Dataset Information

Affinity-based chemoproteomic profiling of UNC0638 and UNC0737 in MCF7 and PBMC lysates identifies CHKA as a shared off-target.

ABSTRACT: To identify the molecular target(s) and elucidate the mechanism of action of UNC0638 and UNC0737, affinity-based chemoproteomics was performed. UNC0965, a biotinylated analogue of UNC0638, was immobilised on streptavidin-coated sepharose beads to enrich binding proteins from whole MCF7 or PBMC cell lysates. UNC0636 or UNC0737 were added as competitors in control experiments to identify specific binders.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Blood Cell, Breast, Breast Adenocarcinoma Cell Line, Blood

SUBMITTER: Ludwig Bauer

LAB HEAD: Kilian Huber

PROVIDER: PXD056865 | Pride | 2025-01-27

REPOSITORIES: Pride

ACCESS DATA

Dataset's files

Source:

			Action	DRS
	QE772_MSQ1022_20170428_JAW_009_PMBC_61_UNC0638_1.raw	Raw
	QE772_MSQ1022_20170428_JAW_009_PMBC_62_UNC0638_2.raw	Raw
	QE772_MSQ1022_20170428_JAW_009_PMBC_71_UNC0737_1.raw	Raw
	QE772_MSQ1022_20170428_JAW_009_PMBC_72_UNC0737_2.raw	Raw
	QE772_MSQ1022_20170428_JAW_009_PMBC_D1_DMSO_1.raw	Raw

Items per page:

1 - 5 of 16

Publications

Phenomics-Based Discovery of Novel Orthosteric Choline Kinase Inhibitors.

Bauer Ludwig G LG Ward Jennifer A JA Díaz-Sáez Laura L Sundström Yvonne Y Tolvanen Tuomas T Alarcón Barrera Juan Carlos JC Kostidis Sarantos S Rogers Catherine M CM Panagakou Ioanna I Singh Usha U Rothweiler Elisabeth M EM Gonzalez Orta Alejandro A Kaniskan H Ümit HÜ Hu Jianping J Jin Jian J Sievers Sonja S Waldmann Herbert H Giera Martin M Sundström Michael M Berg Louise L Huber Kilian V M KVM

Angewandte Chemie (International ed. in English) 20250113 7

Choline kinase alpha (CHKA) is a central mediator of cell metabolism linked to cancer and immune regulation. Cellular and clinical evaluation of CHKA has been hampered by challenges in the development of drug-like choline kinase inhibitors. Here, we identify CHKA as an unexpected off-target of histone methyltransferase inhibitors using an integrated phenomic approach. We confirm CHKA as a direct protein target of the aminoquinazolines UNC0638 and UNC0737 using a combination of chemoproteomic, bi ...[more]

PMID: 39740997

Dataset Information

Affinity-based chemoproteomic profiling of UNC0638 and UNC0737 in MCF7 and PBMC lysates identifies CHKA as a shared off-target.

Dataset's files

Publications

Phenomics-Based Discovery of Novel Orthosteric Choline Kinase Inhibitors.

Similar Datasets

OmicsDI is part of the ELIXIR infrastructure

Tweets

Similar Datasets

Characterization of technical variation in ChIP-on-chip studies
2008-10-31 | E-GEOD-8448 | biostudies-arrayexpress

Small-molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling
2018-07-25 | PXD009724 | Pride

A Chemical Biology Toolbox to Study Protein Methyltransferases and Epigenetic Signaling
2018-12-19 | PXD009028 | Pride

Genome-wide Definition of the SigF Regulon in Mycobacterium tuberculosis (ChIP-chip)
2012-01-20 | E-GEOD-34919 | biostudies-arrayexpress

RNA-seq of SARS-CoV-2-infected human primary hepatocyte-derived spheroids upon interferon a2 and baricitinib treatment
2020-11-18 | E-MTAB-9711 | biostudies-arrayexpress

Skeletal muscle cell protein dysregulation highlights the pathogenesis mechanism of myopathy-associated p97/VCP R155H mutations
2023-07-23 | PXD044004 | Pride

Genome-wide Definition of the SigF Regulon in Mycobacterium tuberculosis
2012-01-20 | E-GEOD-35080 | biostudies-arrayexpress

ATAC-seq in the differentiation system ESC to NPC upon O-GlcNAc removal
2024-08-31 | E-MTAB-14350 | biostudies-arrayexpress

Gene expression patterns of chemoresistant and chemosensitive serous epithelial ovarian tumors with possible predictive value in response to initial chemotherapy
2011-07-23 | E-GEOD-28739 | biostudies-arrayexpress

Plant homeodomain targeting cyclic peptides allosterically modulate KDM7 histone demethylase activity
2023-07-20 | PXD027151 | Pride