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

Slides:



Advertisements
Similar presentations
BIOTRANSFORMATION, Drug metabolism, detoxification
Advertisements

Drug/xenobiotic metabolism and pharmacogenetics George Howell III, Ph.D.
PHASE II: Conjugation Reaction R O S E L Y N A. N A R A N J O.
Drug metabolism Refers to enzyme-mediated biotransformations (detoxication) that alter the pharmacological activity of both endogenous and exogenous compounds.
DISTRIBUTION The body is a container in which a drug is distributed by blood (different flow to different organs) - but the body is not homogeneous. Factors.
3. Metabolism Many xenobiotics undergo chemical transformation (biotransformation; metabolism) when introduced into biologic systems like the human body.
Chapter 2. Metabolism and Elimination A. Liver is the primary site of drug metabolism. First pass effect (or first pass metabolism) : metabolism of a drug.
O-linkage to GalNAc N-linkage to GlcNAc Posttranslation Modifications 1 Vitamin K-Dependent Modifications Vitamin K is a cofactor in the carboxylation.
Factors that Affect the Function of an Enzyme Lab Conclusions.
Phase-II Drug Metabolism
Absorption, Distribution, Metabolism and Elimination: Part II
1 SURVEY OF BIOCHEMISTRY Glycogen. 2 What is Glycogen? Branched polymer of glucose Storage form of glucose –Liver Maintenance of blood glucose levels,
Section 2.5: Enzymes Biology.
Drug Detoxification Dr. Howaida Supervised by : Prepared by:
Metabolism of Xenobiotics
Drug metabolism and elimination Metabolism  The metabolism of drugs and into more hydrophilic metabolites is essential for the elimination of these.
Example2: Building a protein from amino acids: Substrate: Amino acids Product: The protein.
Prepared by Prof .Abdulkader.H.El Daibani
Prof. Hanan Hagar Dr.Abdul latif Mahesar Pharmacology Department Pharmacokinetics III Concepts of Drug Disposition.
NADPH- Cyt. P450 reductase P450 S SOH O 2 H 2 O e NADPH NADP +
Properties of Enzymes. Enzymes are catalysts What properties would ideal catalysts have?
Phase II: Conjugation Synthetic reaction of a xenobiotic (or of a Phase I metabolite of a xenobiotic) with an endogenous substance Results in introduction.
Drug Metabolism and Prodrugs
Phase II: Conjugation Synthetic reaction of a xenobiotic (or of a Phase I metabolite of a xenobiotic) with an endogenous substance Results in introduction.
Terodiline Aromatic p-hydroxylation predominate with R but benzylic hydroxylation is preferred with S (homework)
Chapter 9 Biotransformation
Video Questions What do the following prefixes mean? Mono, Poly, Exo, and End What do you need to have “LIFE”? Draw a picture of an atom. Why do atoms.
Section 1, Lecture 4 Phase I reactions-oxidative occur in the endoplasmic reticulum of liver (microsomal fractions) - catalyzed by the microsomal.
Prof. Hanan Hagar Dr.Abdul latif Mahesar Pharmacology Department.
CYP Biotransformations
Prof. Hanan Hagar Pharmacology Department By the end of this lecture, students should:  Recognize the importance of biotransformation  Know the different.
1 drug molecule Highly lipophyllic lipophilic polar hydrophylic accumulation (fatty tissues) phase I polar phase IIbioinactivation conjugation hydrophylic.
Microbiology for the Health Sciences. Metabolism: the sum of all chemical reactions that occur in a living cell in order that the cell sustains its life’s.
Pharmacology Department
Drug Metabolism and Prodrugs
Concepts of drug disposition Pharmacology Department
Phase II or Conjugation Reactions – Conjugation reactions link an endogenous moiety (an endocon) to the original drug (if polar functions are already present)
Biotransformation Biotransformation Siva Nageswararao Mekala Assistant Professor Dept. of clinical Pharmacology.
Amino Acids, Peptides, and Proteins. Introduction to Amino Acids  There are about 26 amino acids, many others are also known from a variety of sources.
Pharmacology I BMS 242 Lecture 4 Pharmacokienetic Principles (3&4): Drug Metabolism and Excretion [Elimination] Dr. Aya M. Serry 2016.
Reviewing Enzymes. - All enzymes are proteins...proteins are also called “polypeptides”. - Enzymes are made up of amino acids (amino group + carboxyl.
Medicinal Chemistry Lecture Drug Metabolism Lectures 11 & 13 Chemical Delivery Systems Joseph O. Oweta | PHS 2201.
Induction Increased transcription Increased protein synthesis Enhanced stability of protein Synthesis of enzyme with higher catalytic activity Inducible.
Nad metabolites The pyridine dinucleotide, NAD+, is a substrate of sirtuins and coenzyme for hydride transfer enzymes and other NAD+-dependent ADP ribose.
METABOLISM / BIOTRANSFORMATION of TOXICANTS.
Chapter 5 Drug Metabolism
Detoxification by the Liver
Interfering with enzymes (poisons and drugs)
Metabolism - Biotransformation
Metabolism & Detoxification
METABOLISM / BIOTRANSFORMATION of TOXICANTS.
Metabolism of drugs and xenobiotics
METABOLISM OF XENOBIOTICS
By: Dr. Roshini Murugupillai
Drug Metabolism Drugs are most often eliminated by biotransformation and/or excretion into the urine or bile. The process of metabolism transforms lipophilic.
Methylation Methylation with methyl group transfer from S-adenosyl methionine, although feasible, is not an important pathway for drug metabolism. Methylation.
C2 7.2 (a) Acids and metals L/O * acid + metal salt + hydrogen
Biotransformation Saiesh phaldesai 1st year M.pharma Pharmaceutics
Drug Elimination Drug elimination consists of 2 processes
Metabolic Changes of Drugs and Related Organic Compounds
PEGylation Products and Services Profacgen. Introducing polyethylene glycol (PEG) to biomolecules and pharmaceuticals is known to enhance stability and.
Draw an amino acid.
Induction Increased transcription Increased protein synthesis
Phase-II Drug Metabolism Pharmaceutical Medicinal Chemistry-I
Drug conjugation pathways (phase II)
Drug Detoxification Dr. Howaida Supervised by : Prepared by:
Metabolism of drugs and xenobiotics
Enzyme digesting a molecule
Presentation transcript:

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

Conjugation Reactions Sulfation (3`- phosphoad enosine 5`- phosphosul phate( PAPS)

Examples   ethanol   p-hydroxyacetanilide   3-hydroxycoumarin

Sulfation may produce active metabolites

Conjugation Reactions Acetylation

 The transfer of acetyl group takes place in presence of N-acetyl transferases.  In acetylation although water solubility is not increased, it helps in terminating the pharmacological activity of the drug or its amino metabolite.

Examples: Procainamide, isoniazid, sulfanilimide, histamine NAT (N-Acetyl transferase)enzyme is found in many tissues, including liver.

Isoniazide

Amino acid conjugation Cinnamic acid

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