![Rational Drug Design Approach for Overcoming Drug Resistance](http://s1.studyres.com/store/data/022673938_1-643f16021fa29e73c94316ac66727a65-300x300.png)
Rational Drug Design Approach for Overcoming Drug Resistance
... parasite cultures of P. falciparum in vitro was also strongly inhibited by these compounds with 50% inhibition of growth occurring at 3.7 µM for the m-methoxy and 0.6 µM for the m-chloro compounds with the K1 parasite line bearing the double mutation (S108N + C59R), compared to 10.2 µM for pyrimetha ...
... parasite cultures of P. falciparum in vitro was also strongly inhibited by these compounds with 50% inhibition of growth occurring at 3.7 µM for the m-methoxy and 0.6 µM for the m-chloro compounds with the K1 parasite line bearing the double mutation (S108N + C59R), compared to 10.2 µM for pyrimetha ...
Pharmacology 2002
... the intermediary metabolism of steroids such as testosterone, and of lipids. Other isoforms are responsible mainly for metabolising exogenous chemicals including drugs. Each of the isoforms has a wide substrate specificity, but each has its own specific substrate profile. This enables the whole ran ...
... the intermediary metabolism of steroids such as testosterone, and of lipids. Other isoforms are responsible mainly for metabolising exogenous chemicals including drugs. Each of the isoforms has a wide substrate specificity, but each has its own specific substrate profile. This enables the whole ran ...
New Reactions in the Crotonase Superfamily: Structure of
... enzymes, the subunit architecture can be described in terms of two distinct motifs: the larger N-terminal domain that is characterized by 10 strands of β-pleated sheet and the smaller C-terminal domain that is composed of three R-helices. The N-terminal domain contains the binding site for the acylt ...
... enzymes, the subunit architecture can be described in terms of two distinct motifs: the larger N-terminal domain that is characterized by 10 strands of β-pleated sheet and the smaller C-terminal domain that is composed of three R-helices. The N-terminal domain contains the binding site for the acylt ...
Carbapenem
... B. broad- spectrum : antibiotics that are effective against grampositive organisms and also against a significant number of gram-negative bacteria. C. Extended-spectrum: that effect wide variety of microbial species. However, this can be severely alter the nature of the normal bacterial flora (GI), ...
... B. broad- spectrum : antibiotics that are effective against grampositive organisms and also against a significant number of gram-negative bacteria. C. Extended-spectrum: that effect wide variety of microbial species. However, this can be severely alter the nature of the normal bacterial flora (GI), ...
Mechanistic Role of an NS4A Peptide Cofactor with the Truncated
... catalytic cycle, with NS4A binding first. Two distinct kinetic classes of peptidyl inhibitors based upon the 5A/5B cleavage site were identified. An NS4A-independent class is devoid of prime residues. A second class of inhibitors is NS4A-dependent and contains a natural or non-natural cyclic amino a ...
... catalytic cycle, with NS4A binding first. Two distinct kinetic classes of peptidyl inhibitors based upon the 5A/5B cleavage site were identified. An NS4A-independent class is devoid of prime residues. A second class of inhibitors is NS4A-dependent and contains a natural or non-natural cyclic amino a ...
Application of drugs based on release-active
... clinical blood analysis clinical urine analysis biochemical markers Data from regulatory bodies of countries where the drugs have been registered (15 countries) on adverse events associated with the drug use ...
... clinical blood analysis clinical urine analysis biochemical markers Data from regulatory bodies of countries where the drugs have been registered (15 countries) on adverse events associated with the drug use ...
PocketQuery: protein–protein interaction inhibitor
... virtual screening workflow. This functionality is provided under the Export tab of the molecular viewer panel. Export is available for two online virtual screening search engines: AnchorQuery (http://anchorquery.csb .pitt.edu) and ZINCPharmer (http://zincpharmer.csb .pitt.edu). Both AnchorQuery and Z ...
... virtual screening workflow. This functionality is provided under the Export tab of the molecular viewer panel. Export is available for two online virtual screening search engines: AnchorQuery (http://anchorquery.csb .pitt.edu) and ZINCPharmer (http://zincpharmer.csb .pitt.edu). Both AnchorQuery and Z ...
COX-2 inhibitor
... The secondary insult is the result of the mechanism of action. The inhibition of PG synthesis prevents the cytoprotective action of the PG Most of the gastric effects of NSAIDS are attributed to their acidic character which participates in 1) decreasing surface hydrophobicity of the mucus gel layer ...
... The secondary insult is the result of the mechanism of action. The inhibition of PG synthesis prevents the cytoprotective action of the PG Most of the gastric effects of NSAIDS are attributed to their acidic character which participates in 1) decreasing surface hydrophobicity of the mucus gel layer ...
Minimalist Active-Site Redesign: Teaching Old Enzymes New Tricks
... 2. Subtilisin: A Playground for Protein Engineers Hydrolases have been popular objects for enzyme engineering, not only because they were among the earliest characterized enzymes but also because their catalytic activities often have direct industrial applications. Serine proteases catalyze the hydr ...
... 2. Subtilisin: A Playground for Protein Engineers Hydrolases have been popular objects for enzyme engineering, not only because they were among the earliest characterized enzymes but also because their catalytic activities often have direct industrial applications. Serine proteases catalyze the hydr ...
... ABSTRACT: Recent studies have suggested that theophylline, a nonspecific phospho-diesterase inhibitor, has useful anti-inflammatory actions in asthma. Phosphodiesterase 4 (PDE4) represents the predominant PDE isoenzyme present in inflammatory cells. PDE4 inhibitors might, therefore, have beneficial ...
