Waser Group

ECAB member Máté Bezdek t.co/FjAni1RhVZ favorite @helvchimacta.bsky.social article is the one of Alex Adronov because the authors elegantly craft a polymer with affinity for metallic tubes, yielding cleaner dispersions and films with enhanced conductivity doi.org/10.1002/hlca...

Last week, LCSO gathered for our annual Christmas dinner!🧀 We shared a delicious raclette, put our teamwork (and competitive spirit!) to the test with a fun quiz, and wrapped up the night with the… | ... Last week, LCSO gathered for our annual Christmas dinner!🧀 We shared a delicious raclette, put our teamwork (and competitive spirit!) to the test with a fun quiz, and wrapped up the night with the ver...

Last week the LCSO Christmas dinner took place!
www.linkedin.com/feed/update/...

Delighted to share our paper in @jacs.acspublications.org on π-extended Ru-COUBPY photosensitizers enabling one-photon 780 nm NIR in vivo #PDT. Fantastic collaboration with the Marchan Lab
doi.org/10.1021/jacs...

Diversifying the triquinazine scaffold of a Janus kinase inhibitor The exploration of novel three-dimensional scaffolds remains essential for expanding chemical space and discovering new bioactive molecules. Here, we describe a robust synthetic strategy that enables ...

🎊 Our latest paper "Diversifying the Triquinazine Scaffold of a Janus Kinase Inhibitor" by Kleni Mulliri, Kris Meier, Johanna-Dorothea Feuchter, Sacha Javor, Matheus A. Meirelles and Jean-Louis Reymond is published on RSC Medicinal Chemistry! Read the full version here 👉 pubs.rsc.org/en/content/a...

Flavin-Photocatalyzed Benzylic Functionalization, Spirocyclization, and Spiroepoxidation of Phenols para-Quinone methides (p-QMs) are versatile, transient electrophilic dearomatized intermediates in organic synthesis, enabling a range of transformations, such as cycloadditions, nucleophilic addition...

Photogenerated para-Quinone methides undergo efficient transformations. Nice collaboration! #metal-free #photocatalysis #Chemsky
Flavin-Photocatalyzed Benzylic Functionalization, Spirocyclization, and Spiroepoxidation of Phenols @pubs.acs.org pubs.acs.org/doi/10.1021/...

Covalent aptamers: agents with promising therapeutic and diagnostic potential Small molecule- and antibody-based approaches have shown tremendous success in both therapeutic and diagnostic applications. Aptamers, which are engineered nucleic acid ligands for proteins, have not found similar broad applicability, potentially due to their susceptibility to nuclease-mediated degradation and shor

Very insightful review by the group of Alexander Deiters in @rscchembio.rsc.org. They give an overview of the development of covalent #aptamers for protein labeling and inhibition including an overview of the chemistries used. doi.org/10.1039/d5cb...
#ChemSky #ChemBio #NucleicAcids #RNA #DNA

Annulative Skeletal Diversification of Pyrimidines to Expanded Heteroaromatic Space Single-atom skeletal editing has recently emerged as a powerful strategy for the direct diversification of the heterocyclic cores of various compounds. Yet, methods that enable monocycle-to-bicycle tr...

Congratulations to team "Skeletal Annulation" (Phil, Atang, Antonia, Sam, Nicolo, and Takashi) and our collaborators Pfizer
led by @bagphos.bsky.social on the publication of our work in JACS!

doi.org/10.1021/jacs...

#lcsojournalclub | LCSO Lab #LCSOJournalClub 210.1 (highlighted in picture) A light mediated biomimetic synthesis of meroterpenoids involving an electrocyclic reaction, H shift and cycloaddition reported by Jonathan George and c...

Edition 210 of #LCSOJournalClub
www.linkedin.com/feed/update/...

Doctoral program Thesis Distinctions 2025 From left to right Claire Bourmaud c/o Prof Jérémy Luterbacher Weijin Wang c/o Prof Xile Hu Till Marian Schertenleib c/o Prof Wendy Queen Vu Trung Tin Nguyen c/o Prof Jérôme Waser Luc Bondaz c/o Prof ...

LCSO fresh alumni @tinvtnguyen.bsky.social has been awarded a Doctoral Program Thesis Distinction 2025! Congrats!
actu.epfl.ch/news/doctora...

