You have determined the mode of inhibition for NSAMB but you must now determine the KI value to obtain a relative measure of the potency of this inhibitor. Based on the mode of inhibition, how are the equations for KP and VP influenced by the presence of inhibitor? KPP is unaffected by changes in [I]; VAPP Vmaz max 1+ V KAPP M Км Vapp %3D max 1+ 1+ KPP KM(1+ Vapp M max 1+ O Neither K app M nor Vmax are affected by changes in [I о КР - KM(1+ ) app ;Vmax is unaffected by changes in I
Q: The typical distribution of K+ and Na+ ions inside and outside the cell is: [K+]in = 150 mM;…
A: Introduction The reversal potentials of the ions can be calculated by using the Nernst equation…
Q: mode of action of Rosuvastatin and fenofibrates
A: Lipid lowering drugs: As the name states, these are drugs that lower the level of lipids in blood.…
Q: EXTRACELLULAR INTRACELLULAR ION CONCENTRATION CONCENTRATION (mM) (mM) K* 4 140 Na* 145 15 Cl- 110 4…
A: At the peak of action potential no flow of ions occur at equilibrium, means when membrane potential…
Q: what is the best calcium channel blocker for a patient with CAD, asthma, and hyperlipidemia?
A: Calcium channel blockers are drugs used to lower blood pressure. They work by slowing the movement…
Q: PGC1alpha O is regulated by PPAR-delta O affects many tissues relevant to endurance training O is…
A: ANSWER) PGC1 stands for Peroxisome proliferator-activated receptor gamma co-activator 1 alpha and is…
Q: How will you exploit the effector proteins of Type 3 and Type 4 secretion systems to develop novel…
A: Type 3 secretion systems are the needle-like structure which is used in the form of the sensory…
Q: Calculate the free energy of transport for the movement of potassium by the sodium/potassium pump…
A: The Sodium/Potassium pump is a transmembrane ATPase that is situated on the cytosolic side, in the…
Q: Synthetic opioids are frequently being used for analgesia, i.e. as pain killers. While morphine or…
A: * Synthetic opioids used for analgesia as pain killers. *morphine and other agonists like fentanyl…
Q: The catechol system is important for the binding of adrenergic agonists, yet is not required for…
A: Introduction Different types of adrenergic receptors are found to mediate various physiological…
Q: Assuming you have an agonist, a competitive antagonist, and an easy assay for measuring binding of…
A: An agonist is a substance that can bring about a specific physiological response by binding to a…
Q: The administration of specific HGFs is proving to be of considerable clinical importance. Explain…
A: Introduction HGF is a paracrine cellular growth factor. It is produced by mesenchymal cells and acts…
Q: If in an animal cell the Jequilibrium potentials|* of sodium and potassium are essentially equal…
A: Every cell maintain a potential difference across the plasma membrane called as the membrane…
Q: In order to optimize acetylcholinesterase inhibition, a set of benzylamine derivatives were studied,…
A: The given relationship [log(1/C) = -0.187π + 0.57σ + 3.893] represent Hansch QSAR analysis model.…
Q: If you were a medical researcher, what other areas of the blood-clotting pathway would you target…
A: A stroke may be a medical emergency during which the blood supply to any portion of the brain is…
Q: compare the efficacy and potency of each of the following: Furosemide Hydrochlorothiazide Morphine…
A: Drug efficacy: The efficacy of the drug is defined as the ability of the drug to treat a condition…
Q: What happens to an agonist's efficacy ("maximum effect") and potency (potency) in the presence of a…
A: Efficcy means the maximum effect that a substance or drug can produce. and, potency means the…
Q: This question relates to the "Tength constant" (A) and decay of a local graded potential over…
A: It is assumed that the membrane potential is identical in different parts of the membrane in a…
Q: Write down the mode of action of Rosuvastatin and Fenofibrates?
