- 3D-structure of human estrogenic 17beta-HSD1: binding with various steroidsS X Lin
The Medical Research Council Group in Molecular Endocrinology, CHUL Research Center and Laval University, Sainte Foy, QC, Canada
J Steroid Biochem Mol Biol 69:425-9. 1999..These results give evidence for the structural basis of steroid recognition by 17beta-HSD1 and throw light on the design of new inhibitors for this pivotal steroid enzyme...
- Interplay between Catalysts and Substrates for Activity of Class Ib Aminoacyl-tRNA Synthetases and Implications for PharmacologyPreyesh Stephen
Laboratory of Molecular Endocrinology, Research Center CHU and Laval University, Quebec, Canada
Curr Top Med Chem 16:616-33. 2016..Strategies to inhibit class Ib aaRS:tRNA aminoacylation systems, their dysfunction leading to human diseases, and the implications for pharmacology are outlined. ..
- Structure analysis of a new psychrophilic marine proteaseSi Cai Zhang
Laboratory of Structural Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes of Biological Sciences, Chinese Academy of Sciences, Shanghai, China
PLoS ONE 6:e26939. 2011..The structural analysis of this new marine protease provides new information for the study of psychrophilic proteases and is helpful for elucidating the structure-environment adaptation of these enzymes...
- Structural basis of the multispecificity demonstrated by 17beta-hydroxysteroid dehydrogenase types 1 and 5S X Lin
Molecular Endocrinology Research Center at Laval University Hospital Research Center CHUL, CHUQ, Laval University, Que, Canada G1V 4G2
Mol Cell Endocrinol 248:38-46. 2006..The multi-specificity contributes significantly to steroid metabolism in peripheral tissues, due to the high levels of 17beta-HSD5 mRNA in both breast and prostate tissues...
- Magnet used for protein crystallization: novel attempts to improve the crystal qualityS X Lin
Molecular Endocrinology and Oncology Laboratory, Laval University Medical Center, 2705 Boulevard Laurier, Quebec, Quebec, G1V 4G2, Canada
Biochem Biophys Res Commun 275:274-8. 2000..The density difference between the crystal and solution becomes less significant, and the sedimentation speed of the crystals is also reduced in the presence of the magnetization force...
- Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenaseWei Qiu
Canadian Institutes of Health Research Group in Molecular Endocrinology, Laval University Medical Center, Centre Hospitalier de Universités de Québec and Laval University, Quebec G1V 4G2, Canada
J Biol Chem 282:8368-79. 2007....
- Crystal structures of the multispecific 17beta-hydroxysteroid dehydrogenase type 5: critical androgen regulation in human peripheral tissuesWei Qiu
Oncology and Molecular Endocrinology Research Center, Centre Hospitalier de l Université Laval Medical Center CHUL and Laval University, Sainte Foy, Quebec, Canada G1V 4G2
Mol Endocrinol 18:1798-807. 2004..These structures have provided a dynamic view of the enzyme reaction converting androstenedione to testosterone as well as valuable information for the development of potent enzyme inhibitors...
- Identifying androsterone (ADT) as a cognate substrate for human dehydroepiandrosterone sulfotransferase (DHEA-ST) important for steroid homeostasis: structure of the enzyme-ADT complexHo Jin Chang
Canadian Institutes of Health Research Group in Oncology and Molecular Endocrinology Laboratory, CHUL Research Center and Laval University, Sainte Foy, Quebec G1V 4G2, Canada
J Biol Chem 279:2689-96. 2004..Our results identify that this human enzyme is an ADT sulfotransferase as well as a DHEA sulfotransferase, implying an important role in steroid homeostasis for the adrenals and liver...
- A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinityWei Qiu
Oncology and Molecular Endocrinology Research Center, Laval University Medical Center CHUL and Laval University, Quebec, G1V 4G2, Canada
FASEB J 16:1829-31. 2002..These results confirm our initial strategy of combining studies of structural biology and enzyme mechanism in the inhibitor design, which may be applied to other steroidogenic enzymes involved in human diseases...
- How estrogen-specific proteins discriminate estrogens from androgens: a common steroid binding site architectureVirginie Nahoum
Oncology and Molecular Endocrinology Research Center, CHUL Research Center and Laval University, Quebec, Quebec G1V 4G2, Canada
FASEB J 17:1334-6. 2003..As these different estrogen-specific proteins are not related in overall sequence, the inference is that the steroid binding site in these proteins has originated by convergent evolution...
- Estrone and estradiol C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenaseDonald Poirier
Oncology and Molecular Endocrinology Research Center, CHUQ Pavillon CHUL and University Laval, 2705 Laurier Boulevard, Que, Canada G1V 4G2
Mol Cell Endocrinol 248:236-8. 2006..With an IC50 of 0.8 microM, the 16beta-benzyl-E2 (3a) is the best inhibitor in this series...
