Structural highlights
4tz8 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , |
| Related: | 4tyl, 4tz2 |
| Gene: | ATAD2, L16, PRO2000 (HUMAN) |
| Activity: | Adenosinetriphosphatase, with EC number 3.6.1.3 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[ATAD2_HUMAN] May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.[1]
Publication Abstract from PubMed
Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.
Fragment-based screening of the bromodomain of ATAD2.,Harner MJ, Chauder BA, Phan J, Fesik SW J Med Chem. 2014 Oct 14. PMID:25314628[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Zou JX, Revenko AS, Li LB, Gemo AT, Chen HW. ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ERalpha, is required for coregulator occupancy and chromatin modification. Proc Natl Acad Sci U S A. 2007 Nov 13;104(46):18067-72. Epub 2007 Nov 12. PMID:17998543 doi:http://dx.doi.org/10.1073/pnas.0705814104
- ↑ Harner MJ, Chauder BA, Phan J, Fesik SW. Fragment-based screening of the bromodomain of ATAD2. J Med Chem. 2014 Oct 14. PMID:25314628 doi:http://dx.doi.org/10.1021/jm501035j
