Life Science Spotlight
Recent advances in drug discovery, synthetic and medicinal chemistry, chemical biology and related areas.
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Nickel-Mediated Protein Arylation Inside Living Cells
While transition metals drive powerful bond-forming reactions in synthetic chemistry, their use for covalent modification of biomolecules has been largely underexplored…
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When One Catalytic Cycle Is Not Enough
The installation of alkyl substituents through C(sp³)-C(sp³) coupling is in high demand in synthetic and medicinal chemistry. While some strategies towards…
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Accessing Spirocyclic Ethers via Chemical Cascade with Carbyne Equivalents
We chemists love building molecular complexity efficiently and in as few steps as possible. This allows us to transform readily accessible…
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Alcohols as Building Blocks for C-C Cross Coupling
Until now, direct activation of the C─O bond was an unresolved problem, mainly due to high dissociation energy (approximately 96 kcal/mol)…
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Cracking the Oncogenic Star Player KRAS
KRAS has been in the focus of cancer research for quite some time as it has been recognized as a key…
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Design, Development and Optimization of RIPK1 Degrader
Optimization of PROTACs for in vivo applications is non-trivial, thought not impossible. A nice example on this topic represents freshly published…
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Rewriting Chemistry Textbooks: From Alkene to Alkyne via Hetero-Diels-Alder Reaction
Although Hetero-Diels-Alder will play a central role, I am not going to speak about gender. Not today. Instead, I would like…
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Breaking New Ground in mRNA Degradation
About 85% of disease-related proteins lack suitable binding pockets for conventional drug discovery. While RNA-targeting approaches like siRNAs have shown promise…
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Nano-PROTACs Are Gaining Traction
The field of PROTACs continues to evolve. A recent Nature Communications paper describes another self-assembling nano-PROTAC that co-degrades androgen receptor (AR)…
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Is It PROTAC or Molecular Glue? … It Is Both!
Researchers often steer the design of CRBN-based PROTACs to achieve selective degradation of a single target while suppressing degradation of CRBN…
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Smart Molecules Targeting Cancer Powerhouse
How can bioorthogonal chemistry and mitochondrial targeting rewrite cancer immunotherapy? By creating enzyme-responsive nanoparticles that self-assemble in tumors and chemically “click”…
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Are Alpha Emiters the Future of Radiotherapy?
While biotech faces a funding downturn, radioligand therapy (RLT) is attracting major investments. The field stands at an important inflection point…
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Let’s Hijack DCAF2 for TPD?!
Well, not quite yet. But maybe soon. Frontier Medicines evaluated E3 ligase DCAF2 (DTL/CDT2), as a novel ligase for targeted protein…
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PROTAC vs Molecular Glue
It doesn’t happen very often to see a direct comparison of a molecular glue degrader and PROTAC, as it has been…
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Introducing mgTag and cTag
How do you study the 90% of proteins that lack small-molecule binding partners? By tagging the protein! The problem is that…
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From DNA Code to Chemistry
Sumon Pratihar, Eric T. Kool and his team from Stanford University just published new paper in 𝘈𝘯𝘨𝘦𝘸𝘢𝘯𝘥𝘵𝘦 𝘊𝘩𝘦𝘮𝘪𝘦, unlocking a new…
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Why Would You Biotinylate Ubiquitin?
E-STUB: A Precision Tool for Mapping E3 Ligase Substrates In march 2025, colleagues from Dana Faber and The Broad Institute published…
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Think sp³ Rich!
Top notch medchem building blocks got unlocked. Chemists from Enamine Ltd. published a robust route to saturated azabicyclic scaffolds (Angewandte Chemie):…
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A Unified Platform for Nucleoside Analog Synthesis
Why nucleoside analogs matter and why they’re hard to make Nucleoside analogs (NAs) are among the most successful drug classes in…
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BRET: State-Of-The-Art Technology for Target Engagement in Living Cells
Direct monitoring of a binding interaction between biomolecules and their ligands is one of the cornerstones of early drug discovery, chemical…
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Breakthrough in Cross‑Coupling Chemistry
Wang et al. report a new copper-catalyzed methodology for C(sp³)-N cross-coupling of unactivated alkyl halides with diverse nucleophiles under thermal conditions…
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Curious How Drug Discovery Can Be Accelerated by DEL‑ML?
Then I would like to invite you to read our paper in RSC Chem. Biol. which also represents my first corresponding…
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Editing Protein Backbone Inside Living Cells
For decades, creating proteins with extended backbones (β, γ, δ-amino acids) inside living cells has been challenging. Researchers at University of…
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Drugging the “Undruggable” 💊
🔸 50 new CRBN neosubstrates🔸 3 bona fide degraders🔸 MS-proteomic platform expanding druggable proteome All of this packed in single paper❗…
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Nine New TRIM PRYSPRY Structures Uncover Key Drug Design Challenges
My colleagues from The Structural Genomics Consortium (SGC) (Rezart Zhubi, Andreas C. Joerger, Stefan Knapp) just published a paper “𝐒𝐭𝐫𝐮𝐜𝐭𝐮𝐫𝐚𝐥 𝐚𝐧𝐚𝐥𝐲𝐬𝐢𝐬…
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Let it GLOW: Novel Proximity Inducing Modality for DNA Modification
DNA methyltransferases (MTases) can recognize specific DNA sequences and transfer a methyl group from the S-adenosyl-L-methionine (SAM) cofactor to a target…
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Unexpected Organo-Catalysis
Researchers from The Chinese University of Hong Kong discovered an alternative mechanism in which organo-selenium acts as a C-H hydrogen bond…
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Discovery of Small-Molecule Ligands for the E3 Ligase STUB1/CHIP
Finding potent small-molecule E3 ligase binders is notoriously tough. Here’s how teams from AstraZeneca, Pharmaron, and X‑Chem collaborated to overcome this…
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Group-Transfer Chimeras for Induced Proximity (GRIPs)
Induced proximity is more than ubiquitination and targeted protein degradation. In the recent literature we have seen proximity-inducing modalities for phosphorylation…
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Spiro Spiro Spirocycles Everywhere.
The number of spirocyclic-N-heterocycles has increased dramatically in the recent years. From 10,000 in 2023 ➡️ 90,000 in 2025 (Substructure search…
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Skeletal Editing Strikes Back!
Imagine a scaffold hopping strategy where you don’t have to re-design your synthetic route for each scaffold. You don’t need Jedi…
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From serendipity to essential protac profiling
The microcosmos of biological processes is complex and full of surprises. This is also the case for a new preprint from…
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Metal-Free C–N coupling via Smiles Rearrangement
Do you like to Smile? Or perhaps you’re a fan of rearrangement reactions like me? If so, you’ll want to check…
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Carbon–Heteroatom Cross-Coupling via Red-Light Metallaphotocatalysis
Recently published paper in Nature Communications claims (as the title says): “General method for carbon–heteroatom cross-coupling reactions via semiheterogeneous red-light metallaphotocatalysis”…
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A Biocompatible Lossen Rearrangement in Escherichia Coli
Forget your fume hood, E. coli just became your new reaction vessel 💡 What’s new?Researchers have shown that a classic organic transformation…