A: Increased levels of cholesterols in the blood is a worrying scenario as it can cause various medical…
Q: VA 256 192 128 9 1.5 10- 38 25- 19 125- 64. .032- .023 .047
A: The MIC, or minimum inhibitory concentration, is the lowest concentration (in μg/mL) of an…
Q: M An obese man was prescibed the lipophilic drug phenobarbital for treatment of seizures. He noticed…
A: Pharmacokinetics of drug is the what drug does to body and it is measured as Absorption ,…
Q: What is the type of the inhibitor when Km keeps increasing and Vmax keeps decreasing?
A: An enzyme is a biocatalyst and all enzymes are made of proteins. Inhibition in a reaction can happen…
Q: After doing some tests, the patients velocity constant is found to be 0.03 hour^-1. The doctor plans…
A: The velocity constant (k) for the patient is 0.03 hour-1. First of all, the infusion rate should be…
Q: The following is HPLC data. Using the standard curve determine the concentration of caffeine in each…
A: HPLC stands for high-performance liquid chromatography. This technique is used for the separation…
Q: Naproxen 500 mg twice daily has been prescribed for TW. If TW were to experience dyspepsia during…
A: NSAIDs or nonsteroidal anti-inflammatory drugs are the drugs used for pain, inflammation, and fever.…
Q: The EC50 of an agonist for a GPCR is almost always (greater than, equal to, or less than) the KD of…
A: Half maximal effective concentration (EC50) of a ligand or drug defines the concentration of drug…
Q: Atropine (I) and Ipratropium bromide (II) are both muscarinic acetylcholine receptor antagonists.…
A: Atropine and ipratropium bromide are the drug use to treat pulmonary disorders . Ipratropium…
Q: Explain and draw the general mechanism of edurant (rilpivirine) and how it binds to its target.
A: Rilpivirine is an antiviral medication that prevents HIV from spreading in your body. Rilpivirine is…
Q: Ames test: Describe (in detail) the Ames test (discussing both the set up and results of the Control…
A: Introduction The Ames test is a method that uses bacteria to test whether the given chemical can…
Q: What is the maximum allowable dosage of the most commonly used anesthetic solution i.e. 2%…
A: Anesthesia is the process of administering medication (anesthetics) during surgery or procedures in…
Q: How will PP1 interaction with an AMPA receptor alter that receptor's single channel l-V curve?
A: AMPA receptors mediate quick excitatory synaptic transmission within the central nervous system.…
Q: Calculate, or make a best estimate of, the unknown factors in the situations listed in Table 1.…
A: Hi! Thanks for your question. As you have posted multiple questions and have not mentioned which…
Q: Experimental measurements of the reversible interaction between a drug and its receptor show…
A: Given , Rate of dissociation, K2 = 0.005 min-1 and Dissociation constant, KD = 16pm.
Q: Which of the following would have the lowest (most negative) standard reduction potential (E’0)?…
A:
Q: The following kinetic data were collected for prostaglandin endoperoxide synthase, an enzyme…
A: In order to solve this question, first, we need to draw the Lineweaver-Burk plot (LB plot) and find…
Q: Why muscarinic receptor antagonists are different from adrenergic beta-2-receptor agonists. What is…
A: Muscarinic receptor antagonist functions by blocking the cholinergic response. Adrenergic beta 2…
Q: Beyond stimulating aldosterone secretion, list the effects of ANG II. Give examples and brief…
A: The RAAS (renin-angiotensin-aldosterone system) is operated by JGA (juxtaglomerular apparatus). The…
Q: The recommended dose of an anti-epileptic drug is 445 mg for a 180-lb woman, what would be a…
A: Epilepsy is a central nervous system disorder in which brain activity is abnormal, causing seizures…
Q: Shown are different derivatives of acetylcholine. N' A H2N H2N 1. Which one is expected to lose its…
A: Acetylcholine: Acetylcholine is a choline and acetic acid derivative where both are bond by ester…
Q: Calculations Involving Units, mcg/mg and Other Measurement of Potency. Show your complete solution.…
A: First of all ib converted in kg 175 lb divided by 2.2 = 79.5 kg Desired dose = 5mcg/kg/min =…
Q: Consider the effect of a twofold increase in the ECF concentration of Na+ or K+ ions. Which increase…
A: Na+ & K+ ions concentration play an important role in electrical signaling of Heart. Na+ ATPase…
Q: Briefly describe the difference between agonist and antagonists. What is a difference comparing to…
A: Disclaimer: Since you have asked us multiple questions, we have offered the solution for the first…
Q: anti-pain activity of aspirin
A: When your nerves transmit an electrical signal to your brain, you feel pain. When you're hurt, your…
Q: Of two agonists acting at the same receptor, X has an EC50 value of 107 M and Y has an EC50 value of…
A: The amount of drug needed to produce a certain response is known as dug potency. Relative potency is…
Q: Irritability in animals can be measured or determined using the right methodology and apparatus.…
A: The response of animals to the physical and chemical changes occurring in the internal and external…
Q: What are tyrosine kinase and GPCR? Give example of one pathology that can occur in…
A: Tyrosine kinase and GPCR dysregulation and rescue :-
Trending now
This is a popular solution!
