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Martin Schwalm

@martinschwalm.bsky.social
46 followers 29 following 6 posts

A biochemist with an interest in science, music and the restoration of classic cars. Founder of tracerDB.org

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Reposted by Martin Schwalm
Zuzanna Kozicka @zkozicka.bsky.social · 18/03/2025
Very excited for our next seminar this Thursday, March 20th: Martin Schwalm (@thesgc.bsky.social, formerly Knapp lab) will share insights on UPS inhibitors and Dean Clift (TRIMTECH Tx) will discuss hijacking TRIM21 for protein #degradation! 👉Join us at 12 PM EST/ 5 pm CET (‼️ US/EU time mismatch ‼️)
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Reposted by Martin Schwalm
Keith Hornberger @krhornberger.bsky.social · 21/01/2025
Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation
pubs.acs.org
Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation
Small molecule degraders such as PROteolysis TArgeting Chimeras (PROTACs) and molecular glues are new modalities for drug development and important tools for target validation. When appropriately opti...
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Martin Schwalm @martinschwalm.bsky.social · 17/01/2025
We got the 3. journal cover. This time depicting the UPS inhibitors interfering with the different steps of the cascade in @acs.org Chemical Biology. pubs.acs.org/toc/acbcct/c...
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Reposted by Martin Schwalm
Joachim Goedhart @joachimgoedhart.bsky.social · 06/01/2025
A photoswitchable HaloTag for spatiotemporal control of fluorescence in living cells by @clairedeo.bsky.social and team: www.biorxiv.org/content/10.1...
General principle of photoswitchable HaloTag (psHaloTag) and open-closed equilibrium of JF635-HaloTag ligand (HTL).
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Martin Schwalm @martinschwalm.bsky.social · 06/01/2025
Interesting review on TPD which still describes ATTECs as LC3 binding molecules. The paper was revised a month after we published our results that there is no binding to LC3... www.sciencedirect.com/science/arti... See our paper here: www.nature.com/articles/s41...
sciencedirect.com
Recent advances in developing targeted protein degraders
Targeted protein degradation (TPD) represents a promising therapeutic approach, encompassing several innovative strategies, including but not limited …
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Reposted by Martin Schwalm
Geordi Frere @geordifrere.bsky.social · 04/01/2025
A rigorous study of UPS tool compounds for #degrader evaluation is published by Stefan Knapp @thesgc.bsky.social in ACS Chemical Biology! They determine the optimal doses of UPS pathway inhibitors that rescue degradation without displaying off-target activity and toxicity. dx.doi.org/10.1021/acsc...
dx.doi.org
Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation
Small molecule degraders such as PROteolysis TArgeting Chimeras (PROTACs) and molecular glues are new modalities for drug development and important tools for target validation. When appropriately opti...
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Martin Schwalm @martinschwalm.bsky.social · 04/01/2025
Interested in #TPD? This might be for you. What concentrations of UPS inhibitors are safe to use to prove your proteasome dependent degradation mechanism? #PROTAC #TPD #degradation #Science #drugdiscovery pubs.acs.org/doi/10.1021/...
pubs.acs.org
Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation
Small molecule degraders such as PROteolysis TArgeting Chimeras (PROTACs) and molecular glues are new modalities for drug development and important tools for target validation. When appropriately opti...
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Martin Schwalm @martinschwalm.bsky.social · 18/12/2024
Great to contribute to this study. We report on a target-hopping approach for the discovery of novel MLK3 inhibitors pubs.acs.org/doi/10.1021/... #KinaseInhibitors #DrugDiscovery #TargetedTherapies
pubs.acs.org
Design, Synthesis, and Biochemical Evaluation of Novel MLK3 Inhibitors: A Target Hopping Example
The human kinome has tremendous medical potential. In the past decade, mixed-lineage protein kinase 3 (MLK3) has emerged as an interesting and druggable target in oncogenic signaling. The important ro...
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Martin Schwalm @martinschwalm.bsky.social · 06/12/2024
Quality control is often overlooked in novel pathways, and we demonstrate this using ATTECs (Autophagy Tethering Compounds) as a case study. Our new study highlights what’s frequently missing in research! #ProteinDegradation Just out in @naturecomms.bsky.social www.nature.com/articles/s41...
nature.com
Critical assessment of LC3/GABARAP ligands used for degrader development and ligandability of LC3/GABARAP binding pockets - Nature Communications
Autophagosome tethering compounds (ATTECs) are small molecule degraders hijacking the autophagy system. Here, the authors show that current ATTEC ligands did not bind to their designated targets but e...
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Reposted by Martin Schwalm
Ingo Hartung @hartungingo.bsky.social · 25/11/2024
There are no shortcuts in drug discovery. And it takes incredible efforts to make sense of what you can find in the scientific literature. This is an excellent piece of work to quality check what has been claimed as a new avenue in targeted protein degradation (TPD). www.nature.com/articles/s41...
nature.com
Critical assessment of LC3/GABARAP ligands used for degrader development and ligandability of LC3/GABARAP binding pockets - Nature Communications
Autophagosome tethering compounds (ATTECs) are small molecule degraders hijacking the autophagy system. Here, the authors show that current ATTEC ligands did not bind to their designated targets but e...
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Reposted by Martin Schwalm
Derek Lowe @dereklowe.bsky.social · 03/12/2024
That awkward moment when someone publishes a paper saying that they can’t find any evidence that your compounds bind to what your own series of papers say that they bind to. . .
science.org
Do They Even Bind?
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