sulphate conjugation a sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`-...

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Sulphate conjugation Sulphate conjugation A sulphate molecule is transferred A sulphate molecule is transferred from the cofactor (3`- from the cofactor (3`- phosphoadenosine 5`- phosphoadenosine 5`- phosphosulphate, PAPS) to the phosphosulphate, PAPS) to the substrate by enzymes known as substrate by enzymes known as sulfotransferases. sulfotransferases.

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Page 1: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Sulphate conjugationSulphate conjugation

A sulphate molecule is transferred from the A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`-cofactor (3`-phosphoadenosine 5`-phosphosulphate, PAPS) to the substrate by phosphosulphate, PAPS) to the substrate by enzymes known as sulfotransferases.enzymes known as sulfotransferases.

Page 2: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Conjugation ReactionsConjugation Reactions Sulfation Sulfation

)3-`phosphoadenosine 5`-phosphosulphate( PAP

S)

Page 3: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Examples

ethanol p-hydroxyacetanilide 3-hydroxycoumarin

Page 4: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes
Page 5: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Sulfation may produce active Sulfation may produce active metabolitesmetabolites

Page 6: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Conjugation ReactionsConjugation ReactionsAcetylationAcetylation

Page 7: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

The transfer of acetyl group takes place in The transfer of acetyl group takes place in presence of N-acetyl transferases.presence of N-acetyl transferases.

In acetylation although water solubility is not In acetylation although water solubility is not increased, it helps in terminating the increased, it helps in terminating the pharmacological activity of the drug or its pharmacological activity of the drug or its amino metabolite.amino metabolite.

Page 8: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Examples: Procainamide, isoniazid, sulfanilimide, histamine

NAT (N-Acetyl transferase)enzyme is found in many tissues, including liver .

Page 9: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes
Page 10: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Isoniazide

Page 11: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Amino acid conjugationAmino acid conjugation

Cinnamic acid

Page 12: Sulphate conjugation  A sulphate molecule is transferred from the cofactor (3`-phosphoadenosine 5`- phosphosulphate, PAPS) to the substrate by enzymes

Glycine is the most common amino acid used Glycine is the most common amino acid used for conjugation, while a fewfor conjugation, while a few glutamine glutamine conjugates have been identified in humans.conjugates have been identified in humans.