#ChemPro

Stephan Hacker

@stephanhacker2.bsky.social

2 weeks ago

#ABPP2027 will be happening in Leiden on June 2nd to 4th, 2027.

I am excited to be part of the organization together with an amazing team.

Sign up for our mailing list here: www.universiteitleiden.nl/en/science/l...

#ABPP #ChemoProteomics #ChemPro #ProteoProbes #ChemSky #ChemBio #DrugDiscovery

15th International ABPP Meeting

@abpp2027.bsky.social

2 weeks ago

#ABPP #ChemoProteomics #ChemPro #ProteoProbes #ChemSky #ChemBio #DrugDiscovery

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

#ChemBio #ChemSky #ChemPro #ProteoProbes #CovalentInhibitors

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Designer Aromatic Cations for Photo-Induced Protein Ligation, Imaging, and Intracellular Labelling at Extended Wavelengths Photo-induced protein labelling strategies have become essential tools in chemical biology, but most strategies require high energy wavelengths of light as input to drive reactivity. Recently, we reported a biocompatible method for engaging photo-induced electron transfer to drive protein labelling using biaryl pyridinium salts and, here, we report the design of a series of aromatic cation salts that trigger this process using longer wavelengths of light while maintaining a sterically minimal profile. We achieved this through the systematic study of structure-reactivity relationships of various donor-acceptor pyridinium salts possessing extended conjugation, and these studies revealed the need of a constrained trans -stilbene relationship between the probe’s donor and acceptor substituents in order to achieve protein labelling. Probes with chromene-based donor groups in particular showed either robust protein labelling, significant fluorescence quantum yields, or state-dependent photophysical properties; in turn enabling the same probes to be used for both photo-induced protein labelling and wash-free live-cell imaging. We also demonstrate that these enhanced probes possess robust reactivity in complex biological environments through green light-triggered intracellular labelling in live HeLa cells, resulting in the identification of 659 enriched proteins. This series of experiments not only demonstrates the ability of this latest generation of probes to engage in photo-induced labelling using lower energy light in complex proteomes, but also reveals new capabilities for photophysical state-dependent reactivity and measurements. ![Figure][1]</img> ### Competing Interest Statement The authors have declared no competing interest. National Institute of General Medical Sciences, R35 GM143120 U.S. National Science Foundation, https://ror.org/021nxhr62, 1920234, 840336, 9214383, 9729350 [1]: pending:yes

Interesting @biorxivpreprint.bsky.social by the group of Michael Taylor. They designed new derivatives of N-substituted pyridinium salts for tryptophan labeling that allow labeling of the proteome with green light.

www.biorxiv.org/cont...
#ChemSky #ChemBio #ABPP #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

#Chemistry #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes #DrugDiscovery #Glycotime #Peptides #Materials #Synthesis #Undruggable #CovalentInhibitors
(3/3)

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Chemical proteomic profiling reveals prostaglandin termination enzyme PTGR2 as a key molecular target of natural coumarin fraxetin Natural coumarins represent a diverse group of secondary metabolites with a wide range of biological activities. However, their specific molecular targets have remained largely unexplored. Employing chemical proteomics, a comprehensive analysis of the protein targets of the natural coumarin fraxetin has been

Interesting talk by Weining Zhao at #ISCPDD. He talked about the use of #ChemicalProteomics to study the target proteins of Fraxetin. They identified PTGR2 as a relevant target in human cells.

pubs.rsc.org/en/cont...
#ABPP #AfBPP #ChemSky #ChemBio #ProteoProbes #ChemPro

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Very excited to visit Radboud University Nijmegen today and to speak at the Institute for Molecules and Materials (IMM) colloquium. Looking forward to a full day of scientific exchange.

Thank you so much for inviting me, Kevin Neumann. (1/2)

#ChemSky #ChemBio #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

It was great that I could present our work at #ISCPDD. I focused on the isoDTB tags (onlinelibrary.wiley....) and our recent Nature Chemistry publication on the selectivity of diverse electrophiles (www.nature.com/artic...).
#ChemBio #ChemSky #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

FAD-dependent enzyme-catalysed intermolecular [4+2] cycloaddition in natural product biosynthesis - Nature Chemistry A naturally occurring stand-alone and intermolecular Diels–Alderase, MaDA, has been identified from Morus alba cell cultures. MaDA is a FAD-dependent enzyme, which catalyses the intermolecular [4+2] c...

Great talk by Xiaoguang Lei at #ISCPDD. He talked about the use photoaffinity probes based on biosynthetic intermediates to fish for the relevant enzymes to identify e.g. an intermolecular Diels-Alderase.
www.nature.com/articles/s41...
#ChemSky #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Great to see our Nature Chemistry paper out in its final published and printed form.

If you want to check it out, you can find it here: www.nature.com/articles/s41...

#ChemSky #ChemBio #ChemicalProteomics #Chemoproteomics #ProteoProbes #ChemPro

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Great talk by Clive Chung at #ISCPDD. He presented his work on #ChemcalProteomics to find cysteine-directed covalent inhibitors. Exciting insights into NAIA chemistry and into the application to specific proteins of interest.
www.nature.com/articles/s41...
#ChemSky #ChemBio #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

Geat talk by Yu Rao at #ISCPDD. He talked about his group’s work on PROTACs and the use of degradation-based protein profiling (DBPP) to characterize target engagement.
advanced.onlinelibrary.wiley.com/doi/10.1002/...
#TPD #ChemSky #ChemBio #DrugDiscovery #ChemicalProteomics #ChemPro #ProteoProbes

Stephan Hacker

@stephanhacker2.bsky.social

3 months ago

They also compared their identified ligand binding sites to those predicted by Boltz-2. They find that Boltz-2 predicts orthosteric binding well, but tends to also localize non-orthosteric binders to the orthosteric binding site. (2/2)
#ChemSky #ChemBio #ChemicalProteomics #ChemPro #ProteoProbes

Quinn Sievers

@quinnsievers.bsky.social

3 months ago

#chempro