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Zebrafish as tools for drug discovery
... For example, a recent analysis of first‑in‑class drugs approved between 1999 and 2008 revealed that 62% were discovered by phenotype-based screens, despite the fact that such screens represented only a small subset of the overall total1. Several factors may explain the apparent superiority of phenot ...
... For example, a recent analysis of first‑in‑class drugs approved between 1999 and 2008 revealed that 62% were discovered by phenotype-based screens, despite the fact that such screens represented only a small subset of the overall total1. Several factors may explain the apparent superiority of phenot ...
Advances in and applications of proteasome inhibitors
... proteasome inhibitor salinosporamide A revealed an associated b-subunit that may be involved with resistance [32]. It will be intriguing to learn if other biosynthetic gene clusters associated with actinomycete proteasome inhibitors also harbor proteasome b-subunits, and if so, whether this genetic ...
... proteasome inhibitor salinosporamide A revealed an associated b-subunit that may be involved with resistance [32]. It will be intriguing to learn if other biosynthetic gene clusters associated with actinomycete proteasome inhibitors also harbor proteasome b-subunits, and if so, whether this genetic ...
In silico methods in prediction of drug metabolism, mass
... metabolizing reactions transform lipophilic compounds to more hydrophilic form and facilitate their excretion from the body. The reactions are divided into phase I and phase II reactions [5]. Phase I reactions (functionalization reactions), such as oxidation, hydrolysis and reduction, produce or unc ...
... metabolizing reactions transform lipophilic compounds to more hydrophilic form and facilitate their excretion from the body. The reactions are divided into phase I and phase II reactions [5]. Phase I reactions (functionalization reactions), such as oxidation, hydrolysis and reduction, produce or unc ...
Product Monograph for Triumeq
... and share some common features such as fever and/or rash with other symptoms indicating multi-organ involvement (see Clinical Description of HSRs). Clinically it is not possible to determine whether a HSR with TRIUMEQ™ would be caused by abacavir or dolutegravir. Hypersensitivity reactions have been ...
... and share some common features such as fever and/or rash with other symptoms indicating multi-organ involvement (see Clinical Description of HSRs). Clinically it is not possible to determine whether a HSR with TRIUMEQ™ would be caused by abacavir or dolutegravir. Hypersensitivity reactions have been ...
PPT - IAS-USA
... • TAF is virologically as effective as TDF. • Compared with TDF, TAF has more favorable effects on renal and bone markers. − Particularly important in patients who already have renal or bone disease or who are at high risk of these complications. ...
... • TAF is virologically as effective as TDF. • Compared with TDF, TAF has more favorable effects on renal and bone markers. − Particularly important in patients who already have renal or bone disease or who are at high risk of these complications. ...
pKa Prediction of Monoprotic Small Molecules the SMARTS Way
... the Hammett equation. LFER models are still commonly used and are also implemented in popular commercially available software packages, such as SPARC.17-19 One of the most common techniques used in pKa prediction is quantitative structure activity/property relationships (QSAR/QSPR) deriving their fi ...
... the Hammett equation. LFER models are still commonly used and are also implemented in popular commercially available software packages, such as SPARC.17-19 One of the most common techniques used in pKa prediction is quantitative structure activity/property relationships (QSAR/QSPR) deriving their fi ...
Antiparasitic Chemotherapy for Human and Veterinary Use 3rd
... Successful vacuolar pathogens have developed sophisticated strategies to hijack the endomembrane system of host cells and evade antimicrobial responses. The protozoan parasite Leishmania, the causative agent of leishmaniases in humans, is particularly adept at transforming the macrophage into a hosp ...
... Successful vacuolar pathogens have developed sophisticated strategies to hijack the endomembrane system of host cells and evade antimicrobial responses. The protozoan parasite Leishmania, the causative agent of leishmaniases in humans, is particularly adept at transforming the macrophage into a hosp ...
Antimicrobial Pharmacokinetics and Pharmacodynamics
... drug potency in vitro such as the MIC or minimum bactericidal concentration (MBC) of an antimicrobial agent for important pathogens and the pharmacokinetics of the drug in serum. These parameters do not provide information regarding the time course activity of drugs, however. For example, the MIC do ...
... drug potency in vitro such as the MIC or minimum bactericidal concentration (MBC) of an antimicrobial agent for important pathogens and the pharmacokinetics of the drug in serum. These parameters do not provide information regarding the time course activity of drugs, however. For example, the MIC do ...
An Introduction to Medicinal Chemistry
... There can be little doubt that alcohol is a drug and as such causes society more problems than all other drugs put together. One only has to study road accident statistics to appreciate that fact. It has been stated that if alcohol was discovered today, it would be restricted in exactly the same way ...
... There can be little doubt that alcohol is a drug and as such causes society more problems than all other drugs put together. One only has to study road accident statistics to appreciate that fact. It has been stated that if alcohol was discovered today, it would be restricted in exactly the same way ...
