Racemisation of Amino Acids: From Synthetic Challenge to Biological Significance
Racemisation, once considered an undesirable synthetic side reaction, also occurs naturally in amino acids and influences biological processes. Evidence links stereochemical conversion to ageing, protein turnover, and cellular development. This review examines mechanisms, control strategies in synthesis, applications and implications in physiology ...
Othman Al Musaimi
wiley +1 more source
Identification of Urethanases for Biocatalytic Recycling of Toluene Diisocyanate- and Methylene Diphenyl Diisocyanate-Based Polyurethanes. [PDF]
Pastor L +7 more
europepmc +1 more source
Trans‐cyclooctene‐modified 5′‐Cap analogues provide a platform for bioorthogonal modulation of mRNA translation. A controlled synthetic strategy enabled access to functionalized Caps that attenuate translation and permit partial restoration upon tetrazine addition.
Niclas Zips +2 more
wiley +1 more source
3-Component reactions for accessing heterocycle-rich topologies: trapping of pyrrole-stabilized carbenes <i>via</i> net bimolecular C-H or N-H insertion. [PDF]
Guzman AL, Toll KB, Hoye TR.
europepmc +1 more source
We developed new derivatives of the cancer drug ponatinib, significantly reducing and altering its spectrum of target kinases. Compound 5 retained the efficacy in inhibiting the colony formation of MDA‐MB‐231 cells and acted primarily on B‐Raf and Flt‐1 as its main targets in a kinase panel.
Tobias Betzholz +7 more
wiley +1 more source
Discovery of orally active and serine-targeting covalent inhibitors against hCES2A for ameliorating irinotecan-triggered gut toxicity. [PDF]
Zhang Y +15 more
europepmc +1 more source
Design and Synthesis of Pyrimidino[4,5‐d]Pyrimidine‐Based Compounds as Potent B‐RAF V600E Inhibitors
Novel pyrimido[4,5‐d]pyrimidine‐based inhibitors selectively target B‐RAF V600E with nanomolar affinity and adopt distinct type‐II binding modes. Complementary cellular profiling reveals highly active analogs, underscoring the versatility of this chemotype and establishing it as a promising scaffold for the development of next‐generation kinase ...
Eleftheria A. Georgiou +10 more
wiley +1 more source
Transformation of Linear Alkenyl <i>N</i>-Alkoxy Carbamates into Cyclic Bromo Carbonates. [PDF]
Sathyamoorthi S, Kelley SP.
europepmc +1 more source
Probing 3‐Amino‐2H‐Azaindazoles as Allosteric Inhibitors of the Protein Tyrosine Phosphatase SHP2
A palladium‐catalyzed domino reaction facilitated the discovery and rapid synthesis of selective, potent 3‐amino‐2H‐azaindazole derivatives serving as allosteric inhibitors of SHP2. Structural analysis via co‐crystallography confirmed binding at the allosteric site, thereby stabilizing the autoinhibited SHP2 conformation, qualifying this scaffold as a ...
Machoud Amoussa +20 more
wiley +1 more source

