Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor
(2010) In Journal of Medicinal Chemistry 53(14). p.5-5352- Abstract
We report two crystal structures of the PARP domain of human tankyrase-2 (TNKS2). Tankyrases are involved in fundamental cellular processes such as telomere homeostasis and Wnt signaling. The complex of TNKS2 with the potent inhibitor XAV939 provides insights into the molecular basis of the strong interaction and suggests routes for further development of tankyrase inhibitors.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/6a86ab12-b929-414f-9cf9-9a71aaed80fb
- author
- Karlberg, Tobias
LU
; Markova, Natalia
LU
; Johansson, Ida
LU
; Hammarström, Martin
; Schütz, Patrick
; Weigelt, Johan
and Schüler, Herwig
LU
- publishing date
- 2010-07-22
- type
- Contribution to journal
- publication status
- published
- keywords
- Crystallography, X-Ray, Heterocyclic Compounds, 3-Ring/chemistry, Humans, Models, Molecular, Protein Structure, Tertiary, Recombinant Proteins/chemistry, Signal Transduction, Tankyrases/antagonists & inhibitors, Wnt Proteins/physiology
- in
- Journal of Medicinal Chemistry
- volume
- 53
- issue
- 14
- pages
- 4 pages
- publisher
- The American Chemical Society (ACS)
- external identifiers
-
- scopus:77954709179
- pmid:20565110
- ISSN
- 1520-4804
- DOI
- 10.1021/jm100249w
- language
- English
- LU publication?
- no
- id
- 6a86ab12-b929-414f-9cf9-9a71aaed80fb
- date added to LUP
- 2024-11-21 18:00:35
- date last changed
- 2025-06-06 20:34:13
@article{6a86ab12-b929-414f-9cf9-9a71aaed80fb, abstract = {{<p>We report two crystal structures of the PARP domain of human tankyrase-2 (TNKS2). Tankyrases are involved in fundamental cellular processes such as telomere homeostasis and Wnt signaling. The complex of TNKS2 with the potent inhibitor XAV939 provides insights into the molecular basis of the strong interaction and suggests routes for further development of tankyrase inhibitors.</p>}}, author = {{Karlberg, Tobias and Markova, Natalia and Johansson, Ida and Hammarström, Martin and Schütz, Patrick and Weigelt, Johan and Schüler, Herwig}}, issn = {{1520-4804}}, keywords = {{Crystallography, X-Ray; Heterocyclic Compounds, 3-Ring/chemistry; Humans; Models, Molecular; Protein Structure, Tertiary; Recombinant Proteins/chemistry; Signal Transduction; Tankyrases/antagonists & inhibitors; Wnt Proteins/physiology}}, language = {{eng}}, month = {{07}}, number = {{14}}, pages = {{5--5352}}, publisher = {{The American Chemical Society (ACS)}}, series = {{Journal of Medicinal Chemistry}}, title = {{Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor}}, url = {{http://dx.doi.org/10.1021/jm100249w}}, doi = {{10.1021/jm100249w}}, volume = {{53}}, year = {{2010}}, }