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    LECTURES 30 36: Receptor Ligand Binding: Problem 1 Problem 1

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    Rojan Pradhan
    The document discusses three problems related to receptor-ligand binding: 1) Calculating the half-time of ligand binding for different initial ligand concentrations. 2) Determining the specific binding, dissociation constant (kd), and number of receptors per cell using binding data. 3) Deriving a relationship between ligand depletion (u) over time (τ) by solving the model equation for ligand depletion.

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    LECTURES 30 36: Receptor Ligand Binding: Problem 1 Problem 1

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    Rojan Pradhan
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    The document discusses three problems related to receptor-ligand binding: 1) Calculating the half-time of ligand binding for different initial ligand concentrations. 2) Determining the specific binding, dissociation constant (kd), and number of receptors per cell using binding data. 3) Deriving a relationship between ligand depletion (u) over time (τ) by solving the model equation for ligand depletion.

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    Q_&_A_Set_16.pdf

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    The document discusses three problems related to receptor-ligand binding: 1) Calculating the half-time of ligand binding for different initial ligand concentrations. 2) Determining the specific binding, dissociation constant (kd), and number of receptors per cell using binding data. 3) Deriving a relationship between ligand depletion (u) over time (τ) by solving the model equation for ligand depletion.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    87 views8 pages

    LECTURES 30 36: Receptor Ligand Binding: Problem 1 Problem 1

    Uploaded by

    Rojan Pradhan
    The document discusses three problems related to receptor-ligand binding: 1) Calculating the half-time of ligand binding for different initial ligand concentrations. 2) Determining the specific binding, dissociation constant (kd), and number of receptors per cell using binding data. 3) Deriving a relationship between ligand depletion (u) over time (τ) by solving the model equation for ligand depletion.

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    of 8

    LECTURES 30‐36: Receptor‐Ligand Binding

    Problem 1

    Obtain the half-time for the following ligand given the binding to the receptor and
    the following conditions.

    k-1=0.04 min-1 kD = 25 µM

    CL0 = 2,, 20,, 100 µ


    µM
    Solution: The Half-time period for the receptor –ligand binding is given by
    ln 2
    t 1
    2
    =
    ⎛ C ⎞
    k−1 ⎜1 + L0 ⎟ (8.1)
    ⎝ kD ⎠
    For CL0 = 2 µM,
    t 1
    2
    = 16.04 min
    F CL0 = 20 µM,
    For M t 1
    2
    = 9.627
    9 627 min
    i

    For CL0 = 200 µ


    µM, t 1
    2
    = 1.9254 min
    Problem 2

    Use the following data to determine the specific binding of a ligand A


    to a receptor
    p B as well as the values of kd and the number of receptors
    p
    per cell.

    CL0, M
    M Amount bound without unlabeled ligand
    Amount bound without unlabeled ligand  Amount bound with 100 excess 
    Amount bound with 100 excess
    unlabeled ligand
    1.5×10‐10 16, 000 6, 000

    6× 10‐10 60 000
    60, 000 24 000
    24, 000

    2.1×10‐9 120, 000 60, 000

    7 5 10‐99
    7.5×10 350 000
    350, 000 260 000
    260, 000

    1.5×10‐8 600, 000 510, 000


    Solution: The specific binding of ligand to receptor is given below.

    CL0, µM Specific binding of a ligand A to receptor B (Nc)

    1.5×10‐4 10, 000

    6× 10‐4 36, 000

    2.1×10‐3 60, 000

    7.5×10‐33 90, 000

    1.5×10‐2 90, 000

    Calculating Nc/CL0 and after plotting Nc/CL0 Vs. Nc we get

    kd= 6.67×10-10 M

    NRT/kd= 7.2×107 receptors/cell/µM

    Therefore NRT = 4.8×104


    Problem 3: The model equation for ligand depletion is given by
    du
    = (1 − u )(1 − η u ) α − u (1)
    dτ
    NC 0
    with u =u0 = at τ =0.
    N RT
    Solve the model equation to establish a relationship between u and τ.
    τ

    Solution: From equation (1), we can write


    du
    = dτ
    ⎡⎣(1 − u )(1 − η u ) α − u ⎤⎦ (11.1)

    After algebraic manipulations, we get


    du
    = dτ
    ⎡⎣ηα u − (ηα + α + 1) u + α ⎤⎦
    2
    (11.2)
    Taking out ηα common from the denominator, we get

    du
    = dτ (11.3)
    ⎡ 2
    ηα ⎢u −
    (ηα + α + 1) u+
    1 ⎤
    ⎥
    ⎣ ηα ηα ⎦

    Adjusting the terms in denominator to form quadratic equation in


    terms of u,
    du ((11.4))
    = dτ
    ⎡⎛ (ηα + α + 1) ⎞ ⎛ 1 (ηα + α + 1) ⎞ ⎤
    2 2

    ηα ⎢⎜ u − ⎟ + ⎜⎜ − ⎟⎥
    ⎢⎣⎝ 2ηα ⎠ ⎝η 4η α
    2 2
    ⎟⎥
    ⎠⎦
    Integrating equation (11.4) on both sides
    1 du
    ηα ∫ ⎡⎛
    = ∫ dτ (11.5)
    (ηα + α + 1) ⎞ ⎛ 1 (ηα + α + 1) ⎞ ⎤
    2

    ⎢⎜ u − ⎟ +⎜ − ⎟⎥
    ⎢⎣⎝ 2ηα ⎠ ⎝η 4η α
    2 2
    ⎠ ⎥⎦

    Let
    ⎛ 1 (ηα + α + 1) ⎞
    ⎜ − ⎟ = ± K 2

    ⎝η 4η α
    2 2
    ⎠
    Equation (11.5) becomes,
    1 du
    ∫
    ηα ⎡⎛ (ηα + α + 1) ⎞ 2
    ⎤
    = ∫ dτ
    (11.6)
    ⎢⎜ u − ⎟ ±K ⎥
    2

    ⎢⎣⎝ 2ηα ⎠ ⎥⎦
    (11 6) is of the form ∫
    Equation (11.6)
    (
    dx
    )
    x2 ± a2
    having solution
    1
    a
    tan( )
    x +C
    a

    Therefore the solution of equation (11.6) is

    1 ⎡⎣( 2η u + η + 1) + 1⎤⎦
    τ= tan +C (11.7)
    ηα K 2 Kη
    Put initial condition in equation (11.7), then we obtain

    1 ⎛ ⎡⎣( 2η u + η + 1) + 1⎤⎦ ⎡⎣( 2η u0 + η + 1) + 1⎤⎦ ⎞


    τ= ⎜ tan − tan ⎟
    ⎜
    ηα K ⎝ 2 Kη 2 Kη ⎟
    ⎠
    (11.8)

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