Step by step
Solved in 2 steps with 1 images
- Based on your Lineweaver-Burk plot, what is the mode of PaESBL-1 inhibition by NSAMB? What is the equation for the double-reciprocal plot at 20 nMnM NAMB?Which ONE of these statements is the most accurate definition of the mode of action of imatinib? Select one: A.It is a specific inhibitor of the BCR‐ABL1 fusion protein and blocks phosphatase activity by competing with adenosine triphosphate (ATP) binding B.It is a specific inhibitor of the BCR‐ABL1 fusion protein and blocks tyrosine kinase activity by competing with adenosine triphosphate (ATP) binding C.It is a specific inhibitor of the BCR‐ABL1 fusion protein and blocks tyrosine kinase activity by interaction with the enzyme site D.It is a specific inhibitor of the BCR‐ABL1 fusion protein and blocks phosphatase activity by interaction with the enzyme siteDuring an SAR effort to identify tyrosine kinase inhibitors, it was found that compound 2 was significantly more potent and selective than compound 1. To what might you attribute this improvement in activity and selectivity? Explain. IC-5 micromolar IC-0.1 mromolar
- From the Hill Plot below, the of the first binding event for the receptor-ligand system under study is: Q1 4 nM 10 μΜ -2 nM 2 nM Calculate the Hill Coefficient from the receptor-ligand binding data below: Q2 4 100 2 3 (077) log 10 8 6 4 2 0 -2 -4 -6 -6 -4 -2 0 2 4 log [L] (nM) 6 8 10Based on the principles of RP-HPLC, which sub fraction in the figure (P1 to P8) is the most polar? Explain.added ligand concentration of 10 µM is 5 × 10³ s¹. What is the value of the reverse rate constant k_1 = 1 ×10-4 Incorrect Macmillan Learning You have not correctly calculated the value of the reverse rate constant. To begin, calculate the value of k₁ by dividing the rate of receptor-ligand complex formation (the rate of the forward reaction) by the ligand concentration. k₁ = rate forward [L] Then, calculate the value of the reverse rate constant, k_₁, by multiplying the dissociation constant, Kd, and the forward rate constant, k₁. k_1 = Kak₁
- CTP inhibits ATCase; however, the inhibition is not complete. Can you suggest another molecule that might enhance the inhibition of ATCase?Using the information given, determine the Kd for the binding of HABA to BSA. B= y-intercept (E bound) 2457.6x (E unbound) Data for the binding of HABA to BSA y = 4E-06x + 5.2134 R² = 0.928CYP2E1 has a much higher Km for ethanol than ADH (11 mM versus 0.05 mM,respectively). When greater portions of ethanol are ingested (0.08% or 17 mM), which part of the statement would be true?
- Functional and structural analysis indicates that Gleevec is an ATPcompetitive inhibitor of the Bcr-Abl kinase. In fact, many kinase inhibitors under investigation or currently marketed as drugs are ATP competitive. Can you suggest a potential drawback of drugs that utilize this particular mechanism of action?Why does the apparent KM decrease in the presence ofan uncompetitive inhibitor?Two GPCR mutations (Mutant A and Mutant B) were tested for activity. One was confirmed as being a constitutively activating, gain of function GPCR mutation and one was confirmed as being a loss of function GPCR mutation. Which is which? Explain your answer.