Document
... The world's first pharmacogenomic microarray designed for clinical applications that provides comprehensive coverage of gene variations – including deletions and duplications – for the 2D6 and 2C19 genes, which play a role in the metabolism of about 25% of all prescription drugs. It is intended to b ...
... The world's first pharmacogenomic microarray designed for clinical applications that provides comprehensive coverage of gene variations – including deletions and duplications – for the 2D6 and 2C19 genes, which play a role in the metabolism of about 25% of all prescription drugs. It is intended to b ...
Structure-based drug design - Biomolecular Structure Center
... rate of structure determinations has doubled in the last two years, and this rate is still increasing [9]. The large number of structural investigations on medically relevant proteins reflects the general recognition that the structure of a potential drug target is very precious knowledge for a phar ...
... rate of structure determinations has doubled in the last two years, and this rate is still increasing [9]. The large number of structural investigations on medically relevant proteins reflects the general recognition that the structure of a potential drug target is very precious knowledge for a phar ...
Efficacy of Antiviral Drugs against Feline Immunodeficiency Virus
... require intracellular activation for inhibition of the enzyme [8,42]. NNRTIs are a group of structurally diverse compounds that all bind a single site of the RT [55]. The interaction with the allosteric site which is located in close proximity to the catalytic site, leads to a number of conformation ...
... require intracellular activation for inhibition of the enzyme [8,42]. NNRTIs are a group of structurally diverse compounds that all bind a single site of the RT [55]. The interaction with the allosteric site which is located in close proximity to the catalytic site, leads to a number of conformation ...
The Bacterial Heterotrimeric Amidotransferase GatCAB
... For H. pylori, a unique GatCAB catalyzes the conversion of both Asp-tRNAAsn and Glu-tRNAGln into Asn-tRNAAsn and Gln-tRNAGln, respectively, but there are two distinct transamidosomes. In the H. pylori Asn-transamidosome, a speci ic protein named as Hp0100 is required for the transamidosome formation ...
... For H. pylori, a unique GatCAB catalyzes the conversion of both Asp-tRNAAsn and Glu-tRNAGln into Asn-tRNAAsn and Gln-tRNAGln, respectively, but there are two distinct transamidosomes. In the H. pylori Asn-transamidosome, a speci ic protein named as Hp0100 is required for the transamidosome formation ...
Structure and mechanism of action of a novel
... (Chander et al., 1998). These latter organisms include members of Staphylococcus and Streptococcus species, some of which are important human pathogens. Consequently, it is possible that iPGMs could be a target for rational design of a novel antibiotic. Interestingly, some bacteria have genes for bo ...
... (Chander et al., 1998). These latter organisms include members of Staphylococcus and Streptococcus species, some of which are important human pathogens. Consequently, it is possible that iPGMs could be a target for rational design of a novel antibiotic. Interestingly, some bacteria have genes for bo ...
obeticholic acid
... • ≥ 18 YO diagnosed with PBC • Alkaline phosphatase level ≥1.67x UL, or • Abnormal total bilirubin < 2 times UL Nevens, F. et al. NEJM. 2016;375(7):631-43. ...
... • ≥ 18 YO diagnosed with PBC • Alkaline phosphatase level ≥1.67x UL, or • Abnormal total bilirubin < 2 times UL Nevens, F. et al. NEJM. 2016;375(7):631-43. ...
Drug Utilisation Study Of Proton Pumps Inhibitors
... judicious use of PPIs. Methodology: A retrospective cross-sectional study was conducted at the S.S Institute of Medical Science and Research, Davangere. Patient medical records with of PPIs prescription were analysed for drugs used including name of the drug, dosage schedule, duration of treatment a ...
... judicious use of PPIs. Methodology: A retrospective cross-sectional study was conducted at the S.S Institute of Medical Science and Research, Davangere. Patient medical records with of PPIs prescription were analysed for drugs used including name of the drug, dosage schedule, duration of treatment a ...
Twenty-Six Years of Anti-HIV Drug Discovery
... compound in the phosphonamidate form (13, Figure 6) to improve oral bioavailability and cellular uptake. The Gilead group has also studied the metabolism of this prodrug and identified cathepsin A as the major hydrolyzing enzyme.57 Hence, inside the cell 13 is rapidly hydrolyzed to 12, which is then ...
... compound in the phosphonamidate form (13, Figure 6) to improve oral bioavailability and cellular uptake. The Gilead group has also studied the metabolism of this prodrug and identified cathepsin A as the major hydrolyzing enzyme.57 Hence, inside the cell 13 is rapidly hydrolyzed to 12, which is then ...
