Top Tweets for #m3258
#M3258 is an orally bioavailable #immunoproteasome subunit #LMP7 (#β5i) inhibitor. Shows strong #antitumor efficacy in multiple #myeloma xenograft models. Leads to significant and prolonged suppression of tumor LMP7 activity. #apoptosis #drugdiscovery. https://t.co/uiGe64gP3k

Markus Klein now disclosing more details about the discovery program leading to immuno-proteasome inhibitor #M3258. A beautiful example how to dial in high specificity in a structure-guided way & not shying away from unusual structural motifs @merckgroup @EuroMedChem #ISMC21

Recently already highlighted in a small-molecules-of-the-month compilation by @DennisWhom, here is now the discovery story for our immunoproteasome inhibitor #M3258: Congrats to the team for an impressive piece of drug discovery. @ACSBioMed @merckgroup https://t.co/yA8KfzdL92

Small Molecules of the Month - May 2021 | https://t.co/oCLDtk1F9R
A mutant PI3Kα degrader in Ph. III, a wild-type CFTR potentiator for COPD, and a surprisingly well-tolerated Ph. III agent from an aerospace compound
#chemtwitter #biotwitter

Noteworthy first disclosure at #AACR19 by my future colleagues @merckgroup about immuneproteasome inhibitor #M3258: quite unusual structural motifs more conservative MedChems might have backed off from. Convincing selectivity, in vivo PK & efficacy data win over prejudices.

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