Literature DB >> 21446847

Crystal structures of 11β-hydroxysteroid dehydrogenase type 1 and their use in drug discovery.

Mark P Thomas1, Barry V L Potter.   

Abstract

Cortisol is synthesized by 11β-hydroxysteroid dehydrogenase type 1, inhibitors of which may treat disease associated with excessive cortisol levels. The crystal structures of 11β-hydroxysteroid dehydrogenase type 1 that have been released may aid drug discovery. The crystal structures have been analyzed in terms of the interactions between the protein and the ligands. Despite a variety of structurally different inhibitors the crystal structures of the proteins are quite similar. However, the differences are significant for drug discovery. The crystal structures can be of use in drug discovery, but care needs to be taken when selecting structures for use in virtual screening and ligand docking.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21446847      PMCID: PMC4037982          DOI: 10.4155/fmc.10.282

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  56 in total

1.  Novel adipose tissue-mediated resistance to diet-induced visceral obesity in 11 beta-hydroxysteroid dehydrogenase type 1-deficient mice.

Authors:  Nicholas M Morton; Janice M Paterson; Hiroaki Masuzaki; Megan C Holmes; Bart Staels; Catherine Fievet; Brian R Walker; Jeffrey S Flier; John J Mullins; Jonathan R Seckl
Journal:  Diabetes       Date:  2004-04       Impact factor: 9.461

2.  Cortisol--cause and cure for metabolic syndrome?

Authors:  B R Walker
Journal:  Diabet Med       Date:  2006-12       Impact factor: 4.359

3.  Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.

Authors:  Jyoti R Patel; Qi Shuai; Jurgen Dinges; Marty Winn; Marina Pliushchev; Steven Fung; Katina Monzon; William Chiou; Jiahong Wang; Liping Pan; Seble Wagaw; Kenneth Engstrom; Francis A Kerdesky; Kenton Longenecker; Russell Judge; Wenying Qin; Hovis M Imade; Deanne Stolarik; David W A Beno; Michael Brune; Linda E Chovan; Hing L Sham; Peer Jacobson; J T Link
Journal:  Bioorg Med Chem Lett       Date:  2006-10-28       Impact factor: 2.823

4.  Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons.

Authors:  Malin Hult; Naeem Shafqat; Björn Elleby; Doreen Mitschke; Stefan Svensson; Margareta Forsgren; Tjeerd Barf; Jerk Vallgårda; Lars Abrahmsen; Udo Oppermann
Journal:  Mol Cell Endocrinol       Date:  2006-01-20       Impact factor: 4.102

5.  Comparison of super-secondary structures in proteins.

Authors:  S T Rao; M G Rossmann
Journal:  J Mol Biol       Date:  1973-05-15       Impact factor: 5.469

6.  Adipocyte-specific glucocorticoid inactivation protects against diet-induced obesity.

Authors:  Erin E Kershaw; Nicholas M Morton; Harveen Dhillon; Lynne Ramage; Jonathan R Seckl; Jeffrey S Flier
Journal:  Diabetes       Date:  2005-04       Impact factor: 9.461

Review 7.  Function, gene organization and protein structures of 11beta-hydroxysteroid dehydrogenase isoforms.

Authors:  U C Oppermann; B Persson; H Jörnvall
Journal:  Eur J Biochem       Date:  1997-10-15

8.  Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.

Authors:  Yosup Rew; Dustin L McMinn; Zhulun Wang; Xiao He; Randall W Hungate; Juan C Jaen; Athena Sudom; Daqing Sun; Hua Tu; Stefania Ursu; Elisia Villemure; Nigel P C Walker; Xuelei Yan; Qiuping Ye; Jay P Powers
Journal:  Bioorg Med Chem Lett       Date:  2009-01-23       Impact factor: 2.823

9.  2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.