#lcsosynthesisproblem #lcsosynthesisproblem | LCSO Lab Another week, another #LCSOSynthesisProblem! Check out Clément's exercise on the total synthesis of (–)-Maoecrystal V by Baran and co-workers: https://lnkd.in/ePZ5WbGp 📚 Original publication: https:/...

next edition of #LCSOSynthesisProblem
www.linkedin.com/feed/update/...

Bioorthogonal Photocatalytic Protein Labeling and Cross-Linking Enabled by Stabilized Ketyl Radicals Radical reactions offer transformative potential in biological contexts but remain constrained by poor selectivity and off-target reactivity. We address these limitations through visible-light photoca...

Our latest JACS @jacs.acspublications.org paper is out: Atomic-level precision protein labeling achieved in live cells using visible-light catalysis. This technology, based on stabilized ketyl radicals, provides a 'molecular ruler' to map protein dynamics and advance precision medicine.

Miniature Photoenzyme Enables Organelle‐Specific Cellular Control via Deboronative Hydroxylation Genetically encoded miniature photoenzyme miniSOG (12 kDa) enables spatiotemporally controlled bioorthogonal deboronative hydroxylation of 27 diverse organoboronates in live cells via localized super...

Our latest work is out in @angewandtechemie.bsky.social: A miniature photoenzyme (12 kDa) uses visible light to achieve organelle-specific control in living cells via bioorthogonal deboronative hydroxylation. A powerful new platform for light-induced biological modulation.

Opticial Control of Cholesterol, attempting to stay as close to the original as possible. Congratulations to Michael Zott, who defined and spearheaded this study, and to our wonderful collaborator Luca Laraia!

www.organic-chemistry.org/abstracts/li...
A formal (3+2)-cycloaddition of donor-acceptor cyclopropanes and ammonium thiocyanate

Site‐Selective Peptide and Protein Functionalization with Cyclopropenium Cations A cysteine-selective bioconjugation using aromatic cyclopropenium cations is reported. The reaction proceeds rapidly under aqueous conditions, enabling site-selective installation of tetrasubstituted...

Interesting paper by the group of Marcos Suero in @angewandtechemie.bsky.social. They developed a #bioconjugation reaction to thiols using cyclopropenium cations. The resulting product on cysteine can be further modified using a thiol-ene reaction.

onlinelibrary.wiley....
#ChemSky #ChemBio

Synthesis of Spiroindenes via Palladium Catalysis Using Oxabicycles as Acetylene Surrogates We report the palladium-catalyzed synthesis of spiroindenes using oxabicycles as acetylene surrogates. This protocol allows for the synthesis of a diverse library of heterocyclic-tethered spiroindenes...

Nice to see this appear. A big thanks to Clara, Armaan, Xavier, our visitor from Italy Lorenzo, and former group member Greg who has had a long and illustrious career at Merck.

More fun with oxabicycles.

pubs.acs.org/doi/full/10....

#lcsojournalclub | LCSO Lab #LCSOJournalClub 209.1 (highlighted in picture) A preprint at ChemRxiv of Dorian Didier and co-workers from TU Darmstadt on a double carbon insertion on azetines to give pyridines: https://lnkd.in/e-6...

edition 209 of #LCSOJournalClub
www.linkedin.com/feed/update/...

Check out our latest collaborative work with the Baik and Wirth groups in @chemicalscience.rsc.org
pubs.rsc.org/en/Content/A...

#lcsosynthesisproblem #lcsosynthesisproblem | LCSO Lab #LCSOSynthesisProblem is finally back after a long break! This time, Adriana challenged us to the total synthesis of (−)-Illisimonin A by Dai and co-workers. Take a look here: https://lnkd.in/eN4bRjDj...

next edition of #LCSOSynthesisProblem
www.linkedin.com/feed/update/...

The current #1 Bestseller of Helv. Chim. Acta, the Journal of the Swiss Chemical Society, founded 1917, is our paper with the groups of Thomas Poulsen (Aarhus, Denmark) and Oliver Thorn-Seshold (Dresden, Germany): Thank you so much for reading!

onlinelibrary.wiley.com/journal/1522...

