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Drug Resistance
Drug Resistance

... – most are 6-aminopenicillanic acid derivatives and differ in side chain attached to amino group – most crucial feature of molecule is the blactam ring • essential for bioactivity • many penicillin resistant organisms produce blactamase (penicillinase) which hydrolyzes a bond in this ring ...
Figure 2 - Essays in Biochemistry
Figure 2 - Essays in Biochemistry

... β-lactam alternative to penicillin. Methicillin and the penicillins that followed (oxacillin, nafcillin, cloxacillin and dicloxacillin) were designed with bulky side groups so that they would not fit in the active site of the β-lactamase and hence could not be inactivated by these enzymes (Figure 1) ...
Measurement of Antiviral Activities Using Recombinant Human
Measurement of Antiviral Activities Using Recombinant Human

... immune dysfunction such as organ transplantation or acquired immunodeficiency syndrome (AIDS), reactivation of HCMV may occur and this often causes severe clinical consequences with high morbidity and mortality (7). When a fetus is infected, HCMV may cause severe, generalized symptoms of cytomegalic ...
Hepatitis in HIV/AIDS - Vanderbilt University Medical Center
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 ...
particles for plasmid DNA delivery
particles for plasmid DNA delivery

... including plasmid DNA (pDNA). Here, we survey current approaches to PLGA particle preparation for pDNA delivery and discuss recent progress on optimizing formulation development. ß 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci ...
Structure-Guided Discovery of (S)-3
Structure-Guided Discovery of (S)-3

... Trigonal Planar ...
Promega`s P450-GloTM Luminescent Cytochrome
Promega`s P450-GloTM Luminescent Cytochrome

... A large group of enzymes known as cytochromes P450 (CYP or P450) are responsible for the oxidative metabolism of many xenobiotic, hydrophobic chemicals, which include most therapeutic drugs1. P450 metabolism can influence the clearance rate of drugs, their toxicity, and their interactions with other ...
Chemical combination effects predict connectivity in biological systems
Chemical combination effects predict connectivity in biological systems

... pairs by varying one or more of the many kinetic parameters in the pathway model. We approached the problem by focusing not just on the presence or absence of synergy relative to some reference level, but by using a set of shape models to characterize the morphology of full response surfaces. Here w ...
Grand Canonical Monte Carlo Simulation of Ligand−Protein Binding
Grand Canonical Monte Carlo Simulation of Ligand−Protein Binding

... and relative energies of water bound to DNA, showing that the water is more tightly bound to the minor groove than the major groove. The current report describes the basic methodology for the computation of gas-phase binding affinities and demonstrates the ability of this approach to identify high-a ...
- Madhya Pradesh Bhoj Open University
- Madhya Pradesh Bhoj Open University

... specific new molecules that can lead more efficiently to useful drug discovery. Not only did the rapid development of organic & medicinal chemistry make it possible to determine the structure of natural drugs. New drug discovery may be considered broadly in terms of two kinds of investigational acti ...
Interactive Association of Drugs Binding to Human
Interactive Association of Drugs Binding to Human

... presence of three domains, namely domains I (residues 1–195), II (196–383) and III (384–585), which, as predicted from amino acid sequence comparison, are not only topologically identical, but they also have similar three-dimensional structures [14,40]. The three domains are further divided into sub ...
SW_QA226_1_Noacs_Complementary_Medicines_Final
SW_QA226_1_Noacs_Complementary_Medicines_Final

... One in vitro study indicated that saw palmetto showed potent inhibition of the activities of CYP3A4, CYP2D6 and CYP2C9 suggesting the potential for drug interactions. However studies in humans did not find any significant effects on CYP1A2, CYP2D6, CYP2E1 and CYP3A4 activity [1]. Saw palmetto has be ...
DH 250 - Cypress College
DH 250 - Cypress College

... frequent, short term oral corticosteroid treatment bursts in the past 12 months regular use of high dose inhaled corticosteroids in the past 12 months regular use of injected long acting corticosteroids daily use of oral corticosteroids alternate-day oral corticosteroids prolonged use of oral cortic ...
27 Gastrointestinal drugs
27 Gastrointestinal drugs

... and therefore inhibits the metabolism of many drugs, increasing their plasma levels and/or bioavailability. These interactions are most likely to be clinically significant for drugs with a narrow therapeutic index. Famotidine, nizatidine and ranitidine do not inhibit cytochrome P450 to a clinically ...
Bacterial Growth Kinetics of "M. lufu" in the Presence and Absence
Bacterial Growth Kinetics of "M. lufu" in the Presence and Absence

