Ligand 1alpha,25-dihydroxyvitamin D3

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Basic Ligand Information

Molecular Structure
Picture of 1alpha,25-dihydroxyvitamin D3 (click for magnification)
Molecular Formula
BRENDA Name
InChIKey
C27H44O3
1alpha,25-dihydroxyvitamin D3
GMRQFYUYWCNGIN-NKMMMXOESA-N
Synonyms:
1,25(OH)2D3, 1,25-dihydroxyvitamin D, 1,25-dihydroxyvitamin D3, 1-alpha,25-dihydroxyvitamin D3, 1alpha,25-dihydroxy-vitamin D3, 1alpha, 25-dihydroxy-vitamin D3, 1alpha,25-dihydroxycholecalciferol, 1alpha,25-dihydroxyitamin D3, 1alpha,25-dihydroxyvitamin-D3, calcitriol


Show all pahtways known for Show all BRENDA pathways known for 1alpha,25-dihydroxyvitamin D3

Roles as Enzyme Ligand

In Vivo Substrate in Enzyme-catalyzed Reactions (4 results)

EC NUMBER
PROVEN IN VIVO REACTION
REACTION DIAGRAM
LITERATURE
ENZYME 3D STRUCTURE

In Vivo Product in Enzyme-catalyzed Reactions (3 results)

EC NUMBER
PROVEN IN VIVO REACTION
REACTION DIAGRAM
LITERATURE
ENZYME 3D STRUCTURE

Substrate in Enzyme-catalyzed Reactions (14 results)

EC NUMBER
REACTION
REACTION DIAGRAM
LITERATURE
ENZYME 3D STRUCTURE
1alpha,25-dihydroxyvitamin D3 + O2 + [reduced NADPH-hemoprotein reductase] + H+ = 1alpha,25,26-trihydroxyvitamin D3 + [oxidized NADPH-hemoprotein reductase] + H2O
show the reaction diagram
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1alpha,25-dihydroxyvitamin D3 + 2 reduced ferredoxin [iron-sulfur] cluster + 2 H+ + O2 = 1alpha,25(R),26-trihydroxyvitamin D3 + 1alpha,25(S),26-trihydroxyvitamin D3 + 2 oxidized ferredoxin [iron-sulfur] cluster + H2O
show the reaction diagram
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UDP-D-glucuronate + 1alpha,25-dihydroxyvitamin D3 = UDP + 1alpha,25-dihydroxyvitamin D3 25-O-beta-D-glucuronoside
show the reaction diagram
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Product in Enzyme-catalyzed Reactions (14 results)

EC NUMBER
REACTION
REACTION DIAGRAM
LITERATURE
ENZYME 3D STRUCTURE
1alpha-hydroxyvitamin D3 + reduced adrenodoxin + O2 = 1alpha,25-dihydroxyvitamin D3 + oxidized adrenodoxin + H2O
show the reaction diagram
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Activator in Enzyme-catalyzed Reactions (5 results)

EC NUMBER
COMMENTARY
LITERATURE
ENZYME 3D STRUCTURE
gives a strong (100fold) upregulation of 5-lipoxygenase protein in differentiating Mono Mac 6 cells
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upregulation of enzyme activity. In HL-60 cell, stimulation is augmented by retinoid X-receptor agonists, blocked by retinoid X-receptor specific antagonists, and retinoic acid receptor specific agonists and antagonist have no effect. In NB-4 cell, upregulation is unaffected by the specific classical nuclear vitamin D receptor and retinoid X-receptor antagonists, but is blocked by a plasma-membrane associated vitamin D receptor antagonist and increases by plasma-membrane associated vitamin D receptor agonists
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Inhibitor in Enzyme-catalyzed Reactions (3 results)

EC NUMBER
COMMENTARY
LITERATURE
ENZYME 3D STRUCTURE
enzyme activity decreases by approximately 40% in the presence of the hormone
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inhibition of CDK2 activity by 1,25-dihydroxyvitamin D3 is associated with decreased T160 phosphorylation, a residue whose phosphorylation in the nucleus is essential for CDK2 activity. 1,25-dihydroxyvitamin D3 increases the stability of the cyclin-dependent kinase inhibitor p27KIP1. Ectopic expression of cyclin E is sufficient to overcome 1,25-dihydroxyvitamin D3-mediated cytoplasmic mislocalization of CDK2 and all antiproliferative effects of 1,25-dihydroxyvitamin D3, yet endogenous levels of cyclin E or binding to CDK2 are not affected by 1,25-dihydroxyvitamin D3. Targeting CDK2 to the nucleus of 1,25-dihydroxyvitamin D3-sensitive cancer cells blocked G1 accumulation and growth inhibition by 1,25-dihydroxyvitamin D3
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1,25-dihydroxyvitamin D inhibition of TACE is a potential common mechanism underlying the efficacy of therapy with 1,25-dihydroxyvitamin D or its analogs to improve outcomes in chronic kidney disease. 1,25-dihydroxyvitamin D prevents/moderates not only the onset and progression of parathyroid TACE/TGFalpha-driven secondary hyperparathyroidism, but renal TACE/TGFalpha-driven fibrotic and inflammatory lesions to the renal parenchyma, and TACE/TNFalpha-driven systemic inflammation
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3D Structure of Enzyme-Ligand-Complex (PDB) (22 results)

Enzyme Kinetic Parameters

kcat Value (Turnover Number) (11 results)

EC NUMBER
TURNOVER NUMBER [1/S]
TURNOVER NUMBER MAXIMUM [1/S]
COMMENTARY
LITERATURE
0.0009
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26-hydroxylation, mutant R73V/R84A, pH not specified in the publication, temperature not specified in the publication

KM Value (16 results)

EC NUMBER
KM VALUE [MM]
KM VALUE MAXIMUM [MM]
COMMENTARY
LITERATURE
0.0012
-
26-hydroxylation, mutant R73V/R84A, pH not specified in the publication, temperature not specified in the publication

References & Links

Links to other databases for 1alpha,25-dihydroxyvitamin D3

ChEBI
PubChem
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PubChem