Uses
... mixtures of cyclic peptides some with uncommon amino acids and some with common amino acids but with the D absolute stereochemistry. These cyclic substances often have a pendant fatty acid chain. Mode of action: (Disruption of bacterial membrane function) These drugs are usually water soluble and ar ...
... mixtures of cyclic peptides some with uncommon amino acids and some with common amino acids but with the D absolute stereochemistry. These cyclic substances often have a pendant fatty acid chain. Mode of action: (Disruption of bacterial membrane function) These drugs are usually water soluble and ar ...
ABSTRACT Title of Thesis: SOURCES AND OCCURRENCE OF
... Fleming (81), but he was unable to isolate and purify enough drug to be of any use. By 1941, Ernst Chain, Howard Florey, and Norman Heatley had shown the therapeutic value of penicillin (49), but they were also unable to produce enough penicillin for commercial use. Collaboration with Andrew Moyer ...
... Fleming (81), but he was unable to isolate and purify enough drug to be of any use. By 1941, Ernst Chain, Howard Florey, and Norman Heatley had shown the therapeutic value of penicillin (49), but they were also unable to produce enough penicillin for commercial use. Collaboration with Andrew Moyer ...
the aminoglycosides - University of Illinois College of Veterinary
... RESISTANCE DEVELOPMENT Resistance of primary clinical importance is due to plasmid-controlled enzymes in the periplasmic space of gram-negative bacteria. Several of these enzymes are known, with varying specificity across the aminoglycoside antimicrobials. Other mechanisms of resistance include decr ...
... RESISTANCE DEVELOPMENT Resistance of primary clinical importance is due to plasmid-controlled enzymes in the periplasmic space of gram-negative bacteria. Several of these enzymes are known, with varying specificity across the aminoglycoside antimicrobials. Other mechanisms of resistance include decr ...
Full-Text PDF
... thrombin in the coagulation cascade. Selective inhibition of FXa was unable to affect the pre-existing thrombin level, and activation and aggregation of the platelets reduced the risk of bleeding when compared with traditional anti-coagulants [2]. In addition, FXa plays a vital role in amplifying th ...
... thrombin in the coagulation cascade. Selective inhibition of FXa was unable to affect the pre-existing thrombin level, and activation and aggregation of the platelets reduced the risk of bleeding when compared with traditional anti-coagulants [2]. In addition, FXa plays a vital role in amplifying th ...
auspar-rilpivirine-1.. - Therapeutic Goods Administration (TGA)
... Although resistance to rilpivirine was largely associated with more than one, and usually more than two, NNRTI RAMs, the combination of specific RAMs appears to be more indicative of resistance to rilpivirine in vitro rather than their total number. Analysis of the double HIV-1/HXB2 site directed mu ...
... Although resistance to rilpivirine was largely associated with more than one, and usually more than two, NNRTI RAMs, the combination of specific RAMs appears to be more indicative of resistance to rilpivirine in vitro rather than their total number. Analysis of the double HIV-1/HXB2 site directed mu ...
Characterization of Two Pharmacophores on the Multidrug
... the reaction medium of an ADP pulse). The compounds were added to the reaction medium from stock solutions prepared either in DMSO (for VRP, VBL, BCT, PIA, PIIA, and cLF) or ethanol (for PRG, CSA, ACD, and TTX), or from 1:100 dilutions in distilled water. The solvent alone, the concentration of whic ...
... the reaction medium of an ADP pulse). The compounds were added to the reaction medium from stock solutions prepared either in DMSO (for VRP, VBL, BCT, PIA, PIIA, and cLF) or ethanol (for PRG, CSA, ACD, and TTX), or from 1:100 dilutions in distilled water. The solvent alone, the concentration of whic ...
Blind copy - Open Journal Systems
... convenient to support the conclusions on additional techniques. The compatibility study between efavirenz and excipients, some of them already reported using only DSC as well with other excipients that have not been reported, was conducted. Efavirenz is a nonnucleoside reverse transcriptase inhibito ...
... convenient to support the conclusions on additional techniques. The compatibility study between efavirenz and excipients, some of them already reported using only DSC as well with other excipients that have not been reported, was conducted. Efavirenz is a nonnucleoside reverse transcriptase inhibito ...
ARNOLD & I? ORTER May 12, 1998
... At a very minimum, we suggest that approval of any novel mixture of estrogens should require the submission of safety information in accordance with well-recognized FDA and other regulatory requirements. To our knowledge, such studies have not been performed with most of the individual estrogens in ...
... At a very minimum, we suggest that approval of any novel mixture of estrogens should require the submission of safety information in accordance with well-recognized FDA and other regulatory requirements. To our knowledge, such studies have not been performed with most of the individual estrogens in ...