... observation in Figs. 1-4. In contrast to the results presented in Figs. 1-2 for INH, PTH, and also DDS, where the new steady state growth rates obtained after drug addition are maintained throughout the total observation time, the growth rates return to the control rate in the presence of low concen ...
Overcoming Multidrug Resistance in Cancer
Overcoming Multidrug Resistance in Cancer

... Multidrug resistance (MDR) in tumor cells is a significant obstacle to the success of chemotherapy in many cancers. Multidrug resistance is a phenomenon whereby tumor cells in vitro that have been exposed to one cytotoxic agent develop cross-resistance to a range of structurally and functionally unr ...
Blood Drugs
Blood Drugs

... Drug therapy to promote haemostasis is rarely Drug therapy to treat or prevent thrombosis or thromboembolism, is extensively used because such diseases are common as well as serious Drugs affect haemostasis and thrombosis in three distinct ways, by affecting: 1) Blood coagulation (fibrin formation) ...
Expert position paper on the use of proton pump inhibitors in
Expert position paper on the use of proton pump inhibitors in

... has been reported that concomitant use of PPIs reduces the protective efficacy of ASA in patients with ischaemic heart disease.6,7 A case–control study investigated the antiplatelet effect of ASA in 418 ASA-treated CVD patients, 54 of whom were also treated with PPIs.7 Patients receiving PPIs had re ...
A Board Preparation Study Guide
A Board Preparation Study Guide

... Niacin niacin NIASPAN, SLO-NIACIN Cholesterol Absorption Inhibitor ezetimibe ZETIA Bile Acid Sequestrants colesevelam WELCHOL colestipol COLESTID cholestyramine QUESTRAN, PREVALITE Omega-3 Fatty Acids docosahexaenoic and eicosapentaenoic acids LOVAZA ...
View Full Text-PDF
View Full Text-PDF

... The purpose of this study was to explore the analgesic and anti-inflammatory activity of some synthesized 2-substituted acetamido-5-aryl-1,3,4-thiadiazoles (sixteen compounds). Analgesic activity was determined by using hot wire analgesiometer. The in-vivo anti-inflammatory effects of the thiadiazol ...
New Drugs in the Management of Type 2 Diabetes
New Drugs in the Management of Type 2 Diabetes

... Concentrated Insulin Glargine By concentrating insulin glargine (U-300), an extended profile of action was achieved  A “smoother” profile also resulted, with duration of activity of up to 36 hours postinjection ...
Benefits and risks of combination therapy for hepatitis B
Benefits and risks of combination therapy for hepatitis B

... chronic viral infections. Because emergence of these drugresistant viral variants can limit future therapeutic options, minimizing this complication is critical for a successful regimen. The ideal combination therapy would target different aspects of HBV replication using agents that have no crossre ...
Fragment-Based Discovery of the Pyrazol-4
Fragment-Based Discovery of the Pyrazol-4

... the series already possessed three hydrogen bond donors, a weakly basic morpholine group (pKa ≈ 7) was chosen in order minimize the increase in effective hydrogen bond donors. This initial strategy, as exemplified by 8 and 9, was successful in increasing cellular potency (Table 1). The increase in c ...
Document
Document

... The pharmacodynamic interaction between clopidogrel and PPIs and the initial findings from observational studies suggested an increased risk of cardiovascular events in concomitant users of clopidogrel and PPIs. Recently published data from a randomized clinical trial suggest that this risk is likel ...
Simultaneous Inhibition of Fatty Acid Amide Hydrolase and
Simultaneous Inhibition of Fatty Acid Amide Hydrolase and

... NJ) per day after sessions. Forty-five mice used for brain dissection had continuous access to food (Teklad 7912; Harlan, Houston, TX) in the home cage. Water was continuously available in the home cage for all mice. Mice were maintained and experiments were conducted in accordance with the Universi ...
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Discovery and development of integrase inhibitors

The first human immunodeficiency virus (HIV) case was reported in the United States in the early 1980s. Many drugs have been discovered to treat the disease but mutations in the virus and resistance to the drugs make development difficult. Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. Integrase inhibitors are a new class of drugs used in the treatment of HIV. The first integrase inhibitor, raltegravir, was approved in 2007 and other drugs were in clinical trials in 2011.
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