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    CHE631-Module 4 - Enzymes

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    rutwick
    The document discusses the classification, active sites, and kinetics of enzymes. It describes factors that affect enzymatic reaction rates, such as substrate concentration and temperature. The Michaelis-Menten equation is introduced as a model for enzyme kinetics. Theories of drug action include the occupancy theory, rate theory, and induced fit theory. Structure-activity relationships examine how minor changes in a drug's structure can impact its biological activity.

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    CHE631-Module 4 - Enzymes

    Uploaded by

    rutwick
    76 views26 pages
    The document discusses the classification, active sites, and kinetics of enzymes. It describes factors that affect enzymatic reaction rates, such as substrate concentration and temperature. The Michaelis-Menten equation is introduced as a model for enzyme kinetics. Theories of drug action include the occupancy theory, rate theory, and induced fit theory. Structure-activity relationships examine how minor changes in a drug's structure can impact its biological activity.

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    CHE631-Module 4 - enzymes-converted

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    The document discusses the classification, active sites, and kinetics of enzymes. It describes factors that affect enzymatic reaction rates, such as substrate concentration and temperature. The Michaelis-Menten equation is introduced as a model for enzyme kinetics. Theories of drug action include the occupancy theory, rate theory, and induced fit theory. Structure-activity relationships examine how minor changes in a drug's structure can impact its biological activity.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    76 views26 pages

    CHE631-Module 4 - Enzymes

    Uploaded by

    rutwick
    The document discusses the classification, active sites, and kinetics of enzymes. It describes factors that affect enzymatic reaction rates, such as substrate concentration and temperature. The Michaelis-Menten equation is introduced as a model for enzyme kinetics. Theories of drug action include the occupancy theory, rate theory, and induced fit theory. Structure-activity relationships examine how minor changes in a drug's structure can impact its biological activity.

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    © All Rights Reserved
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    Download as pdf or txt
    of 26

    Molecules of life (CHE 631)

    (CBZ- Dr. Riya Datta)

    MISSION VISION CORE VALUES


    CHRIST is a nurturing ground for an individual’s Excellence and Service Faith in God | Moral Uprightness
    holistic development to make effective contribution to Love of Fellow Beings
    the society in a dynamic environment Social Responsibility | Pursuit of Excellence
    CHRIST
    Deemed to be University

    Enzymes and correlation with drug action

    Classification-active site- Fischer and Koshland models-Enzyme kinetics-


    factors affecting rate of enzymatic reactions- Michaelis-Menten
    equation. Mechanism of enzyme action, factors affecting enzyme
    action, Coenzymes and cofactors and their role in biological reactions,
    Specificity of enzyme action (including stereospecificity), Enzyme
    inhibitors and their importance, phenomenon of inhibition (Competitive
    and Non- competitive inhibition).
    Theories of drug activity: Occupancy theory, rate theory and induced fit
    theory. Structure –activity relationships of drug molecules.

    Excellence and Service


    CHRIST
    Deemed to be University

    Enzymes

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Naming of enzymes

    Excellence and Service


    CHRIST
    Classification Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Coenzyme

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Linkage

    Excellence and Service


    CHRIST
    Deemed to be University

    Active site

    ● The specific area of the enzyme that binds the substrate and transforms it.
    ● It represents a small portion of the enzyme surface.
    ● It is a 3 dimensional entity containing amino acids residues from different
    parts of the enzyme molecule.

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Factors affecting rates of enzymatic reactions

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Vo =1/2 Vmax
    Km+S= 2S
    Km=S

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Excellence and Service


    CHRIST
    Deemed to be University

    Theories of drug activity


    Once a drug molecule attaches to the receptor site it may either initiate a
    response or prevent a response from occurring. This is similar to the lock and
    key theory of enzyme action. Only ligands that fulfill all criteria for fitting into
    the receptor can produce an effect. Some ligands can fit into the receptor site
    but not perfectly and so will not produce a response. By doing this these
    ligands prevent the original ligand from binding to the receptor and producing
    a response.
    Eg: To prevent the constriction of airway smooth muscles in asthmatic conditions
    one can administer drugs that prevent the actions of the signaling molecules
    causing muscle contraction.

    Excellence and Service


    CHRIST
    Deemed to be University

    Occupancy Theory
    ● This theory was Proposed by Clarke. It considers receptor-ligand interaction to be a
    bimolecular interaction in which the receptor-ligand complex is responsible for the
    biological effect. Clarke assumed that the effect of drugs were proportional to the
    fraction of receptors occupied by the drug. For a maximum effect of the drug it has to
    occupy all receptors. According to this theory the drug(A) interacts in a reversible way
    with the receptor (R) and the formed complex (AR) gives rise to the effect.
    ● A+R ↔ AR → Effect
    The rate of association =k1 [A][R]
    The rate of dissociation =k2 [AR] within a certain period of time the same number of
    molecules A will bind to and dissociate from the receptor.
    At equilibrium the dissociation constant K=k1/k2=[A][R]/[AR]
    Excellence and Service
    CHRIST
    Deemed to be University

    Rate theory
    ● This theory was Proposed by Paton and Rang in 1965.The most important
    factor in determining drug action is the rate at which drug-receptor
    combination takes place. Paton proposed that the stimulus was produced
    only when the ligand first occupied the receptor site. Stimulation does not
    continue even though the site was still occupied. This is because the receptor
    undergoes a second conformational change, which results in its inactivation.
    As long as the ligand is bound to the receptor, the receptor is unable to
    produce a further stimulus. As soon as the ligand disengages from the
    receptor it returns to its original conformation. As a result, further stimulation
    of the receptor can now occur.

    Excellence and Service


    CHRIST
    Deemed to be University

    Induced fit theory

    ● After combination the substrate induces a change in conformation of the


    enzyme leading to an enzymatically active orientation of groups. The induced
    fit is brought about by the intermolecular binding interactions that can take
    place between the drug and the binding site. This is similar to enzyme
    substrate binding but in this case no catalysed reaction follows binding.

    Excellence and Service


    CHRIST
    Deemed to be University
    Structure–activity relationship (SAR)
    ● Based on the observation that compounds with similar structures to a pharmacologically active drug
    are often themselves biologically active. A study of the SAR of a lead compound may be used to
    determine the parts of its structure that are responsible for its biological activity. This information
    may be used to develop a new drug that has increased activity by selecting the structure with the
    optimum activity, a different activity from an existing drug and fewer unwanted side effects. SAR
    studies are carried out by making minor changes to the structure of a lead to produce analogues
    and assessing its effect on biological activity.
    ● These changes may be classified as changing: the size and shape of the carbon skeleton; the
    nature and degree of substitution; and the stereochemistry of the lead .The selection of the changes
    required to produce analogues of a lead is made by considering the activities of compounds with
    similar structures and also the possible chemistry and biochemistry of the intended analogue.
    Changing the structure of the lead compound could result in an analogue that is too big to fit its
    intended target site.
    Excellence and Service

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