The challenge of selecting protein kinase assays
... study by Beasley et al. [11], many strong inhibitors generated from the FP-based assay were shown as weak inhibitors in the TRF and TR-FRET assays. The authors suggest that a few situations could cause the observed high mP values. The first was the low concentration of phosphorylated substrate and h ...
... study by Beasley et al. [11], many strong inhibitors generated from the FP-based assay were shown as weak inhibitors in the TRF and TR-FRET assays. The authors suggest that a few situations could cause the observed high mP values. The first was the low concentration of phosphorylated substrate and h ...
Binding of Imipramine to Phospholipid Bilayers Using
... those in the bulk solution (Cevc 1990; Miyazaki et al. 1992). The thermodynamic factors giving rise to shifts in pK also cause a difference in partitioning between the protonated and unprotonated forms of the amphiphile. Analysis of binding isotherms Analysis of binding isotherms of IMI follows the ...
... those in the bulk solution (Cevc 1990; Miyazaki et al. 1992). The thermodynamic factors giving rise to shifts in pK also cause a difference in partitioning between the protonated and unprotonated forms of the amphiphile. Analysis of binding isotherms Analysis of binding isotherms of IMI follows the ...
Zebrafish: A Complete Animal Model for In Vivo Drug Discovery and
... Screening of drug in zebrafish that have been carried out so far have demonstrated that it is feasible to screen libraries of compounds with specific biological activities. The zebrafish is an outstanding vertebrate system for developing in vivo disease-related assays that can be useful for high vol ...
... Screening of drug in zebrafish that have been carried out so far have demonstrated that it is feasible to screen libraries of compounds with specific biological activities. The zebrafish is an outstanding vertebrate system for developing in vivo disease-related assays that can be useful for high vol ...
7 Antifungal therapy c h a P t e r
... effective in the treatment of infections caused by Candida albicans and Cryptococcus neoformans; however, the development of 5FC resistance soon limited its use as monotherapy. Nonetheless, 5FC is still used in combination with AmB in the treatment of cryptococcal meningitis.1 Miconazole and clotrim ...
... effective in the treatment of infections caused by Candida albicans and Cryptococcus neoformans; however, the development of 5FC resistance soon limited its use as monotherapy. Nonetheless, 5FC is still used in combination with AmB in the treatment of cryptococcal meningitis.1 Miconazole and clotrim ...
Extract from the Clinical Evaluation Report for tenofovir disoproxil
... This is a Category 1 submission to register Truvada for a pre-exposure prophylaxis indication (PrEP) and to make editorial changes to the current indication. Truvada is a fixed dose combination tablet containing tenofovir disoproxil fumarate 300 mg and emtricitabine 200 mg. Tenofovir disoproxil fuma ...
... This is a Category 1 submission to register Truvada for a pre-exposure prophylaxis indication (PrEP) and to make editorial changes to the current indication. Truvada is a fixed dose combination tablet containing tenofovir disoproxil fumarate 300 mg and emtricitabine 200 mg. Tenofovir disoproxil fuma ...
Activity and Enzyme Kinetics of Human UDP
... Human UDP-glucuronosyltransferases (UGTs) are important in the metabolic elimination of xenobiotics and endogenous compounds from the body. These enzymes transfer glucuronic acid moiety from the cosubstrate, UDP-glucuronic acid (UDPGA), to nucleophilic groups of small organic molecules, such as hydr ...
... Human UDP-glucuronosyltransferases (UGTs) are important in the metabolic elimination of xenobiotics and endogenous compounds from the body. These enzymes transfer glucuronic acid moiety from the cosubstrate, UDP-glucuronic acid (UDPGA), to nucleophilic groups of small organic molecules, such as hydr ...
week5
... 2. Repeat the above study for ShK-K-amide (an analogue with improved selectivity) to rationalize the experimental results. ...
... 2. Repeat the above study for ShK-K-amide (an analogue with improved selectivity) to rationalize the experimental results. ...
260-670-1
... days. A 2 mg/kg NVP dose at 48 - 72 h keeps NVP >0.1 mg/l for a week in most infants (0.11 - 0.28 mg/l in 7-day-old infants). A study evaluating chronic NVP (4 mg/kg from birth to 14 days, then 8 mg/kg until 24 weeks) for breastfeeding infants found NVP >0.1 mg/l in 95% and 100% of those receiving t ...
... days. A 2 mg/kg NVP dose at 48 - 72 h keeps NVP >0.1 mg/l for a week in most infants (0.11 - 0.28 mg/l in 7-day-old infants). A study evaluating chronic NVP (4 mg/kg from birth to 14 days, then 8 mg/kg until 24 weeks) for breastfeeding infants found NVP >0.1 mg/l in 95% and 100% of those receiving t ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
![](https://en.wikipedia.org/wiki/Special:FilePath/RTenzyme-hand.jpg?width=300)
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).