ArticleHormone molecular biology and clinical investigation2010
Structural rearrangement of SULT2A1: effects on dehydroepiandrosterone and raloxifene sulfation.
Article in Hormone molecular biology and clinical investigation, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
24 citing papers in PubMed.
- Bazedoxifene and Beyond: Identifying This SERM's Targets and Deciphering Its Molecular Mechanisms.Advances in pharmacological and pharmaceutical sciences · 2026Review
- Allosteric Mechanisms Triggering Substrate and Cofactor Binding in the SULT1A1 Dimer as Revealed by Molecular Dynamics Simulations.Journal of chemical information and modeling · 2025Article
- Mechanistic Insights into the Effect of Ligands on Structural Stability and Selectivity of Sulfotransferase 2A1 (SULT2A1).ACS omega · 2019Article
- Arenobufagin is a novel isoform-specific probe for sensing human sulfotransferase 2A1.Acta pharmaceutica Sinica. B · 2018Article
- A high frequency missense SULT1B1 allelic variant (L145V) selectively expressed in African descendants exhibits altered kinetic properties.Xenobiotica; the fate of foreign compounds in biological systems · 2018Article
- On the Molecular Basis Underlying the Metabolism of Tapentadol Through Sulfation.European journal of drug metabolism and pharmacokinetics · 2017Article
- Expression, purification and characterization of human cytosolic sulfotransferase (SULT) 1C4.Hormone molecular biology and clinical investigation · 2017Article
- Modification ofDrug target insights · 2017Article
- An engineered heterodimeric model to investigate SULT1B1 dependence on intersubunit communication.Biochemical pharmacology · 2016Article
- In Silico Prediction of Human Sulfotransferase 1E1 Activity Guided by Pharmacophores from Molecular Dynamics Simulations.The Journal of biological chemistry · 2016Article
- Celecoxib influences steroid sulfonation catalyzed by human recombinant sulfotransferase 2A1.The Journal of steroid biochemistry and molecular biology · 2015Article
- Dimeric human sulfotransferase 1B1 displays cofactor-dependent subunit communication.Pharmacology research & perspectives · 2015Article
- Human genetic disorders and knockout mice deficient in glycosaminoglycan.BioMed research international · 2014Review
- High accuracy in silico sulfotransferase models.The Journal of biological chemistry · 2013Article
- Structure, dynamics and selectivity in the sulfotransferase family.Drug metabolism reviews · 2013Review
- Testing the sulfotransferase molecular pore hypothesis.The Journal of biological chemistry · 2013Article
- Potent inhibition of human sulfotransferase 1A1 by 17α-ethinylestradiol: role of 3'-phosphoadenosine 5'-phosphosulfate binding and structural rearrangements in regulating inhibition and activity.Drug metabolism and disposition: the biological fate of chemicals · 2012Article
- A nucleotide-gated molecular pore selects sulfotransferase substrates.Biochemistry · 2012Article
- Sulfation of fulvestrant by human liver cytosols and recombinant SULT1A1 and SULT1E1.Pharmacogenomics and personalized medicine · 2011Article
- Site-directed mutagenesis of human cytosolic sulfotransferase (SULT) 2B1b to phospho-mimetic Ser348Asp results in an isoform with increased catalytic activity.The Journal of steroid biochemistry and molecular biology · 2011Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
backgroundHuman cytosoloic sulfotransferase (SULT) 2A1 is a major hepatic isoform and sulfates hydroxyl groups in structurally diverse sterols and xenobiotics. SULT2A1 crystal structures resolved in the presence and absence of 3',5'-diphosphoadenosine (PAP) or dehydropeiandrosterone (DHEA) suggest a significant rearrangement of the peptide that forms the surface of the active site in the presence of PAP. MATERIALS AND
methodsMolecular modeling was used to examine the effects of the rearrangement in SULT2A1 associated with 3'-phosphoadenosine 5'-phosphosulfate (PAPS) binding on the binding of DHEA and raloxifene. The kinetics of DHEA and raloxifene sulfation was analyzed to investigate the effects of the rearrangement on SULT2A1 activity.
resultsMolecular models indicate that DHEA is able to bind to SULT2A1 in both conformations (open, without PAP; closed, with PAP) in a catalytic configuration, whereas raloxifene bound in a catalytic conformation only in the open structure. Raloxifene did not bind in the smaller, closed substrate binding pocket. Kinetic analysis of DHEA sulfation was consistent with a random Bi-Bi reaction mechanism, whereas raloxifene sulfation was more indicative of an ordered reaction mechanism with raloxifene binding first. Initial burst kinetics with DHEA yielded similar results after preincubation of SULT2A1 with DHEA or PAPS. Preincubation of SULT2A1 with raloxifene showed a burst of raloxifene sulfate formation with the addition of PAPS. In contrast, little raloxifene sulfate was formed if SULT2A1 was preincubated with PAPS and the reaction initiated with raloxifene.
conclusionsThe structural rearrangements in SULT2A1 caused by PAPS binding can alter the sulfation mechanism and kinetics of different substrates.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.