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K562 lysate CHKA target engagement with CETSA

ABSTRACT: Studying the target enagement of UNC0638 and UNC737 in K562 cell lysate with CETSA.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Lymphoblast, Blood

DISEASE(S): Chronic Myeloid Leukemia

SUBMITTER: Tuomas Tolvanen

LAB HEAD: Daniel Martinez-Molina

PROVIDER: PXD058045 | Pride | 2025-01-28

REPOSITORIES: Pride

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			Action	DRS
	20220308_EXI281_TMT73_.msf	Msf
	20220308_EXI281_TMT73_.pdResult	Other
	20220308_EXI281_TMT73_01.raw	Raw
	20220308_EXI281_TMT73_02.raw	Raw
	20220308_EXI281_TMT73_03.raw	Raw

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1 - 5 of 38

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

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Intact HepG2 CHKA target engagement with CETSA

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2025-01-28 | PXD057925 | Pride

An oxygen-sensing network of RNA-binding proteins controls glycolysis via hypoxic translatome remodeling.

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MonoMac6 (MM6) cells proteomics LC-MS/MS

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Quantitative proteomic analysis of hypoxia induced primary kidney cells

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2021-01-19 | PXD019678 | Pride

Multilayered proteomics uncovers Notch/PKC targeting to overcome resistance to Notch inhibition in acute lymphoblastic leukemia

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