IOSR Journal of Dental and Medical Sciences (IOSR-JDMS)
... Type2 Diabetes is a progressive, chronic metabolic disease characterized by hyperglycemia. The effect of excessive glucose concentration regarded as “glucotoxicity” contributes to pancreatic beta cell failure and insulin resistance. The incidence and prevalence of diabetes keeps uncontrollably incre ...
... Type2 Diabetes is a progressive, chronic metabolic disease characterized by hyperglycemia. The effect of excessive glucose concentration regarded as “glucotoxicity” contributes to pancreatic beta cell failure and insulin resistance. The incidence and prevalence of diabetes keeps uncontrollably incre ...
No Slide Title
... e-withdrawing group at position 5 increases activity (based on only 2 compounds though) H-bond donor group at positions 3, 4,or 5 is good for activity Term = 1 if a HBD group is at any of these positions Term = 2 if HBD groups are at two of these positions Term = 0 if no HBD group is present at thes ...
... e-withdrawing group at position 5 increases activity (based on only 2 compounds though) H-bond donor group at positions 3, 4,or 5 is good for activity Term = 1 if a HBD group is at any of these positions Term = 2 if HBD groups are at two of these positions Term = 0 if no HBD group is present at thes ...
in silico for prediction of resistance
... domain that contains the atP binding site is sandwiched between the two lobes. this domain sits beneath the P-loop (that is, the phosphate-binding loop or glycinerich loop) that has a role in determining the shape of the atP binding site. in the active kinase, a characteristic DFG-motif or catalytic ...
... domain that contains the atP binding site is sandwiched between the two lobes. this domain sits beneath the P-loop (that is, the phosphate-binding loop or glycinerich loop) that has a role in determining the shape of the atP binding site. in the active kinase, a characteristic DFG-motif or catalytic ...
evaluation of ethanolic leaf extract of dioscorea hispida dennst
... acetic acid induced writhing methods to assess its analgesic activity. The extract was also evaluated for its antiinflammatory activity by subjecting it to ‘carrageenan’ induced paw oedema test for its effect on acute phase inflammation models in rats, as well as analgesic activity in mice. It was f ...
... acetic acid induced writhing methods to assess its analgesic activity. The extract was also evaluated for its antiinflammatory activity by subjecting it to ‘carrageenan’ induced paw oedema test for its effect on acute phase inflammation models in rats, as well as analgesic activity in mice. It was f ...
In vitro and in vivo structure and activity relationship analysis of
... polymethoxylated flavones and flavanones have been reported to have promising anticancer and anticarcinogenesis activity, which are frequently associated with excessive angiogenesis, the effect of this subclass of flavonoids on angiogenesis remains unclear. Only two recent studies touched on the ant ...
... polymethoxylated flavones and flavanones have been reported to have promising anticancer and anticarcinogenesis activity, which are frequently associated with excessive angiogenesis, the effect of this subclass of flavonoids on angiogenesis remains unclear. Only two recent studies touched on the ant ...
Biron_JSBMB_2015_rev - Corpus UL
... Like other NRs, the AR displays a modular structure composed of an N-terminal domain (NTD) bearing the activation function (AF) 1, a DNA-binding domain (DBD), a connecting hinge region containing a nuclear localization signal (NLS) and a C-terminal ligand-binding domain (LBD) (Fig. 1). The LBD is co ...
... Like other NRs, the AR displays a modular structure composed of an N-terminal domain (NTD) bearing the activation function (AF) 1, a DNA-binding domain (DBD), a connecting hinge region containing a nuclear localization signal (NLS) and a C-terminal ligand-binding domain (LBD) (Fig. 1). The LBD is co ...
Facilitated diffusion of glucosamine-6
... permeases are not essential for fungal growth [9]. Conversion of FMDP into its acetoxymethyl ester gave a lipophilic ‘pro-drug’, with the antifungal activity a little higher than that of the parent compound, but still unsatisfactory [4]. 2-Amino-2-deoxy-D-glucitol-6-P (ADGP) was reported to be a tra ...
... permeases are not essential for fungal growth [9]. Conversion of FMDP into its acetoxymethyl ester gave a lipophilic ‘pro-drug’, with the antifungal activity a little higher than that of the parent compound, but still unsatisfactory [4]. 2-Amino-2-deoxy-D-glucitol-6-P (ADGP) was reported to be a tra ...
Document
... children (up to 5mg/kg/dose twice daily). Under-dosing must be avoided wherever possible due to low barrier development of HIV drug resistance. A reduced dose (150200mg/m2/dose once daily) is recommended for the first 2 weeks when initiating NVP treatment regimens. Young children require a higher NV ...
