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Mechanism-based Inhibition: Deriving KI and kinact
... The IC50 value is typically defined as concentration of the inhibitor, at which the velocity of product formation is half the velocity without inhibitor (Cheng and Prusoff, 1973). For reversible inhibition, this is identical to the inhibitor concentration that decreases the metabolite concentration ...
... The IC50 value is typically defined as concentration of the inhibitor, at which the velocity of product formation is half the velocity without inhibitor (Cheng and Prusoff, 1973). For reversible inhibition, this is identical to the inhibitor concentration that decreases the metabolite concentration ...
Kitonde et al., Afr J Tradit Complement Altern Med. (2013) 10 (1):000
... accepted p-value≤0.05 (5% error) and therefore it was rejected. (a)Parts of plant used: In this study, mean inhibition zones were used as the results for figures 2, 3 and 4 below. All the organic crude extracts of V. glabra parts used were active on at least one of the four test-organisms used (see ...
... accepted p-value≤0.05 (5% error) and therefore it was rejected. (a)Parts of plant used: In this study, mean inhibition zones were used as the results for figures 2, 3 and 4 below. All the organic crude extracts of V. glabra parts used were active on at least one of the four test-organisms used (see ...
CHAPTER 7 DETERMINATION OF THE ANTIMYCOBACTERIAL ACTIVITY OF THE FRACTIONS AND ISOLATED COMPOUNDS
... alternative preventive-therapy regimens (American Thoraic Society. 1986, Ferebee, ...
... alternative preventive-therapy regimens (American Thoraic Society. 1986, Ferebee, ...
Angiotensin Converting Enzyme Inhibitors and
... animals were different from those of the non-treated controls; however, this difference was not addressed carefully by determining the heart weight/body weight ratio. Myocyte necrosis and calcification were also decreased upon captopril treatment, although the degree of inflammation was unchanged. T ...
... animals were different from those of the non-treated controls; however, this difference was not addressed carefully by determining the heart weight/body weight ratio. Myocyte necrosis and calcification were also decreased upon captopril treatment, although the degree of inflammation was unchanged. T ...
A PRELIMINARY ANTIHYPERGLYCEMIC AND ANTINOCICEPTIVE ACTIVITY EVALUATION OF CAMPANULATUS
... corms of A. campanulatus, has the potential of acting synergistically and producing a strong antihyperglycemic effect, as has been observed in the present study with oral glucose tolerance tests. The presence of lupeol, stigmasterol, and -sitosterol in corms can also explain the observed antinocice ...
... corms of A. campanulatus, has the potential of acting synergistically and producing a strong antihyperglycemic effect, as has been observed in the present study with oral glucose tolerance tests. The presence of lupeol, stigmasterol, and -sitosterol in corms can also explain the observed antinocice ...
Available Online through - International Journal of Pharmacy and
... levels were not affected. Testicular biopsy revealed that spermatogenesis is not affected. Reduction in testosterone levels in circulation may be responsible for the reduced secretary activity of the accessory glands which results in decrease in volume of semen 46. A clinical trial of oral contracep ...
... levels were not affected. Testicular biopsy revealed that spermatogenesis is not affected. Reduction in testosterone levels in circulation may be responsible for the reduced secretary activity of the accessory glands which results in decrease in volume of semen 46. A clinical trial of oral contracep ...
accuracy of biological activity spectra predicting
... Basic elements of PASS include: presentation of biological activity, description of chemical structure, training set of compounds, training procedure, prediction procedure. The current version of PASS differs essentially from the previous11. Biological Activity. Biological activities in PASS are des ...
... Basic elements of PASS include: presentation of biological activity, description of chemical structure, training set of compounds, training procedure, prediction procedure. The current version of PASS differs essentially from the previous11. Biological Activity. Biological activities in PASS are des ...
vitekta - Gilead
... The safety assessment of VITEKTA is primarily based on data from a controlled clinical trial, Study 145, in which 712 HIV-1 infected, antiretroviral treatment-experienced adults received VITEKTA (N=354) or raltegravir (N=358), each administered with a background regimen consisting of a fully active ...
... The safety assessment of VITEKTA is primarily based on data from a controlled clinical trial, Study 145, in which 712 HIV-1 infected, antiretroviral treatment-experienced adults received VITEKTA (N=354) or raltegravir (N=358), each administered with a background regimen consisting of a fully active ...
27 Gastrointestinal drugs
... taking antacids and milk to excess. For example, a man presented with nausea, vomiting, constipation, polyuria and polydipsia, which was diagnosed as milk-alkali syndrome, due to daily treatment with 6 tablets of Caved-S and about 2 litres (3.5 pints) of milk, for dyspepsia related to a peptic ulcer ...
... taking antacids and milk to excess. For example, a man presented with nausea, vomiting, constipation, polyuria and polydipsia, which was diagnosed as milk-alkali syndrome, due to daily treatment with 6 tablets of Caved-S and about 2 litres (3.5 pints) of milk, for dyspepsia related to a peptic ulcer ...
drug interactions with calcium channel blockers: possible
... complex formation experiment) were obtained from Gentest Corp. (Woburn, MA). Microsomes prepared from insect cells with cDNAs of human CYP3A4 and NADPH-dependent reductase coexpressed were prepared and characterized at Merck Research Laboratories (West Point, PA). Assays for P-450 Activities. Assays ...
