Dataset Information

TAK285 induced degradation – selectivity profiling in NALM-6 cells

ABSTRACT: The hit compound TAK285 was subjected to full proteome profiling by TMTpro 6-plex to assess its degradation selectivity in NALM-6 cells. TAK285 induced the degradation of the kinase BLK. The compound was further mechanistically dissected as reported with orthogonal assays such as FACS-based CRISPR/Cas9 screens and BioID.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Fabian Frommelt

LAB HEAD: Georg E. Winter

PROVIDER: PXD059599 | Pride | 2025-09-04

REPOSITORIES: Pride

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Dataset's files

Source:

			Action	DRS
	CC_GW_200-M1218-.mzML	Mzml
	CC_GW_200-M1218-A01-Fraction1-P13630-1.raw	Raw
	CC_GW_200-M1218-A02-Fraction2-P13631-1.raw	Raw
	CC_GW_200-M1218-A03-Fraction3-P13632-1.raw	Raw
	CC_GW_200-M1218-A04-Fraction4-P13633-1.raw	Raw

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Publications

Inhibitors supercharge kinase turnover through native proteolytic circuits.

Scholes Natalie S NS Bertoni Martino M Comajuncosa-Creus Arnau A Kladnik Katharina K Guo Xuefei X Frommelt Fabian F Hinterndorfer Matthias M Razumkov Hlib H Prokofeva Polina P Schwalm Martin P MP Born Florian F Roehm Sandra S Imrichova Hana H Santini Brianda L BL Barone Eleonora E Schätz Caroline C Muñoz I Ordoño Miquel M Lechner Severin S Rukavina Andrea A Serrano Iciar I Abele Miriam M Koren Anna A Kubicek Stefan S Knapp Stefan S Gray Nathanael S NS Superti-Furga Giulio G Kuster Bernhard B Shi Yigong Y Aloy Patrick P Winter Georg E GE

Nature 20251126 8098

Targeted protein degradation is a pharmacological strategy that relies on small molecules such as proteolysis-targeting chimeras (PROTACs) or molecular glues, which induce proximity between a target protein and an E3 ubiquitin ligase to prompt target ubiquitination and proteasomal degradation<sup>1</sup>. Sporadic reports indicated that ligands designed to inhibit a target can also induce its destabilization<sup>2-4</sup>. Among others, this has repeatedly been observed for kinase inhibitors<sup ...[more]

PMID: 41299171

Dataset Information

TAK285 induced degradation – selectivity profiling in NALM-6 cells

Dataset's files

Publications

Inhibitors supercharge kinase turnover through native proteolytic circuits.

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