Authors:  Lars Johansson; Christopher Fotsch; Michael D Bartberger; Victor M Castro; Michelle Chen; Maurice Emery; Sonja Gustafsson; Clarence Hale; Dean Hickman; Evert Homan; Steven R Jordan; Renee Komorowski; Aiwen Li; Kenneth McRae; George Moniz; Guy Matsumoto; Carlos Orihuela; Gunnar Palm; Murielle Veniant; Minghan Wang; Meredith Williams; Jiandong Zhang
Journal:  J Med Chem       Date:  2008-04-18       Impact factor: 7.446

Review 10.  Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target.

Authors:  Malgorzata Wamil; Jonathan R Seckl
Journal:  Drug Discov Today       Date:  2007-06-27       Impact factor: 7.851

View more
  9 in total

Review 1.  Virtual screening applications in short-chain dehydrogenase/reductase research.

Authors:  Katharina R Beck; Teresa Kaserer; Daniela Schuster; Alex Odermatt
Journal:  J Steroid Biochem Mol Biol       Date:  2017-03-09       Impact factor: 4.292

2.  Impaired oxidoreduction by 11β-hydroxysteroid dehydrogenase 1 results in the accumulation of 7-oxolithocholic acid.

Authors:  Carlos A Penno; Stuart A Morgan; Anna Vuorinen; Daniela Schuster; Gareth G Lavery; Alex Odermatt
Journal:  J Lipid Res       Date:  2013-08-09       Impact factor: 5.922

3.  Mechanistic Insight on the Mode of Action of Colletoic Acid.

Authors:  Taotao Ling; Darcie J Miller; Walter H Lang; Elizabeth Griffith; Adaris Rodriguez-Cortes; Ikbale El Ayachi; Gustavo Palacios; Jaeki Min; Gustavo Miranda-Carboni; Richard E Lee; Fatima Rivas
Journal:  J Med Chem       Date:  2019-07-24       Impact factor: 7.446

Review 4.  11β-hydroxysteroid dehydrogenases: intracellular gate-keepers of tissue glucocorticoid action.

Authors:  Karen Chapman; Megan Holmes; Jonathan Seckl
Journal:  Physiol Rev       Date:  2013-07       Impact factor: 37.312

5.  Discovery of adamantyl heterocyclic ketones as potent 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Nigel Vicker; Mark P Thomas; Fabienne Pradaux-Caggiano; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-05-23       Impact factor: 3.466

6.  Adamantyl ethanone pyridyl derivatives: potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1.

Authors:  Xiangdong Su; Fabienne Pradaux-Caggiano; Nigel Vicker; Mark P Thomas; Heather Halem; Michael D Culler; Barry V L Potter
Journal:  ChemMedChem       Date:  2011-06-28       Impact factor: 3.466

7.  16-nor Limonoids from Harrisonia perforata as promising selective 11β-HSD1 inhibitors.

Authors:  Xiao-Hui Yan; Ping Yi; Pei Cao; Shi-Ying Yang; Xin Fang; Yu Zhang; Ying Leng; Ying-Tong Di; Yang Lv; Xiao-Jiang Hao
Journal:  Sci Rep       Date:  2016-11-11       Impact factor: 4.379

8.  Adamantyl carboxamides and acetamides as potent human 11β-hydroxysteroid dehydrogenase type 1 inhibitors.

Authors:  Xiangdong Su; Heather A Halem; Mark P Thomas; Cecile Moutrille; Michael D Culler; Nigel Vicker; Barry V L Potter
Journal:  Bioorg Med Chem       Date:  2012-09-12       Impact factor: 3.641

Review 9.  Pharmacophore Models and Pharmacophore-Based Virtual Screening: Concepts and Applications Exemplified on Hydroxysteroid Dehydrogenases.

Authors:  Teresa Kaserer; Katharina R Beck; Muhammad Akram; Alex Odermatt; Daniela Schuster
Journal:  Molecules       Date:  2015-12-19       Impact factor: 4.411

  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.