A large variety of chemistry‐based ubiquitin probes have been developed. ABSTRACT Ubiquitin (Ub) and ubiquitin‐like proteins (Ubls) orchestrate diverse cellular processes through reversible post‐translational modification of target proteins. Their conjugation is governed by a cascade of E1 activating, E2 conjugating, and E3 ligating enzymes, while ...
Saibal Chanda, Wenshe Ray Liu
wiley +2 more sources
A generalizable assay for intracellular accumulation to profile cytosolic drug delivery in mammalian cells. [PDF]
Bhandari S +6 more
europepmc +1 more source
Harnessing Methyltransferase‐Guided Targeting for Sequence‐Specific Proximity Labeling of DNA
A novel methyltransferase‐mediated approach leveraging rationally designed S‐adenosyl‐L‐methionine (SAM) analogues was developed to achieve sequence‐specific DNA labeling but in proximity to the natural transfer site, addressing key limitations of previously established methods, including ligand instability and methylation‐sensitive labeling.
Xiong Chen +8 more
wiley +2 more sources
Click-based determination of accumulation of molecules in Escherichia coli. [PDF]
Ongwae GM +13 more
europepmc +1 more source
Fluorine‐18‐labeled CD73 inhibitor [18F]PSB‐19427 enables noninvasive PET mapping of CD73 overexpression in triple‐negative breast (TNBC) and pancreatic cancer. For [18F]PSB‐19427, specific binding in human tumor tissues, favorable biodistribution with prolonged blood retention, robust tumor uptake, and superiority to [18F]FDG in a TNBC model ...
Clemens Dobelmann +23 more
wiley +2 more sources
On-DNA Platform Molecules Based on a Diazide Scaffold II: A Compact Diazide Platform Designed for Small-Molecule Drug Discovery. [PDF]
Miyachi H, Koshimizu M, Suzuki M.
europepmc +1 more source
Trisoxazole Macrolides Potentiate the Microtubule Assembly and Antimitotic Activities of Taxanes
Photoaffinity experiments identified tubulin as a new target of mycalolides. Though weakly cytotoxic, the trisoxazole macrolactone moiety enhanced paclitaxel's microtubule assembly and antimitotic effects. Molecular modeling studies suggested that MyC stabilizes α/β‐tubulin heterodimer interactions.
Shohei Ebihara +4 more
wiley +2 more sources
Enabling the synthesis of multi-payload thio-antibody conjugates through the use of pyridazinediones, <i>p</i>-anisidine derivatives and various click chemistries. [PDF]
McMahon C +9 more
europepmc +1 more source
The Copper-Catalyzed Azide-Alkyne Cycloaddition Reaction: Why Two Is Faster than One. [PDF]
Vermeeren P.
europepmc +1 more source
We developed a novel domino polymerization to synthesize reductively degradable poly(disulfide)s with tunable side chains. A novel monomer bearing thiolactone and pyridyl disulfide groups reacts with various amines, enabling continuous ring‐opening and disulfide exchange.
Yukiya Kitayama +2 more
wiley +2 more sources