... complex formation experiment) were obtained from Gentest Corp. (Woburn, MA). Microsomes prepared from insect cells with cDNAs of human CYP3A4 and NADPH-dependent reductase coexpressed were prepared and characterized at Merck Research Laboratories (West Point, PA). Assays for P-450 Activities. Assays ...
Nicotinamide adenine dinucleotide metabolism as an
... Structural comparisons show that Asp219 in NMPRTase may be a determinant of the substrate specificity of this enzyme [46,50]. NMPRTase has high affinity towards the NM substrate, with Km of ∼ 2 µM [13,46-48], but it is inactive towards the NA substrate. The Asp219 side chain is hydrogen-bonded to th ...
... Structural comparisons show that Asp219 in NMPRTase may be a determinant of the substrate specificity of this enzyme [46,50]. NMPRTase has high affinity towards the NM substrate, with Km of ∼ 2 µM [13,46-48], but it is inactive towards the NA substrate. The Asp219 side chain is hydrogen-bonded to th ...
Acetylsalicylic acid Krka gastro
... displacement of oral anticoagulants from their plasma protein binding sites. The bleeding time should be monitored (see section 4.4). Particularly, treatment with acetylsalicylic acid should not be initiated within the first 24 hours after treatment with alteplase in acute stroke patients. Concomita ...
... displacement of oral anticoagulants from their plasma protein binding sites. The bleeding time should be monitored (see section 4.4). Particularly, treatment with acetylsalicylic acid should not be initiated within the first 24 hours after treatment with alteplase in acute stroke patients. Concomita ...
Synthesis and Physicochemical Characterization of Folate
... investigated as targeting molecule for active anticancer drug delivery. Proper synthesis procedures have been pointed out to link folic acid to drug carriers to produce targeting drug delivery systems. In particular, it was demonstrated that the glutamate γ-carboxyl group activation does not provoke ...
... investigated as targeting molecule for active anticancer drug delivery. Proper synthesis procedures have been pointed out to link folic acid to drug carriers to produce targeting drug delivery systems. In particular, it was demonstrated that the glutamate γ-carboxyl group activation does not provoke ...
patrick_ch22_p1
... • The imidazole ring of histamine is not ionised when it interacts with the imidazole binding region • The ionised form of burimamide is unlikely to bind well • Decreasing the basicity and ionisation of the imidazole ring in burimamide closer to that of histamine may increase the binding interaction ...
... • The imidazole ring of histamine is not ionised when it interacts with the imidazole binding region • The ionised form of burimamide is unlikely to bind well • Decreasing the basicity and ionisation of the imidazole ring in burimamide closer to that of histamine may increase the binding interaction ...
N-terminal portion acts as an initiator of the inactivation of pepsin at
... the wild-type. The results of the above three mutants demonstrated that the distribution of the negatively charged residues on the surface of the porcine pepsin helped to stabilize the enzyme, however, the degree of stabilization was not substantial. Since Lin et al. had shown that the initial denat ...
... the wild-type. The results of the above three mutants demonstrated that the distribution of the negatively charged residues on the surface of the porcine pepsin helped to stabilize the enzyme, however, the degree of stabilization was not substantial. Since Lin et al. had shown that the initial denat ...
Protocol(Ascites) - HAL
... ability of a strain to be neutralised by circulating or administrated antibodies [29, 30]. This may also have an impact on viral propagation and therefore represent a component of viral fitness. Several studies have examined the altered antigenicity of common antiviral drug selected mutations that a ...
... ability of a strain to be neutralised by circulating or administrated antibodies [29, 30]. This may also have an impact on viral propagation and therefore represent a component of viral fitness. Several studies have examined the altered antigenicity of common antiviral drug selected mutations that a ...
Hepatitis in HIV/AIDS - Vanderbilt University Medical Center
... • Metabolism: PTV: CYP3A4 major, CYP3A5 minor; RTV: CYP3A4 major, 2D6 minor; OBV: amide hydrolysis • Drug interaction potential: PTV levels may be ↑ or ↓ by drugs that inhibit or induce metabolism. RTV is a potent CYP3A4 inhibitor. OBV and PTV also inhibit UGT1A1. ◦◦ The dose of ritonavir used for ...
... • Metabolism: PTV: CYP3A4 major, CYP3A5 minor; RTV: CYP3A4 major, 2D6 minor; OBV: amide hydrolysis • Drug interaction potential: PTV levels may be ↑ or ↓ by drugs that inhibit or induce metabolism. RTV is a potent CYP3A4 inhibitor. OBV and PTV also inhibit UGT1A1. ◦◦ The dose of ritonavir used for ...