BALANCING ANTI-AMYLOID AND ANTI-CHOLINESTERASE CAPACITY IN A SINGLE CHEMICAL INSILICO Research Article
... ACh level in the brain by decreasing the hydrolysis of ACh. Amyloidβ (Aβ), formed by the continuously proteolytic processing of β amyloid precursor protein (APP) by β and γ-secretase [7, 8], plays a central role in the pathogenesis of AD. Recent evidence indicated certain links between Aβ and AChE [ ...
... ACh level in the brain by decreasing the hydrolysis of ACh. Amyloidβ (Aβ), formed by the continuously proteolytic processing of β amyloid precursor protein (APP) by β and γ-secretase [7, 8], plays a central role in the pathogenesis of AD. Recent evidence indicated certain links between Aβ and AChE [ ...
Summer Fellow Poster template
... Future Research: Following characterization, tissue culturing will be used to determine whether it is worth pursuing in vivo studies. We will utilize fibroblasts as our culture cell because studies have shown that adhesion cells are very similar to fibroblasts in both growth and connection [1]. If t ...
... Future Research: Following characterization, tissue culturing will be used to determine whether it is worth pursuing in vivo studies. We will utilize fibroblasts as our culture cell because studies have shown that adhesion cells are very similar to fibroblasts in both growth and connection [1]. If t ...
Antihypertensive Drugs 1
... Angiotensin receptor blockers Angiotensin II receptor blockers (ARBs) interfere with the renin-angiotensin system by impairing the binding of angiotensin II to the AT1 receptor on the cell membrane, thereby inhibiting the action of angiotensin II. Blockade of the action of angiotensin II leads to el ...
... Angiotensin receptor blockers Angiotensin II receptor blockers (ARBs) interfere with the renin-angiotensin system by impairing the binding of angiotensin II to the AT1 receptor on the cell membrane, thereby inhibiting the action of angiotensin II. Blockade of the action of angiotensin II leads to el ...
Discovery of PF-04457845: A Highly Potent
... FAAH (hFAAH) and rat FAAH (rFAAH) assay as described previously.17,22 Unlike IC50 values, kinact/Ki values are independent of preincubation times and substrate concentrations and are considered the best measure of potency for irreversible inhibitors. We found that incorporating a methylenepiperidine ...
... FAAH (hFAAH) and rat FAAH (rFAAH) assay as described previously.17,22 Unlike IC50 values, kinact/Ki values are independent of preincubation times and substrate concentrations and are considered the best measure of potency for irreversible inhibitors. We found that incorporating a methylenepiperidine ...
TAMIFLU Product Monograph
... adverse events were nausea and vomiting. These events were transient and generally occurred with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse even ...
... adverse events were nausea and vomiting. These events were transient and generally occurred with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse even ...
1946814726Revised review article greety
... Union and by FDA in October 2010) for the prevention of stroke and blood clots from AF based on the results of RE-LY trial (Randomized Evaluation of Long Term Anticoagulant Therapy, warfarin compared with dabigatran)5. This oral direct reversible thrombin inhibitor connects to thrombin with high spe ...
... Union and by FDA in October 2010) for the prevention of stroke and blood clots from AF based on the results of RE-LY trial (Randomized Evaluation of Long Term Anticoagulant Therapy, warfarin compared with dabigatran)5. This oral direct reversible thrombin inhibitor connects to thrombin with high spe ...
TAMIFLU Product Monograph
... adverse events were nausea and vomiting. These events were transient and generally occurred with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse even ...
... adverse events were nausea and vomiting. These events were transient and generally occurred with first dosing. These events did not lead to patient discontinuation of study drug in the vast majority of instances. At the recommended dose of 75 mg twice daily, the most frequently reported adverse even ...
2-Cell wall syn Inhibitor(Lec.1,2&3)
... peptidoglycan synthesis (transglycosylation) & proven to be effective against wide range of gram positive cocci & bacilli (no effect against gram negatives)causing life threatening types of both nosocomial & community acquired infections . During administration patient developed severe itching & ery ...
... peptidoglycan synthesis (transglycosylation) & proven to be effective against wide range of gram positive cocci & bacilli (no effect against gram negatives)causing life threatening types of both nosocomial & community acquired infections . During administration patient developed severe itching & ery ...
BioFiles v5 n1 - Sigma
... The sialyltransferases (ST) of the Golgi attach Neu5Ac residues to oligosaccharides using CMP-Neu5Ac as the sugar donor. These transferases produce specific glycosidic linkages for sialic acid (α2→3, α2→6, or α2→8) and have preferences for monosaccharide acceptors used in attachment. These specifici ...
... The sialyltransferases (ST) of the Golgi attach Neu5Ac residues to oligosaccharides using CMP-Neu5Ac as the sugar donor. These transferases produce specific glycosidic linkages for sialic acid (α2→3, α2→6, or α2→8) and have preferences for monosaccharide acceptors used in attachment. These specifici ...
Therapeutic Agents for Alzheimer`s Disease
... blocking cholinergic neurotransmission produces some improvement or impairment in learning and memory. ACh, a neurotransmitter in the brain plays a critical role in the function of learning and memory. ACh is synthesized from acetyl-CoA and choline by cholineacetyltransferase, and is released into t ...
... blocking cholinergic neurotransmission produces some improvement or impairment in learning and memory. ACh, a neurotransmitter in the brain plays a critical role in the function of learning and memory. ACh is synthesized from acetyl-CoA and choline by cholineacetyltransferase, and is released into t ...