- Pseudo-symmetry of C19 steroids, alternative binding orientations, and multispecificity in human estrogenic 17beta-hydroxysteroid dehydrogenaseAnne Gangloff
Oncology and Molecular Endocrinology Research Center, CHUL Research Center and Laval University, Quebec, Canada, G1V 4G2
FASEB J 17:274-6. 2003....
- Crystal structure of chloramphenicol acetyltransferase B2 encoded by the multiresistance transposon Tn2424Wei Qiu
Oncology and Molecular Endocrinology Research Centre and Université Laval, Quebec, Canada
Proteins 57:858-61. 2004
- Mapping of steroids binding to 17 beta-hydroxysteroid dehydrogenase type 1 using Monte Carlo energy minimization reveals alternative binding modesJonathan Blanchet
CHUL Research Centre, Laval University, Quebec City, Quebec, Canada
Biochemistry 44:7218-27. 2005..The methodology can be used for mapping ligand-receptor interactions in various systems, for example, in ion channels and G-protein-coupled receptors that bind elongated ligands in confined space between transmembrane helices...
- Crystal structure of human dehydroepiandrosterone sulphotransferase in complex with substratePeter H Rehse
Oncology and Molecular Endocrinology Research Center, Laval University Medical Center CHUL CHUQ, 2705 Boul Laurier, Quebec City, Quebec, G1V 4G2, Canada
Biochem J 364:165-71. 2002..The results presented here describe details of substrate binding to DHEA-ST and the potential relationship to substrate inhibition...
- Purification, crystallization and preliminary X-ray diffraction results of human 17beta-hydroxysteroid dehydrogenase type 5Ming Zhou
Molecular Endocrinology Laboratory, CHUL Research Center, Laval University, Canada
Acta Crystallogr D Biol Crystallogr 58:1048-50. 2002..41, b = 77.16, c = 48.67 A, beta = 116.32 degrees. Form II crystals obtained at pH 6.5 diffracted to 2.0 A and belonged to space group P6(3), with unit-cell parameters a = b = 110.58, c = 56.89 A...
- Purification, reconstitution, and steady-state kinetics of the trans-membrane 17 beta-hydroxysteroid dehydrogenase 2Ming Liang Lu
Oncology and Molecular Endocrinology Research Center, Laval University Medical Center CHUQ and Laval University, Quebec, Quebec G1V 4G2, Canada
J Biol Chem 277:22123-30. 2002..The kinetic constants using estradiol, testosterone, dihydrotestosterone, and 20 alpha-dihydroprogesterone as substrates were also determined...
- Structure function analysis of west nile virus RNA dependent RNA polymerase: molecular model and implications for drug designArezki Azzi
Oncology and Molecular Endocrinology Research Center, Laval University Medical Center CHUQ, 2705 Boul Laurier, Quebec, Canada
Med Chem 3:455-9. 2007..These results provide a preliminary basis for the development of anti-WNV agents based on RNA dependant RNA polymerase inhibition...
- Endocrine and intracrine sources of androgens in women: inhibition of breast cancer and other roles of androgens and their precursor dehydroepiandrosteroneFernand Labrie
Molecular Endocrinology and Oncology Research Center, Laval University Medical Center Centre Hospitalier de l Université Laval and Laval University, Quebec City, Quebec G1V 4G2, Canada
Endocr Rev 24:152-82. 2003....
- Analysis and statistics of crystallisation success increase by composition modification of protein and precipitant mixing ratioChen Yan Zhang
Laboratory of Molecular Endocrinology and Oncology, Centre Hospitalier de Université Laval Research Center CHUL, CHUQ and Laval University, Quebec, G1V 4G2, Canada
Protein Pept Lett 18:991-6. 2011..These proteins gradually become more concentrated during the vapour diffusion process starting from a larger protein solution ratio in the initial mixture...
- Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenaseDonald Poirier
Oncology and Molecular Endocrinology Research Center, CHUQ Pavillon CHUL and Université Laval, Quebec G1V 4G2, Canada
J Med Chem 48:8134-47. 2005..Moreover, the 3D-structure analysis of EM-1,745 complexed with type 1 17beta-HSD showed key interactions with both substrate- and cofactor-binding sites...
- Cofactor hydrogen bonding onto the protein main chain is conserved in the short chain dehydrogenase/reductase family and contributes to nicotinamide orientationRong Shi
Oncology and Molecular Endocrinology Research Center, Laval University Medical Center CHUQ and Laval University, Quebec G1V 4G2, Canada
J Biol Chem 279:16778-85. 2004..This common feature reveals a general mechanism among the SDR family, providing a rational basis for inhibitor design against biologically relevant SDR targets...
- Three-dimensional modeling of cytomegalovirus DNA polymerase and preliminary analysis of drug resistanceRong Shi
Research Center in Molecular Endocrinology, Centre Hospitalier Universitaire de Québec CHUL hospital and Laval University, Quebec City, Canada
Proteins 64:301-7. 2006..These results constitute a first step towards facilitating our understanding of drug resistance mechanisms for CMV and the interpretation of novel viral mutations...