Isolation of antibacterials from the mangrove, Avicennia marina and
... was recorded the maximum at the retention time of 30.94 with 10.7026 % of peak value followed by 2-cyclohexen1-one, 4-hydroxy-3,5,5-trimethyl-4-(3-oxo-1-butenyl) (8.6%), phytol (8.4 %), hexadecanoic acid, ethyl ester (6.2 %) and 3,7,11,15-tetramethyl-2-hexadecen-1-ol (4.9 %) at the retention time of ...
... was recorded the maximum at the retention time of 30.94 with 10.7026 % of peak value followed by 2-cyclohexen1-one, 4-hydroxy-3,5,5-trimethyl-4-(3-oxo-1-butenyl) (8.6%), phytol (8.4 %), hexadecanoic acid, ethyl ester (6.2 %) and 3,7,11,15-tetramethyl-2-hexadecen-1-ol (4.9 %) at the retention time of ...
General Outline for Antibiotics (a good study guide)
... A. sulfonamide – generic term for derivatives of para-aminobenzenesulfonamide B. analogues of para-aminobenzoic acid C. sodium salts are water soluble II. Effect on Microbes A. spectrum of coverage – broad (both G+ and G-) B. mechanism of action 1. competitive inhibitors of dihydropteroate synthase ...
... A. sulfonamide – generic term for derivatives of para-aminobenzenesulfonamide B. analogues of para-aminobenzoic acid C. sodium salts are water soluble II. Effect on Microbes A. spectrum of coverage – broad (both G+ and G-) B. mechanism of action 1. competitive inhibitors of dihydropteroate synthase ...
Cyclooxygenase-2 (COX-2) Inhibitors
... ankylosing spondylitis may be chronically administered based on patient need. 3) Celecoxib safety and efficacy in pediatric patients 2 years of age and older with JRA for greater than a six-month treatment duration have not been established. Patient profiles containing prescriptions for JRA for grea ...
... ankylosing spondylitis may be chronically administered based on patient need. 3) Celecoxib safety and efficacy in pediatric patients 2 years of age and older with JRA for greater than a six-month treatment duration have not been established. Patient profiles containing prescriptions for JRA for grea ...
ANALGESIC AND ANTHELMINTIC ACTIVITY OF VARIOUS EXTRACTS OF ANDROGRAPHIS Research Article
... the extracts of Andrographispaniculata (N). Some of these phytoconstituents may be responsible to show a potent analgesic and anthelmintic activity. The results of the present study confirm the analgesic activity of 95% ethanolic and ether extract of Andrographispaniculata(N) bark. The tail-flick an ...
... the extracts of Andrographispaniculata (N). Some of these phytoconstituents may be responsible to show a potent analgesic and anthelmintic activity. The results of the present study confirm the analgesic activity of 95% ethanolic and ether extract of Andrographispaniculata(N) bark. The tail-flick an ...
Viral Infections - University of Kentucky
... immune system for recovery from viral infections. • If immunity does not recover. – Mortality is increased – Response to therapy is usually delayed. – Risk of selecting resistant viruses may be higher in such patients. • Mutations within the viral genome • Usually detected only by a lack of clinical ...
... immune system for recovery from viral infections. • If immunity does not recover. – Mortality is increased – Response to therapy is usually delayed. – Risk of selecting resistant viruses may be higher in such patients. • Mutations within the viral genome • Usually detected only by a lack of clinical ...
IOSR Journal of Agriculture and Veterinary Science (IOSR-JAVS)
... appreciable antitrypanosomal activity compared to the standard drug, berenil, since it was able to prolong the lifespan of the test animals beyond that of the untreated control by 24 days. This observation is similar to that of [9] who reported strong activity of methanolic extracts of Solanum schim ...
... appreciable antitrypanosomal activity compared to the standard drug, berenil, since it was able to prolong the lifespan of the test animals beyond that of the untreated control by 24 days. This observation is similar to that of [9] who reported strong activity of methanolic extracts of Solanum schim ...
DESIGNING AND COMPUTATIONAL STUDY OF SOME NOVEL LAMIVUDINE ANALOGUES AS
... Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV infection. When HIV infects a cell, reverse transcriptase copies the viral single stranded RNA genome into a double-stranded viral DNA. The viral DNA is then integrated into the host chromosomal DNA, which t ...
... Reverse-transcriptase inhibitors (RTIs) are a class of antiretroviral drug used to treat HIV infection. When HIV infects a cell, reverse transcriptase copies the viral single stranded RNA genome into a double-stranded viral DNA. The viral DNA is then integrated into the host chromosomal DNA, which t ...
TAS-116, a Highly Selective Inhibitor of Heat Shock
... To establish an orthotopic lung tumor model, NCI-H1975 was engineered to stably express luciferase (H1975-Luc) by using a lentiviral vector (Life Technologies Corp.). H1975-Luc cells (1 106 cells/mouse) were mixed with Matrigel (BD Biosciences) and directly transplanted into the left lobe of the e ...
... To establish an orthotopic lung tumor model, NCI-H1975 was engineered to stably express luciferase (H1975-Luc) by using a lentiviral vector (Life Technologies Corp.). H1975-Luc cells (1 106 cells/mouse) were mixed with Matrigel (BD Biosciences) and directly transplanted into the left lobe of the e ...