implications of protein flexibility for drug discovery
... The structure of donepezil (Aricept; 3) (FIG. 5), a marketed anticholinergic drug, bound to Torpedo californica acetylcholinesterase (TcAchE) has been determined at 2.5 Å resolution15. It has a Ki = 3.35 nM for acetylcholinesterase. It binds in the active-site gorge through π–π STACKING and CATION–π ...
... The structure of donepezil (Aricept; 3) (FIG. 5), a marketed anticholinergic drug, bound to Torpedo californica acetylcholinesterase (TcAchE) has been determined at 2.5 Å resolution15. It has a Ki = 3.35 nM for acetylcholinesterase. It binds in the active-site gorge through π–π STACKING and CATION–π ...
Enzymes
... Chemical reactions in organisms have to take place at an organism’s body temperature. Often, reactants are found in low concentrations. Because the reactions must take place very quickly, they usually need a catalyst. Enzymes are catalysts for chemical reactions in living things. Enzymes, like other ...
... Chemical reactions in organisms have to take place at an organism’s body temperature. Often, reactants are found in low concentrations. Because the reactions must take place very quickly, they usually need a catalyst. Enzymes are catalysts for chemical reactions in living things. Enzymes, like other ...
CME GP`s Auckland and Northland, 17 October 2009, Omapere
... • SCOPE trial (Study of COgnition and Prognosis in the Elderly) had 5000 pat aged 70-89 years with SBP 160-180 or DBP 90-99 • Randomised to candesartan or diuretic • In candesartan group reduction of MAP of 22 mmHg against 18 in diuretics • Marked reduction in stroke in candesartan but no decrease i ...
... • SCOPE trial (Study of COgnition and Prognosis in the Elderly) had 5000 pat aged 70-89 years with SBP 160-180 or DBP 90-99 • Randomised to candesartan or diuretic • In candesartan group reduction of MAP of 22 mmHg against 18 in diuretics • Marked reduction in stroke in candesartan but no decrease i ...
Angiotensin-Receptor Blockade in Acute Myocardial Infarction — A
... affect the care of high-risk patients after acute myocardial infarction? Given that valsartan was as effective as captopril in reducing the rates of death and other cardiovascular events, the ultimate question raised by this trial is whether high-risk patients should receive ACE inhibitors or angiot ...
... affect the care of high-risk patients after acute myocardial infarction? Given that valsartan was as effective as captopril in reducing the rates of death and other cardiovascular events, the ultimate question raised by this trial is whether high-risk patients should receive ACE inhibitors or angiot ...
Antifungal Agents
... Nystatin -- more toxic than Amphotericin B * bind to ergosterol in fungal membranes, making them unstable Antimetabolites: Flucytosine -- will get to CNS; resistance develops quickly, so often given w/ amphotericin B Antifungal azoles: Clotrimazole -- used topically Miconazole -- used topically...ca ...
... Nystatin -- more toxic than Amphotericin B * bind to ergosterol in fungal membranes, making them unstable Antimetabolites: Flucytosine -- will get to CNS; resistance develops quickly, so often given w/ amphotericin B Antifungal azoles: Clotrimazole -- used topically Miconazole -- used topically...ca ...
Nonsteroidal Anti-inflammatory Drugs
... Absorption is decreased by food. Half-life 11hours Highly bound to plasma proteins No effect on platelet aggregation Metabolized in liver by CYP2C9 to in active metabolite. • Its clearance is decreased in liver ...
... Absorption is decreased by food. Half-life 11hours Highly bound to plasma proteins No effect on platelet aggregation Metabolized in liver by CYP2C9 to in active metabolite. • Its clearance is decreased in liver ...
CARBOXYLIC ACIDS STUDY GUIDE 1. Name the following
... dressing and how it works. What common food product is added to home made salad dressing which is very rich in lecithin? 26. Name a surfactant ( full name and abbreviation ) that is used as a laxative. What medical procedure frequent uses it as a “prep”? 27. Why are nonionic surfactants often combin ...
... dressing and how it works. What common food product is added to home made salad dressing which is very rich in lecithin? 26. Name a surfactant ( full name and abbreviation ) that is used as a laxative. What medical procedure frequent uses it as a “prep”? 27. Why are nonionic surfactants often combin ...
Enzymes
... Chemical reactions in organisms have to take place at an organism’s body temperature. Often, reactants are found in low concentrations. Because the reactions must take place very quickly, they usually need a catalyst. Enzymes are catalysts for chemical reactions in living things. Enzymes, like other ...
... Chemical reactions in organisms have to take place at an organism’s body temperature. Often, reactants are found in low concentrations. Because the reactions must take place very quickly, they usually need a catalyst. Enzymes are catalysts for chemical reactions in living things. Enzymes, like other ...
Tutorial - 4: Respiratory Drug Development
... Structure (1) is terbutaline, a selective β2 adrenoceptor agonist used as a bronchodilator for the treatment of asthma. Structure (2) is bambuterol, an orally active long acting β2adrenoceptor agonist used in the treatment of asthma. Terbutaline has short duration of action due to the enzymati ...
... Structure (1) is terbutaline, a selective β2 adrenoceptor agonist used as a bronchodilator for the treatment of asthma. Structure (2) is bambuterol, an orally active long acting β2adrenoceptor agonist used in the treatment of asthma. Terbutaline has short duration of action due to the enzymati ...
Tranquilizers and Sedative-Hypnotics
... - 5,5 disubstituted with R2 & R3 for maxiumum activity • - R= C5—C6 long chain for good activity, and enhance potency . C9 • increase lipophlicity. - Branching of R , cyclic or uncaturated C=C • Enhanced short duration of action • - N-methyl decrease activity of BA • -Replace ( S ) in position 2 ( ...
... - 5,5 disubstituted with R2 & R3 for maxiumum activity • - R= C5—C6 long chain for good activity, and enhance potency . C9 • increase lipophlicity. - Branching of R , cyclic or uncaturated C=C • Enhanced short duration of action • - N-methyl decrease activity of BA • -Replace ( S ) in position 2 ( ...
Document
... Reserpine was isolated in 1952 from the dried root of Rauwolfia serpentina (Indian snakeroot),[4] and introduced in 1954, two years after chlorpromazine.[5] Reserpine almost irreversibly blocks the uptake (and storage) of noradrenaline and dopamine into synaptic vesicles by inhibiting the Vesicular ...
... Reserpine was isolated in 1952 from the dried root of Rauwolfia serpentina (Indian snakeroot),[4] and introduced in 1954, two years after chlorpromazine.[5] Reserpine almost irreversibly blocks the uptake (and storage) of noradrenaline and dopamine into synaptic vesicles by inhibiting the Vesicular ...
Discovery and development of ACE inhibitors
The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. This led to the development of Captopril, the first ACE inhibitor. When the adverse effects of Captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began.