Powerpoint
... • M.tuberculosis Enoyl-acyl carrier protein reductase ENR (InhA) discovered as potential new drug target • ENR is the primary target of many existing anti-TB drugs but all are very toxic • ENR catalyses the final, rate-determining step in the fatty acid elongation cycle • Alignment of the COMT and E ...
... • M.tuberculosis Enoyl-acyl carrier protein reductase ENR (InhA) discovered as potential new drug target • ENR is the primary target of many existing anti-TB drugs but all are very toxic • ENR catalyses the final, rate-determining step in the fatty acid elongation cycle • Alignment of the COMT and E ...
A conformationally restricted uniconazole analogue as a specific
... gibberellin (GA). However, UNI also inhibits brassinosteroid (BR) biosynthesis4,5 and alters the level of other plant hormones, such as auxins, cytokinins, ethylene and abscisic acid (ABA).6 In particular, UNI strongly inhibits ABA 8'-hydroxylase (CYP707A), a key enzyme in ABA catabolism (Figure 1). ...
... gibberellin (GA). However, UNI also inhibits brassinosteroid (BR) biosynthesis4,5 and alters the level of other plant hormones, such as auxins, cytokinins, ethylene and abscisic acid (ABA).6 In particular, UNI strongly inhibits ABA 8'-hydroxylase (CYP707A), a key enzyme in ABA catabolism (Figure 1). ...
Chemical Genetics: Where Genetics and Pharmacology
... control sensitivity to a wide range of small molecule inhibitors (Bishop et al., 2000b). This gatekeeper residue is conserved as a large hydrophobic amino acid among protein kinases, but mutation of the gatekeeper to alanine or glycine creates a novel pocket that can be uniquely accessed by an inhib ...
... control sensitivity to a wide range of small molecule inhibitors (Bishop et al., 2000b). This gatekeeper residue is conserved as a large hydrophobic amino acid among protein kinases, but mutation of the gatekeeper to alanine or glycine creates a novel pocket that can be uniquely accessed by an inhib ...
Acid Peptic Disease : Therapeutic Concepts
... • Most IV PPI data is based on trials using IV OMEPRAZOLE which is not available in the US • Most studies involved bleeding ulcers requiring endoscopic therapeutic interventions (injection therapy or heater probe) ...
... • Most IV PPI data is based on trials using IV OMEPRAZOLE which is not available in the US • Most studies involved bleeding ulcers requiring endoscopic therapeutic interventions (injection therapy or heater probe) ...
Slajd 1 - Zakład Farmakologii Klinicznej w Poznaniu
... - in adults unable to tolerate or with a contraindication to the use of beta-blockers - or in combination with beta-blockers in pts inadequately controlled with an optimal betablocker dose and whose rate is > 60 bpm Treatment of chronic heart failure ...
... - in adults unable to tolerate or with a contraindication to the use of beta-blockers - or in combination with beta-blockers in pts inadequately controlled with an optimal betablocker dose and whose rate is > 60 bpm Treatment of chronic heart failure ...
Combination Therapy of HIV Infection
... different reverse transcriptase regions (codons 98 to 108 and 179 to 190). None of the mutations overlaps with mutations conferring resistance to NRTIs (Figure 3B). However, some of the mutations cause broad cross-resistance among all members of the NNRTI drug class (eg, K103N) (11). ...
... different reverse transcriptase regions (codons 98 to 108 and 179 to 190). None of the mutations overlaps with mutations conferring resistance to NRTIs (Figure 3B). However, some of the mutations cause broad cross-resistance among all members of the NNRTI drug class (eg, K103N) (11). ...
Effects of Monotherapy and Combination Therapy with Inhibitors of
... from combination therapy with ACE inhibitors and ARBs is not certain. First, the available studies did not assess safety well, a finding that is consistent with a recent systematic review. Limitations include lack of systematic assessment methods and inadequate reporting. Second, although ARBs and A ...
... from combination therapy with ACE inhibitors and ARBs is not certain. First, the available studies did not assess safety well, a finding that is consistent with a recent systematic review. Limitations include lack of systematic assessment methods and inadequate reporting. Second, although ARBs and A ...
Site-directed mutagenesis of key amino acids in the active site of
... conditions. The initial activity increased 25 and 6 times for H187Q and H392N, respectively, when the glycogen concentration was increased from 0.1 to 30 g/L, while about a 33-fold increase was observed for the wild-type enzyme (Tab. 1). These two His interact by hydrogen bonding with the glucosyl r ...
... conditions. The initial activity increased 25 and 6 times for H187Q and H392N, respectively, when the glycogen concentration was increased from 0.1 to 30 g/L, while about a 33-fold increase was observed for the wild-type enzyme (Tab. 1). These two His interact by hydrogen bonding with the glucosyl r ...
