

AgamOBP1‐Directed Discovery of Repellents to Control the Spread of Mosquito‐Borne Diseases

open access: yesChemMedChem, EarlyView.
Toward the discovery of novel mosquito repellents, a library of potential binders of AgamOBP1 (secondary amines) generated from two amines and seven aldehydes was designed aiming to enable interactions with critical amino acids at the DEET‐site and to bridge the DEET‐ and Icaridin sIC‐binding pockets. 1H STD NMR spectroscopy in the presence of AgamOBP1
Evanthia Chazapi   +10 more
wiley   +1 more source

Enantioselective Synthesis of α-(Hetero)aryl Piperidines through Asymmetric Hydrogenation of Pyridinium Salts and Its Mechanistic Insights.

open access: yesOrganic Letters, 2018
Bo Qu   +20 more
semanticscholar   +1 more source

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of 18F‐Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3

open access: yesChemMedChem, EarlyView.
Fluorinated peptidomimetics targeting muscarinic acetylcholine receptor subtype M3: Fluorinated peptidomimetic compounds based on a β‐alanine‐glycine scaffold, with lead compound 24 demonstrating high M3 selectivity and submicromolar potency. The first M3‐selective positron emission tomography radioligand, [18F]24, is synthesized and will be evaluated ...
Miguel A. Herrera‐Rueda   +4 more
wiley   +1 more source

Home - About - Disclaimer - Privacy