... children (up to 5mg/kg/dose twice daily). Under-dosing must be avoided wherever possible due to low barrier development of HIV drug resistance. A reduced dose (150200mg/m2/dose once daily) is recommended for the first 2 weeks when initiating NVP treatment regimens. Young children require a higher NV ...
Synopsis of Some Recent Tactical Application of Bioisosteres in
... conservative example of bioisosterism given the similarities between the two isotopes, but there are circumstances in drug design where this change can offer a significant advantage. The differences in physical chemical properties between H and D are small but measurable: D is slightly less lipophil ...
... conservative example of bioisosterism given the similarities between the two isotopes, but there are circumstances in drug design where this change can offer a significant advantage. The differences in physical chemical properties between H and D are small but measurable: D is slightly less lipophil ...
Impact of Cooking Procedures on Antibacterial Drug
... tylosin concentration in raw tissue could not be applied for consumer exposure and dietary intake calculations when the whole cooked product is consumed. It is verified that cooking reduced macrolide residues in meat although, it is necessary to regard correct consumption of veterinary drug in anima ...
... tylosin concentration in raw tissue could not be applied for consumer exposure and dietary intake calculations when the whole cooked product is consumed. It is verified that cooking reduced macrolide residues in meat although, it is necessary to regard correct consumption of veterinary drug in anima ...
Identification of GZD824 as an Orally Bioavailable Inhibitor That
... inhibition (Table 1). Although many studies have demonstrated that the “flag-methyl” group at the R2 position is critical for compound 1 and many other Bcr-Abl inhibitors to maintain their kinase inhibition, compound 10b, in which the methyl group was removed, displayed potency comparable to that of ...
... inhibition (Table 1). Although many studies have demonstrated that the “flag-methyl” group at the R2 position is critical for compound 1 and many other Bcr-Abl inhibitors to maintain their kinase inhibition, compound 10b, in which the methyl group was removed, displayed potency comparable to that of ...
Syddansk Universitet The Monoamine Oxidase Inhibitor
... The early MAOI diets recommended were unnecessarily restrictive. In fact, very few foods have sufficient tyramine content to approach the threshold of a serious hypertensive reaction [28]. A high-tyramine meal, however, is sufficient to increase blood pressure critically, when a substantial part of ...
... The early MAOI diets recommended were unnecessarily restrictive. In fact, very few foods have sufficient tyramine content to approach the threshold of a serious hypertensive reaction [28]. A high-tyramine meal, however, is sufficient to increase blood pressure critically, when a substantial part of ...
Meropenem-Clavulanic Acid Has High In Vitro Activity against Multidrug-Resistant Mycobacterium tuberculosis
... a -lactamase inhibitor (18, 20–23). The combination of -lactam antibiotics and -lactamase inhibitors has shown anti-TB effect in humans (24, 25), rodents (26), within macrophages (10), and against nonreplicating M. tuberculosis in vitro (8). MEM has poor intrinsic activity (12) but is bactericida ...
... a -lactamase inhibitor (18, 20–23). The combination of -lactam antibiotics and -lactamase inhibitors has shown anti-TB effect in humans (24, 25), rodents (26), within macrophages (10), and against nonreplicating M. tuberculosis in vitro (8). MEM has poor intrinsic activity (12) but is bactericida ...
Kwartaalbericht
... removal from the protective pouch. Each patch provides analgesia for 7 days. After removal of the patch, a new patch should be applied to a different skin site every week making sure that at least 3 weeks pass before the same skin site is used again. When only 2 weeks had passed between applications ...
... removal from the protective pouch. Each patch provides analgesia for 7 days. After removal of the patch, a new patch should be applied to a different skin site every week making sure that at least 3 weeks pass before the same skin site is used again. When only 2 weeks had passed between applications ...
Science of PARP (Parp inhibitor, Parp inhibitors
... roles in cellular processes, most notably in DNA repair and programmed cell death. Healthy cells can use PARP to repair themselves and live out their normal life cycle. But cancer cells may also use PARP to repair DNA damage, thus extending their uncontrolled growth. Such cancers can become resistan ...
... roles in cellular processes, most notably in DNA repair and programmed cell death. Healthy cells can use PARP to repair themselves and live out their normal life cycle. But cancer cells may also use PARP to repair DNA damage, thus extending their uncontrolled growth. Such cancers can become resistan ...
Pharmacological Evaluation of Saraca indica Leaves for Central
... compared with the control and it also ...
... compared with the control and it also ...
Selective Cox-2 Inhibitor
... The products of arachidonic acid metabolism affect a variety of biologic processes, such as inflammation and hemostasis, and play important roles in renal, cardiovascular, and pulmonary systems. Arachidonic acid is liberated from the phospholipid membrane by phospholipase and is then metabolized by ...