- ISpatula
... From sesquiterpenes we will continue to our next group of the terpenoids substances. We talked about 10C "monoterpenes" , 15C "sesquiterpenes" , and now we'll talk about 20C "Diterpenes" substances. We know that the aliphatic compound is the first compound in the biosynthesis of any subclass of the ...
... From sesquiterpenes we will continue to our next group of the terpenoids substances. We talked about 10C "monoterpenes" , 15C "sesquiterpenes" , and now we'll talk about 20C "Diterpenes" substances. We know that the aliphatic compound is the first compound in the biosynthesis of any subclass of the ...
Factors affecting drug metabolism
... Examples: fluoroquinolones, cimetidine, azoles antifungal ...
... Examples: fluoroquinolones, cimetidine, azoles antifungal ...
AEROSOLIZED ANTI-INFECTIVE AGENTS
... TOBI should be stored at refrigerated temperatures of 2-8°C (36-46°F). After removing from refrigeration, or if refrigeration is not available, the pouches in which the drug is provided can be stored at room temperature less than 25°C (77°F) for up to 28 days. Drug ampoules should not be exposed to ...
... TOBI should be stored at refrigerated temperatures of 2-8°C (36-46°F). After removing from refrigeration, or if refrigeration is not available, the pouches in which the drug is provided can be stored at room temperature less than 25°C (77°F) for up to 28 days. Drug ampoules should not be exposed to ...
10.4 Factors That Affect Enzyme Activity, Continued
... 10.1 Enzymes and Their Substrates, Continued There are two enzyme–substrate models: 1. In the Lock-and-key model, the active site is thought to be a rigid, inflexible shape that is an exact complement to the shape of the substrate. The substrate fits in the active site much like a key fits in a loc ...
... 10.1 Enzymes and Their Substrates, Continued There are two enzyme–substrate models: 1. In the Lock-and-key model, the active site is thought to be a rigid, inflexible shape that is an exact complement to the shape of the substrate. The substrate fits in the active site much like a key fits in a loc ...
Efforts to Support the Development of Fusidic Acid in the United States
... protein binding of FA (up to 97%) was thought to limit free drug availability in infected tissues [15, 27]. FA was also known to be metabolized and excreted by the liver and to inhibit CYP3A4, suggesting possible drug interaction issues [16]. Cempra scientists examined published reports [28] indicat ...
... protein binding of FA (up to 97%) was thought to limit free drug availability in infected tissues [15, 27]. FA was also known to be metabolized and excreted by the liver and to inhibit CYP3A4, suggesting possible drug interaction issues [16]. Cempra scientists examined published reports [28] indicat ...
Competitive advantage
... • An enzyme involved in the process of bone destruction. • By inhibiting cathepsin K, the bone destruction process is reduced. ...
... • An enzyme involved in the process of bone destruction. • By inhibiting cathepsin K, the bone destruction process is reduced. ...
Tuberculosis - ichapps.com
... mycobacterium, with a MIC against M. tuberculosis of 0.01 to 0.25 mcg/mL. Most nontuberculous mycobacterium such as M. avium is resistant to Isoniazid. Isoniazid is readily absorbed from the GI tract and from intramuscular injection sites. Isoniazid should be given on an empty stomach whenever poss ...
... mycobacterium, with a MIC against M. tuberculosis of 0.01 to 0.25 mcg/mL. Most nontuberculous mycobacterium such as M. avium is resistant to Isoniazid. Isoniazid is readily absorbed from the GI tract and from intramuscular injection sites. Isoniazid should be given on an empty stomach whenever poss ...
iPPI small molecule inhibitor of Protein
... orally available are known at this time) or can be allosteric inhibitors, thereby binding at, near or far away from the interface in cavities with recognition characteristics that could be highly similar to enzyme active sites. It would seem logical to explore and attempt to rationalize the propert ...
... orally available are known at this time) or can be allosteric inhibitors, thereby binding at, near or far away from the interface in cavities with recognition characteristics that could be highly similar to enzyme active sites. It would seem logical to explore and attempt to rationalize the propert ...
Cardiovascular drugs: some important interaction
... • When ACE inhibitors are chronically used for heart failure, postinfarct protection and highhigh-risk prevention, they are still beneficial when aspirin is added • Aspirin did reduce but not eliminate the ACE inhibitor’s beneficial effect on major clinical events: o A practical policy is to keep th ...
... • When ACE inhibitors are chronically used for heart failure, postinfarct protection and highhigh-risk prevention, they are still beneficial when aspirin is added • Aspirin did reduce but not eliminate the ACE inhibitor’s beneficial effect on major clinical events: o A practical policy is to keep th ...