![3. Antiproliferative and antimetabolic drugs](http://s1.studyres.com/store/data/008262620_1-9c2279a64cdab51a2eff7bb7a066e2bb-300x300.png)
3. Antiproliferative and antimetabolic drugs
... • Binding to the εchain of CD3, a monomorphic component of the T-cell receptor complex involved in antigen recognition, cell signaling, and proliferation ...
... • Binding to the εchain of CD3, a monomorphic component of the T-cell receptor complex involved in antigen recognition, cell signaling, and proliferation ...
Cholinoceptor blocking drugs
... similar to that which would occur following reduction of activity in postganglionic, parasympathetic and postganglionic cholinergic sympathetic nerves. Both drugs also block CNS muscarinic receptors ...
... similar to that which would occur following reduction of activity in postganglionic, parasympathetic and postganglionic cholinergic sympathetic nerves. Both drugs also block CNS muscarinic receptors ...
Q22 Describe the factors that increase the risk of
... • Relative potency à relative toxicity approximates the relative potency of the agent used • Mechanism à all act via binding to and inactivating sodium channels, however bupivacaine is ten times slower at ...
... • Relative potency à relative toxicity approximates the relative potency of the agent used • Mechanism à all act via binding to and inactivating sodium channels, however bupivacaine is ten times slower at ...
`drug`.
... The drug must fit into the Binding Site and shape complementarity is an important feature of a drug molecule. Competitive enzyme inhibitors often bear a resemblance to the substrate, as they bind to the same Active Site. This is also true for some receptor antagonists, but not all. The strength of a ...
... The drug must fit into the Binding Site and shape complementarity is an important feature of a drug molecule. Competitive enzyme inhibitors often bear a resemblance to the substrate, as they bind to the same Active Site. This is also true for some receptor antagonists, but not all. The strength of a ...
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... drugs is 1.2mmol/l Most drugs therapeutic plasma level < 1.2 mmol/l so binding sites not saturated and fraction unbound not dependant on drug concentration Important if therapeutic concentration nearing saturation ( sulphonamides and tolbutamide) doubling dose can more than double free ...
... drugs is 1.2mmol/l Most drugs therapeutic plasma level < 1.2 mmol/l so binding sites not saturated and fraction unbound not dependant on drug concentration Important if therapeutic concentration nearing saturation ( sulphonamides and tolbutamide) doubling dose can more than double free ...
Paclitaxel- and lapatinib-loaded lipopolymer micelles overcome multidrug resistance in prostate cancer.
... transporters in prostate cancer cells (Fig. 1). These transporters, such as P-glycoprotein (P-gp), breast cancer resistance protein, and multiple drug resistance protein, increase drug efflux and reduce drug accumulation in tumor cells [3–5]. The prognosis of patients with MDR cancer is poor, due to ...
... transporters in prostate cancer cells (Fig. 1). These transporters, such as P-glycoprotein (P-gp), breast cancer resistance protein, and multiple drug resistance protein, increase drug efflux and reduce drug accumulation in tumor cells [3–5]. The prognosis of patients with MDR cancer is poor, due to ...
Free drug fraction vs. free drug concentration
... When equilibrium is achieved, according to eqn 8, fu increases and according to eqns 16 and 17 (warfarin is a low extraction ratio drug), if fu increases then Ctot decreases but Cfree remains unchanged (Fig. 1). Cfree can only transiently increase until redistribution and elimination of the generall ...
... When equilibrium is achieved, according to eqn 8, fu increases and according to eqns 16 and 17 (warfarin is a low extraction ratio drug), if fu increases then Ctot decreases but Cfree remains unchanged (Fig. 1). Cfree can only transiently increase until redistribution and elimination of the generall ...
Chapter 6 Mitosis
... I can show you what the different phases of cell division look like and explain what is happening. SPI 0707.1.4 Sequence a series of diagrams that depict chromosome movement during plant cell division. ...