We are able to put two different cofactors in one protein scaffold and make them do catalysis together. It is amazing that it actually works. Chemchat chemsky

Evaluating BindCraft for Generative Design of High-Affinity Peptides Discovering high-affinity ligands directly from protein structures remains a key challenge in drug discovery. BindCraft is a structure-guided generative modeling platform able to de novo design miniproteins with a high affinity for a large set of targets. While miniproteins are valuable research tools, short peptides offer substantially greater therapeutic potential. However, given their lack of stabilized tertiary structures, de novo generation of functional peptides is a remarkable challenge. Here, we show that BindCraft is able to generate high affinity peptides, solely based on target structure, with remarkable success rates. For the oncoprotein MDM2, BindCraft generated 70 unique peptides; 15 were synthesized, and 7 showed specific binding with nanomolar affinities. Competition assays confirmed site-specific binding for the intended target site. For another oncology target, WDR5, six out of nine candidates bound the MYC binding WBM site with submicromolar affinity. Bindcraft’s high fidelity structure prediction enabled one shot peptide optimization via rational chemical modification, improving the potency of one WDR5 binder by 6-fold to a KD of 39 nM. BindCraft also generated candidate peptides for targeting PD-1 and PD-L1. However, none of the tested peptides showed detectable binding. Together, these results establish a first evaluation of BindCraft for peptide binder prediction. Despite remaining limitations, this tool shows the potential to rival display technologies in delivering high-affinity ligands for therapeutic development.

Are you interested in peptide-based #DrugDiscovery?

Check out the newest study by the group of @sebastianpomplun.bsky.social of our @led3hub.bsky.social. Being able to predict peptide binders solely based on structure may be closer than you think.

pubs.acs.org/doi/10.1021/...
#ChemSky #ChemBio

Inverse Molecular Design for the Discovery of Organic Energy Transfer Photocatalysts: Bridging Global and Local Chemical Space Exploration The discovery of new organic photocatalysts (PCs) for energy transfer (EnT) catalysis remains a significant challenge, largely due to the vast and underexplored chemical space and the delicate balance...

Preprint alert! 🚨

Excited to share our latest work on generative modelling for accelerating the discovery of organic photocatalysts💡✨

👉Read more: doi.org/10.26434/che...

Congratulations to Leon Schlosser, Nils Rendel, Julius Gemen, @gloriusfrank.bsky.social, and @valencekjell.com

https://doi.org/10.1002/hlca.202400182

ECAB member Emmanuelle Allouche www.siegfried.ch favorite @helvchimacta.bsky.social article is the one of @novartis.bsky.social because it describes the development of a safe and scalable difluoromethylation of 3-hydroxypyridines using continuous-flow technology doi.org/10.1002/hlca...

In our new review in Helv. Chim. Acta, we summarize the first decade of CPDs – cell-penetrating poly(disulfide)s - comprehensively. It was gratifying to see how useful their thiol-mediated uptake has become in practice, also in living animals.

onlinelibrary.wiley.com/doi/10.1002/...

Synthesis of Collinoketones via Biomimetic [6 + 4] Cycloaddition Cycloadditions are among the most powerful reactions for constructing molecular complexity. The archetypal example is the [4 + 2] (Diels–Alder) cycloaddition, which efficiently furnishes cyclohexene d...

[6+4] Cycloadditions! Introducing our first dive into this fascinating subject in a very enjoyable collaboration with Ken Houk and his team. Congrats to Harrison and Tufan!

pubs.acs.org/doi/10.1021/...

A table showing profit margins of major publishers. A snippet of text related to this table is below. 1. The four-fold drain 1.1 Money Currently, academic publishing is dominated by profit-oriented, multinational companies for whom scientific knowledge is a commodity to be sold back to the academic community who created it. The dominant four are Elsevier, Springer Nature, Wiley and Taylor & Francis, which collectively generated over US$7.1 billion in revenue from journal publishing in 2024 alone, and over US$12 billion in profits between 2019 and 2024 (Table 1A). Their profit margins have always been over 30% in the last five years, and for the largest publisher (Elsevier) always over 37%. Against many comparators, across many sectors, scientific publishing is one of the most consistently profitable industries (Table S1). These financial arrangements make a substantial difference to science budgets. In 2024, 46% of Elsevier revenues and 53% of Taylor & Francis revenues were generated in North America, meaning that North American researchers were charged over US$2.27 billion by just two for-profit publishers. The Canadian research councils and the US National Science Foundation were allocated US$9.3 billion in that year.

