Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226.
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| Title: | Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226. |
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| Authors: | Feng Wang1, Xiao-Qin Liu1, He Li1, Kai-Ni Liang1, Miner, Jeffrey N.2, Mei Hong2, Kallel, E. Adam2, van Oeveren, Arjan2, Lin Zhi2, Tao Jiang1 x-ray@sun5.ibp.ac.cn |
| Source: | Acta Crystallographica: Section F (Wiley-Blackwell). Nov2006, Vol. 62 Issue 11, p1067-1071. 5p. 5 Diagrams, 1 Chart. |
| Subjects: | Androgens, Steroid hormones, Ligands (Chemistry), Antiandrogens, Phenotypes |
| Abstract: | The androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. As the androgens play a dominant role in male sexual development and function, steroidal androgen agonists have been used clinically for some years. However, there is a risk of potential side effects and most steroidal androgens cannot be dosed orally, which limits the use of these substances. 1,2-Dihydro-6- N, N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quinolinone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective AR modulator. The crystal structure of the complex of LGD2226 with the androgen receptor ligand-binding domain (AR LBD) at 2.1 Å was solved and compared with the structure of the AR LBD–R1881 complex. It is hoped that this will aid in further explaining the selectivity of LGD2226 observed in in vitro and in vivo assays and in developing more selective and effective therapeutic agents. [ABSTRACT FROM AUTHOR] |
| Copyright of Acta Crystallographica: Section F (Wiley-Blackwell) is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
| Database: | Engineering Source |
| FullText | Links: – Type: pdflink Text: Availability: 0 |
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| Header | DbId: egs DbLabel: Engineering Source An: 22930918 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Feng+Wang%22">Feng Wang</searchLink><relatesTo>1</relatesTo><br /><searchLink fieldCode="AR" term="%22Xiao-Qin+Liu%22">Xiao-Qin Liu</searchLink><relatesTo>1</relatesTo><br /><searchLink fieldCode="AR" term="%22He+Li%22">He Li</searchLink><relatesTo>1</relatesTo><br /><searchLink fieldCode="AR" term="%22Kai-Ni+Liang%22">Kai-Ni Liang</searchLink><relatesTo>1</relatesTo><br /><searchLink fieldCode="AR" term="%22Miner%2C+Jeffrey+N%2E%22">Miner, Jeffrey N.</searchLink><relatesTo>2</relatesTo><br /><searchLink fieldCode="AR" term="%22Mei+Hong%22">Mei Hong</searchLink><relatesTo>2</relatesTo><br /><searchLink fieldCode="AR" term="%22Kallel%2C+E%2E+Adam%22">Kallel, E. Adam</searchLink><relatesTo>2</relatesTo><br /><searchLink fieldCode="AR" term="%22van+Oeveren%2C+Arjan%22">van Oeveren, Arjan</searchLink><relatesTo>2</relatesTo><br /><searchLink fieldCode="AR" term="%22Lin+Zhi%22">Lin Zhi</searchLink><relatesTo>2</relatesTo><br /><searchLink fieldCode="AR" term="%22Tao+Jiang%22">Tao Jiang</searchLink><relatesTo>1</relatesTo><i> x-ray@sun5.ibp.ac.cn</i> – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22Acta+Crystallographica%3A+Section+F+%28Wiley-Blackwell%29%22">Acta Crystallographica: Section F (Wiley-Blackwell)</searchLink>. Nov2006, Vol. 62 Issue 11, p1067-1071. 5p. 5 Diagrams, 1 Chart. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Androgens%22">Androgens</searchLink><br /><searchLink fieldCode="DE" term="%22Steroid+hormones%22">Steroid hormones</searchLink><br /><searchLink fieldCode="DE" term="%22Ligands+%28Chemistry%29%22">Ligands (Chemistry)</searchLink><br /><searchLink fieldCode="DE" term="%22Antiandrogens%22">Antiandrogens</searchLink><br /><searchLink fieldCode="DE" term="%22Phenotypes%22">Phenotypes</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: The androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. As the androgens play a dominant role in male sexual development and function, steroidal androgen agonists have been used clinically for some years. However, there is a risk of potential side effects and most steroidal androgens cannot be dosed orally, which limits the use of these substances. 1,2-Dihydro-6- N, N-bis(2,2,2-trifluoroethyl)amino-4-trifluoromethyl-2-quinolinone (LGD2226) is a synthetic nonsteroidal ligand and a novel selective AR modulator. The crystal structure of the complex of LGD2226 with the androgen receptor ligand-binding domain (AR LBD) at 2.1 Å was solved and compared with the structure of the AR LBD–R1881 complex. It is hoped that this will aid in further explaining the selectivity of LGD2226 observed in in vitro and in vivo assays and in developing more selective and effective therapeutic agents. [ABSTRACT FROM AUTHOR] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of Acta Crystallographica: Section F (Wiley-Blackwell) is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1107/S1744309106039340 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 5 StartPage: 1067 Subjects: – SubjectFull: Androgens Type: general – SubjectFull: Steroid hormones Type: general – SubjectFull: Ligands (Chemistry) Type: general – SubjectFull: Antiandrogens Type: general – SubjectFull: Phenotypes Type: general Titles: – TitleFull: Structure of the ligand-binding domain (LBD) of human androgen receptor in complex with a selective modulator LGD2226. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Feng Wang – PersonEntity: Name: NameFull: Xiao-Qin Liu – PersonEntity: Name: NameFull: He Li – PersonEntity: Name: NameFull: Kai-Ni Liang – PersonEntity: Name: NameFull: Miner, Jeffrey N. – PersonEntity: Name: NameFull: Mei Hong – PersonEntity: Name: NameFull: Kallel, E. Adam – PersonEntity: Name: NameFull: van Oeveren, Arjan – PersonEntity: Name: NameFull: Lin Zhi – PersonEntity: Name: NameFull: Tao Jiang IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 11 Text: Nov2006 Type: published Y: 2006 Identifiers: – Type: issn-print Value: 17443091 Numbering: – Type: volume Value: 62 – Type: issue Value: 11 Titles: – TitleFull: Acta Crystallographica: Section F (Wiley-Blackwell) Type: main |
| ResultId | 1 |
