Communication
BrainBike peptidomimetic enables efficient transport of proteins across brain endothelium
BrainBikes, a new family of bicyclic brain shuttle peptides, can efficiently transport protein therapeutics across brain endothelium.
Paper
Identification and engineering of potent cyclic peptides with selective or promiscuous binding through biochemical profiling and bioinformatic data analysis
In this work different methods stemming from mRNA display were investigated toward developing potent binding cyclic peptides with distinct selectivity profiles against targets of a related protein family.
Paper
Covalent targeting of non-cysteine residues in PI4KIIIβ
The synthesis and characterisation of fluorosulfate covalent inhibitors of the catalytic lysine, a distal tyrosine or both residues in the lipid kinase PI4KIIIβ is described.
Paper
Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead
The first covalent cereblon-based PROTAC was developed using a fluorosulfate warhead to site-specifically engage His353 in the sensor loop of the E3 ligase, yielding a degrader with prolonged pharmacodynamics.
Paper
A covalent inhibitor of the YAP–TEAD transcriptional complex identified by high-throughput screening
A pyrazolopyrimidine-based inhibitor covalently targets the four TEAD paralogs, inhibiting YAP dependent cell growth and transcription.
Paper
A mitochondria-targeted chemiluminescent probe for detection of hydrogen sulfide in cancer cells, human serum and in vivo
Mitochondria-targeted chemiluminescent probe MCH enables visualization of hydrogen sulfide activity in cancer cells, human serum, and animal models.
Paper
Siderocalin fusion proteins enable a new 86Y/90Y theranostic approach
The mammalian protein siderocalin binds hydroxypyridinone complexes of trivalent rare-earth metals and f-elements through cation-π and electrostatic interactions. It can also be fused with biological vectors for the targeted delivery of imaging and therapeutic radionuclides.
Paper
Accessing three-branched high-affinity cereblon ligands for molecular glue and protein degrader design
The Petasis borono-Mannich reaction was employed for an entry towards three-branched cereblon ligands. The high-affinity ligands were used to assemble molecular glues and proteolysis targeting chimeras (PROTACs) targeting BRD4 for degradation.
About this collection
This collection highlights some of the very best work published in RSC Chemical Biology in 2023, hand-picked by our dedicated editorial team and the Editor-in-Chief, Prof Hiroaki Suga.