... I can show you what the different phases of cell division look like and explain what is happening. SPI 0707.1.4 Sequence a series of diagrams that depict chromosome movement during plant cell division. ...
lec.8-426
... • The primary use of anticonvulsants drugs is in the prevention and control of epileptic seizures. • The ideal antiepileptic drug should completely suppress seizures in doses that do not cause sedation or other undesired CNS toxicity. • It should be well tolerated and highly effective against vario ...
... • The primary use of anticonvulsants drugs is in the prevention and control of epileptic seizures. • The ideal antiepileptic drug should completely suppress seizures in doses that do not cause sedation or other undesired CNS toxicity. • It should be well tolerated and highly effective against vario ...
new-ff-Benzodiazepines-
... greater the binding. They are also very effectively distributed to the brain. Compounds without 3-OH group have long half-lives and undergo conversion to the 3-hydroxyl compounds by hepatic oxidation. Compounds with 3-OH (oxazepam, lorazepam) are short-acting because they are rapidly conjugated and ...
... greater the binding. They are also very effectively distributed to the brain. Compounds without 3-OH group have long half-lives and undergo conversion to the 3-hydroxyl compounds by hepatic oxidation. Compounds with 3-OH (oxazepam, lorazepam) are short-acting because they are rapidly conjugated and ...
PatrickChapter2
... Strongest of the intermolecular bonds (20-40 kJ mol-1) Takes place between groups of opposite charge The strength of the ionic interaction is inversely proportional to the distance between the two charged groups Stronger interactions occur in hydrophobic environments The strength of interaction drop ...
... Strongest of the intermolecular bonds (20-40 kJ mol-1) Takes place between groups of opposite charge The strength of the ionic interaction is inversely proportional to the distance between the two charged groups Stronger interactions occur in hydrophobic environments The strength of interaction drop ...
Absorption, distribution, metabolism and excretion
... Lipid solubility: weak acids and weak bases/Clinical Significance, contd. In drug poisoning, renal elimination of drugs can be enhanced by changing urinary pH to increase drug ionization and inhibits tubular reabsorption. Alkalinization of urine by NaHCO3 increases excretion of acidic drugs e.g. ...
... Lipid solubility: weak acids and weak bases/Clinical Significance, contd. In drug poisoning, renal elimination of drugs can be enhanced by changing urinary pH to increase drug ionization and inhibits tubular reabsorption. Alkalinization of urine by NaHCO3 increases excretion of acidic drugs e.g. ...
Key to Problems for Drug Design Courses (II)
... 1. The nature of the pathological target. It’s the site of action, nature of desired action, stability, ease of absorption and distribution, metabolism, dosage form and regimen. 2. See the preface of the textbook. The factors affecting the pharmacokinetic phase are absorption, distribution, metaboli ...
... 1. The nature of the pathological target. It’s the site of action, nature of desired action, stability, ease of absorption and distribution, metabolism, dosage form and regimen. 2. See the preface of the textbook. The factors affecting the pharmacokinetic phase are absorption, distribution, metaboli ...
View/Open - University of Khartoum
... Nepetin and Parthenolide were predicted to have anticancer activities. The activity of Nepetin appeared to be mediated through UCK-2 inhibition. On the other hand, inhibition of MEK-1 and enhancement of TP53 expression were predicted as the anticancer mechanisms of Parthenolide. The three compounds ...
... Nepetin and Parthenolide were predicted to have anticancer activities. The activity of Nepetin appeared to be mediated through UCK-2 inhibition. On the other hand, inhibition of MEK-1 and enhancement of TP53 expression were predicted as the anticancer mechanisms of Parthenolide. The three compounds ...
Pharmacodynamics
... Strongest of the intermolecular bonds (20-40 kJ mol-1) Takes place between groups of opposite charge The strength of the ionic interaction is inversely proportional to the distance between the two charged groups Stronger interactions occur in hydrophobic environments The strength of interaction drop ...