... The products of arachidonic acid metabolism affect a variety of biologic processes, such as inflammation and hemostasis, and play important roles in renal, cardiovascular, and pulmonary systems. Arachidonic acid is liberated from the phospholipid membrane by phospholipase and is then metabolized by ...
Drug metabolizing enzyme activities versus genetic variances for
... approximately a quarter of all the commonly therapeutic drugs in used clinical practice today. CYP 2D6 hydroxylates aromatic rings or an accompanying short side-chain of basic aryl-alkyl amines containing a protonated nitrogen. Of all enzymes of pharmacokinetic importance, the CYP 2D6 gene that enco ...
... approximately a quarter of all the commonly therapeutic drugs in used clinical practice today. CYP 2D6 hydroxylates aromatic rings or an accompanying short side-chain of basic aryl-alkyl amines containing a protonated nitrogen. Of all enzymes of pharmacokinetic importance, the CYP 2D6 gene that enco ...
Antibacterial Agents which Act Against Cell Metabolism
... and/or silver sulfacetamide) from 4-aminobenzene sulfonamide. 3.Explain how an ‘azo-dye’ breaks down in vivo to yield sulphanilamide? 4.N1-substitution in sulphanilamide is more effective and useful than N4-. Explain. 5.Classify sulphonamide on the basis of their site of action. Give the structure, ...
... and/or silver sulfacetamide) from 4-aminobenzene sulfonamide. 3.Explain how an ‘azo-dye’ breaks down in vivo to yield sulphanilamide? 4.N1-substitution in sulphanilamide is more effective and useful than N4-. Explain. 5.Classify sulphonamide on the basis of their site of action. Give the structure, ...
Selective Inhibition of Brain Na,K-ATPase by Drugs
... this enzyme. According to the drug concentrations that inhibit 50 % of enzyme activity (IC50), the potency can be listed in the following order: methyldigoxin >> promethazine > verapamil ≥ propranolol. From the inhibition of commercially available purified Na,K-ATPase isolated from porcine cerebral ...
... this enzyme. According to the drug concentrations that inhibit 50 % of enzyme activity (IC50), the potency can be listed in the following order: methyldigoxin >> promethazine > verapamil ≥ propranolol. From the inhibition of commercially available purified Na,K-ATPase isolated from porcine cerebral ...
ELAEOCARPUS SPHAERICUS EXTRACT Research Article
... maintained between the 1st and 2nd phase is due to release of kinin like substances and the 2nd phase due to the release of prostaglandins like compound13. Prostaglandins (PGs) play a major role in the development of the second phase of inflammatory reaction which is measured at 3rd hr14. It can be ...
... maintained between the 1st and 2nd phase is due to release of kinin like substances and the 2nd phase due to the release of prostaglandins like compound13. Prostaglandins (PGs) play a major role in the development of the second phase of inflammatory reaction which is measured at 3rd hr14. It can be ...
PerspectiVe
... This information can be used to quickly build up which parts of the active site are “hot spots” for gaining affinity and which groups on the inhibitor are the most effective. GE can also be used to elegantly illustrate how the addition of relatively large groups with moderate gains in potency is not ...
... This information can be used to quickly build up which parts of the active site are “hot spots” for gaining affinity and which groups on the inhibitor are the most effective. GE can also be used to elegantly illustrate how the addition of relatively large groups with moderate gains in potency is not ...
MedWatch - Boca Medical Products, Inc
... Re: Use of Skin Products Containing Numbing Ingredients (Topical Anesthetic Drugs) for Cosmetic Procedures and Potential Life-Threatening Side Effects FDA informed consumers and healthcare professionals of the potential hazards of using skin numbing products containing topical anesthetic drugs such ...
... Re: Use of Skin Products Containing Numbing Ingredients (Topical Anesthetic Drugs) for Cosmetic Procedures and Potential Life-Threatening Side Effects FDA informed consumers and healthcare professionals of the potential hazards of using skin numbing products containing topical anesthetic drugs such ...
Table 3: Detailed Pediatric DR-TB Drug Information
... renal failure -Regarding “Levels”: same approach as for aminoglycosides above ...
... renal failure -Regarding “Levels”: same approach as for aminoglycosides above ...
Erectile Dysfunction Drugs Changed the Protein Expressions and
... The cytochrome P450s (CYPs) are superfamily of hemoproteins, which metabolise various compounds. The currently known CYPs in humans are classified into 18 different families and 44 subfamilies according to their amino acids sequence homology [5]. CYPs are widely accepted to be the key enzymes in can ...
... The cytochrome P450s (CYPs) are superfamily of hemoproteins, which metabolise various compounds. The currently known CYPs in humans are classified into 18 different families and 44 subfamilies according to their amino acids sequence homology [5]. CYPs are widely accepted to be the key enzymes in can ...