Dataset Information

WDR5 protein interactions at the WIN-site

ABSTRACT: The WIN site of WDR5 is a druggable pocket that impairs WDR5 protein function and carries therapeutic potential for treating cancer. This study evaluates the protein interactions affected by small molecule blockade of this surface on WDR5. Inhibited and uninhibited WDR5-containing complexes from HEK293 cells were quantitatively compared by SILAC-based proteomics. Of the high confidence proteins affected by this inhibition, one protein, PDPK1, was investigated further by mass spectrometry for identification of post translational modifications that could influence binding to WDR5.

INSTRUMENT(S): Q Exactive Plus

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Kidney Cell

SUBMITTER: Kristie Lindsey Rose

LAB HEAD: Kristie Lindsey Rose

PROVIDER: PXD019209 | Pride | 2021-01-25

REPOSITORIES: Pride

ACCESS DATA

Dataset's files

Source:

			Action	DRS
	5206PDPK1AspNdigestPeptideReport.xlsx	Xlsx
	5206PDPK1trypsindigestPeptideReport.xlsx	Xlsx
	ns_5206_AG_053118_PDPK1_AspN.raw	Raw
	ns_5206_AG_053118_PDPK1_trypsin.raw	Raw
	peptides_5206_2.xlsx	Xlsx

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Publications

Impact of WIN site inhibitor on the WDR5 interactome.

Guarnaccia Alissa D AD Rose Kristie L KL Wang Jing J Zhao Bin B Popay Tessa M TM Wang Christina E CE Guerrazzi Kiana K Hill Salisha S Woodley Chase M CM Hansen Tyler J TJ Lorey Shelly L SL Shaw J Grace JG Payne William G WG Weissmiller April M AM Olejniczak Edward T ET Fesik Stephen W SW Liu Qi Q Tansey William P WP

Cell reports 20210101 3

The chromatin-associated protein WDR5 is a promising pharmacological target in cancer, with most drug discovery efforts directed against an arginine-binding cavity in WDR5 called the WIN site. Despite a clear expectation that WIN site inhibitors will alter the repertoire of WDR5 interaction partners, their impact on the WDR5 interactome remains unknown. Here, we use quantitative proteomics to delineate how the WDR5 interactome is changed by WIN site inhibition. We show that the WIN site inhibito ...[more]

PMID: 33472061

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