... Strongest of the intermolecular bonds (20-40 kJ mol-1) Takes place between groups of opposite charge The strength of the ionic interaction is inversely proportional to the distance between the two charged groups Stronger interactions occur in hydrophobic environments The strength of interaction drop ...
Chapter 10
... - Nucleotide Analogs can distort shapes of nucleic acid molecules and prevent further replication, transcription, or translation - PABA is coenzyme used in nucleotide synthesis – these drugs compete for enzyme active site - Humans use folic acid as coenyzme so these drugs do not effect our cells ...
... - Nucleotide Analogs can distort shapes of nucleic acid molecules and prevent further replication, transcription, or translation - PABA is coenzyme used in nucleotide synthesis – these drugs compete for enzyme active site - Humans use folic acid as coenyzme so these drugs do not effect our cells ...
主論文の要旨 EML4 promotes the loading of NUDC to the spindle for
... with anti-tubulin and Hoechst. Most of control cells showed organized bipolar spindle and properly alignment chromosomes in metaphase. In contrast, about 60% EML4 depleted cells showed un-congressed chromosomes and disformed spindles (Fig.2A). EML4 depletion significantly reduced the number of metap ...
... with anti-tubulin and Hoechst. Most of control cells showed organized bipolar spindle and properly alignment chromosomes in metaphase. In contrast, about 60% EML4 depleted cells showed un-congressed chromosomes and disformed spindles (Fig.2A). EML4 depletion significantly reduced the number of metap ...
Kinetic and Affinity Analysis using Biacore
... low immobilization capacity and lower surface charge density. • Allows to reduce non specific binding in case of complex mixture such as cell extract or culture medium. • Advantageous for kinetic experiments where low immobilization levels are recommended. ...
... low immobilization capacity and lower surface charge density. • Allows to reduce non specific binding in case of complex mixture such as cell extract or culture medium. • Advantageous for kinetic experiments where low immobilization levels are recommended. ...
Fragment-based Drug Discovery of the Synthetic Small Molecule
... Fragment 1, was identified as having a Kd of 790μM for HSP90 and the experimental binding mode indicated a clear pathway to optimise the molecule After three iterations of structure-guided medicinal chemistry, compound 4 was identified which is just six heavy atoms larger than fragment 1 but is over ...
... Fragment 1, was identified as having a Kd of 790μM for HSP90 and the experimental binding mode indicated a clear pathway to optimise the molecule After three iterations of structure-guided medicinal chemistry, compound 4 was identified which is just six heavy atoms larger than fragment 1 but is over ...
lecture1-GENERAL PHA..
... limited systemic effect less side effects no first pass effect Dosage form: volatile gases e.g. anesthetics aerosol, nebulizer for asthma ...
... limited systemic effect less side effects no first pass effect Dosage form: volatile gases e.g. anesthetics aerosol, nebulizer for asthma ...
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... area of small molecule therapeutic discovery. The goal is to create a comprehensive in silico drug discovery pipeline to increase the odds of initial preclinical hits and leads leading to significantly better outcomes downstream in the clinic. The knowledge-based drug discovery pipeline will adopt a ...
... area of small molecule therapeutic discovery. The goal is to create a comprehensive in silico drug discovery pipeline to increase the odds of initial preclinical hits and leads leading to significantly better outcomes downstream in the clinic. The knowledge-based drug discovery pipeline will adopt a ...
Vaginitis Presentation
... contain cholesterol instead of ergosterol and so they are much less susceptible. (Note: as polyene's hydrophobic chain is reduced, its sterol binding activity is increased. Therefore, increased reduction of the hydrophobic chain may result in it binding to cholesterol, making it toxic to animals.) ...
... contain cholesterol instead of ergosterol and so they are much less susceptible. (Note: as polyene's hydrophobic chain is reduced, its sterol binding activity is increased. Therefore, increased reduction of the hydrophobic chain may result in it binding to cholesterol, making it toxic to animals.) ...