A figure detailing the drain on researcher time. 1. The four-fold drain 1.2 Time The number of papers published each year is growing faster than the scientific workforce, with the number of papers per researcher almost doubling between 1996 and 2022 (Figure 1A). This reflects the fact that publishers’ commercial desire to publish (sell) more material has aligned well with the competitive prestige culture in which publications help secure jobs, grants, promotions, and awards. To the extent that this growth is driven by a pressure for profit, rather than scholarly imperatives, it distorts the way researchers spend their time. The publishing system depends on unpaid reviewer labour, estimated to be over 130 million unpaid hours annually in 2020 alone (9). Researchers have complained about the demands of peer-review for decades, but the scale of the problem is now worse, with editors reporting widespread difficulties recruiting reviewers. The growth in publications involves not only the authors’ time, but that of academic editors and reviewers who are dealing with so many review demands. Even more seriously, the imperative to produce ever more articles reshapes the nature of scientific inquiry. Evidence across multiple fields shows that more papers result in ‘ossification’, not new ideas (10). It may seem paradoxical that more papers can slow progress until one considers how it affects researchers’ time. While rewards remain tied to volume, prestige, and impact of publications, researchers will be nudged away from riskier, local, interdisciplinary, and long-term work. The result is a treadmill of constant activity with limited progress whereas core scholarly practices – such as reading, reflecting and engaging with others’ contributions – is de-prioritized. What looks like productivity often masks intellectual exhaustion built on a demoralizing, narrowing scientific vision.

A table of profit margins across industries. The section of text related to this table is below: 1. The four-fold drain 1.1 Money Currently, academic publishing is dominated by profit-oriented, multinational companies for whom scientific knowledge is a commodity to be sold back to the academic community who created it. The dominant four are Elsevier, Springer Nature, Wiley and Taylor & Francis, which collectively generated over US$7.1 billion in revenue from journal publishing in 2024 alone, and over US$12 billion in profits between 2019 and 2024 (Table 1A). Their profit margins have always been over 30% in the last five years, and for the largest publisher (Elsevier) always over 37%. Against many comparators, across many sectors, scientific publishing is one of the most consistently profitable industries (Table S1). These financial arrangements make a substantial difference to science budgets. In 2024, 46% of Elsevier revenues and 53% of Taylor & Francis revenues were generated in North America, meaning that North American researchers were charged over US$2.27 billion by just two for-profit publishers. The Canadian research councils and the US National Science Foundation were allocated US$9.3 billion in that year.

The costs of inaction are plain: wasted public funds, lost researcher time, compromised scientific integrity and eroded public trust. Today, the system rewards commercial publishers first, and science second. Without bold action from the funders we risk continuing to pour resources into a system that prioritizes profit over the advancement of scientific knowledge.

We wrote the Strain on scientific publishing to highlight the problems of time & trust. With a fantastic group of co-authors, we present The Drain of Scientific Publishing:

a 🧵 1/n

Drain: arxiv.org/abs/2511.04820
Strain: direct.mit.edu/qss/article/...
Oligopoly: direct.mit.edu/qss/article/...

#ICIQJobs

🚀 Join ICIQ as a Junior Group Leader!

We’re seeking talented, innovative scientists ready to push the frontiers of research.

Apply now 👉🏼 careers.iciq.org/jobs/6745027...

@cerca.cat @bist.eu #SOMM_alliance

#lcsojournalclub | LCSO Lab #LCSOJournalClub 207.1 (Highlighted in picture) a simple selective C3-halogenation of pyridines developed by Ning Jiao, Song Song and co-workers from Peking University in Nat. Synth. https://lnkd.in/e...

Edition 207 of #LCSOJournalClub
www.linkedin.com/feed/update/...

Synthetic Approaches to the New Drugs Approved during 2023 This review is the next installment of an annual series that discusses the synthetic routes to access 28 small molecule drugs that were approved worldwide in 2023. A brief description of each drug’s m...

May I recommend this series:
Published annually by Pfizer Merck Takeda and others
Review of synthetic methods to marketed drugs
Great look at the current state of pharma synthesis