Topic 3 Proteins as Drug Targets
... Inhibitor binds reversibly to the allosteric site Intermolecular bonds are formed Induced fit alters the shape of the enzyme Active site is distorted and is not recognised by the substrate Increasing substrate concentration does not reverse inhibition Inhibitor is not similar in structure to the sub ...
... Inhibitor binds reversibly to the allosteric site Intermolecular bonds are formed Induced fit alters the shape of the enzyme Active site is distorted and is not recognised by the substrate Increasing substrate concentration does not reverse inhibition Inhibitor is not similar in structure to the sub ...
Patrick_Chapter_4
... Covalent bond formed between the drug and the enzyme Substrate is blocked from the active site Increasing substrate concentration does not reverse inhibition Inhibitor likely to be similar in structure to the substrate ...
... Covalent bond formed between the drug and the enzyme Substrate is blocked from the active site Increasing substrate concentration does not reverse inhibition Inhibitor likely to be similar in structure to the substrate ...
- Opus
... with ~44% of the efficiency of 3-fluoro-2-methyldecanoyl-CoA and was is a promising drug target for prostate and other cancers, but until now it has significantly more efficient than ‘racemisation’ of 2-methyldecanoyl-CoA (as been under-exploited because of the difficulties in determining enzyme jud ...
... with ~44% of the efficiency of 3-fluoro-2-methyldecanoyl-CoA and was is a promising drug target for prostate and other cancers, but until now it has significantly more efficient than ‘racemisation’ of 2-methyldecanoyl-CoA (as been under-exploited because of the difficulties in determining enzyme jud ...
zanamivir Relenza Pharmacologic class: selective neuraminidase
... zanamivir Relenza Pharmacologic class: selective neuraminidase inhibitor Pregnancy risk category C AVAILABLE FORMS Powder for inhalation: 5 mg/blister INDICATIONS & DOSAGES ➤Uncomplicated acute illness caused by influenza virus A and B in patients who have had symptoms for no longer than 2 days Adul ...
... zanamivir Relenza Pharmacologic class: selective neuraminidase inhibitor Pregnancy risk category C AVAILABLE FORMS Powder for inhalation: 5 mg/blister INDICATIONS & DOSAGES ➤Uncomplicated acute illness caused by influenza virus A and B in patients who have had symptoms for no longer than 2 days Adul ...
Metrifonate
... leading to increase in brain Ach levels within 1 hour of oral administration it undergoes little protein binding <15% • Metabolism: It is a prodrug biotransformation of mertifonate occurs independently of the hepatic cytochrome P450 It is slowly and non-enzymatically transformed to DDVP whic ...
... leading to increase in brain Ach levels within 1 hour of oral administration it undergoes little protein binding <15% • Metabolism: It is a prodrug biotransformation of mertifonate occurs independently of the hepatic cytochrome P450 It is slowly and non-enzymatically transformed to DDVP whic ...
P026 The role of histidine in tryptophan 2,3
... Tryptophan 2,3-dioxygenase (TDO) from Xanthomonas campestris is a heme-containing enzyme from a small family of homologous enzymes, which includes indoleamine 2,3-dioxygenase (IDO). TDO is a homotetrameric enzyme and displays high specificity for L-tryptophan (L-Trp) and related derivatives such as ...
... Tryptophan 2,3-dioxygenase (TDO) from Xanthomonas campestris is a heme-containing enzyme from a small family of homologous enzymes, which includes indoleamine 2,3-dioxygenase (IDO). TDO is a homotetrameric enzyme and displays high specificity for L-tryptophan (L-Trp) and related derivatives such as ...
Study guide for research assistants
... Note that all 220,000 compounds were initially screened at a single concentration (3 µM) and that hits from this first round of screening were then tested over a range of concentrations. This is a pretty standard approach. The paper says, "A number of other inhibitors from unique structural classes ...
... Note that all 220,000 compounds were initially screened at a single concentration (3 µM) and that hits from this first round of screening were then tested over a range of concentrations. This is a pretty standard approach. The paper says, "A number of other inhibitors from unique structural classes ...
Neuraminidase inhibitors as anti
... lipophilic amides (compounds 13 and 14) led to very potent NA inhibitors (Sollis et al., 1996). Interestingly, this class of compounds exhibited more potent influenza A NA inhibitory activity compared to that of influenza B. The detailed X-ray crystallographic analysis of 13 bound to NA illustrates ...
... lipophilic amides (compounds 13 and 14) led to very potent NA inhibitors (Sollis et al., 1996). Interestingly, this class of compounds exhibited more potent influenza A NA inhibitory activity compared to that of influenza B. The detailed X-ray crystallographic analysis of 13 bound to NA illustrates ...
chapter 8 - Lange Textbooks
... that inhibit HSV and to a lesser extent varicella-zoster virus (VZV) 2. Intravenous acyclovir is used for serious HSV ii. Treatment and Prophylaxis 1. Effective against herpes and zoster c. Valacyclovir, Famciclovir, and Penciclovir 1. Valacyclovir is a prodrug of acyclovir that is better absorbed a ...
... that inhibit HSV and to a lesser extent varicella-zoster virus (VZV) 2. Intravenous acyclovir is used for serious HSV ii. Treatment and Prophylaxis 1. Effective against herpes and zoster c. Valacyclovir, Famciclovir, and Penciclovir 1. Valacyclovir is a prodrug of acyclovir that is better absorbed a ...
Detection and management of antiviral resistance for influenza
... (from 66 to 91 hour) and decrease (by sevenfold) the viral burst size, that is, the total number of virions produced per cell.38 However, the infectious-unit-to-particle ratio of the H275Y mutant strain was 12-fold higher than that of oseltamivir-susceptible strain (019 versus 0016 per RNA copy) ...
... (from 66 to 91 hour) and decrease (by sevenfold) the viral burst size, that is, the total number of virions produced per cell.38 However, the infectious-unit-to-particle ratio of the H275Y mutant strain was 12-fold higher than that of oseltamivir-susceptible strain (019 versus 0016 per RNA copy) ...
rational drug design
... 25. Would you expect negatively charged ions to be attracted to or repelled away from this ring of negatively charged amino acids? Explain your answer. Should be repelled as like charges repel. 26. Outside the cell there is a soup of positive and negative ions and other chemicals. Explain how the st ...
... 25. Would you expect negatively charged ions to be attracted to or repelled away from this ring of negatively charged amino acids? Explain your answer. Should be repelled as like charges repel. 26. Outside the cell there is a soup of positive and negative ions and other chemicals. Explain how the st ...
antiviral_Hammer
... 6. The drugs are useful for treatment and prophylaxis of influenza A virus infections. 7. Drug resistance is mediated by mutations in the M2 coding region and drug resistant virus can be transmitted person to person. B. Zanamivir and Oseltamivir Recent progress in the treatment of influenza viruses ...
... 6. The drugs are useful for treatment and prophylaxis of influenza A virus infections. 7. Drug resistance is mediated by mutations in the M2 coding region and drug resistant virus can be transmitted person to person. B. Zanamivir and Oseltamivir Recent progress in the treatment of influenza viruses ...
The Mechanism of Influenza Virus Haemagglutination
... that the influenza virus possesses a specific enzyme grouping on its surface. It is only comparatively recently, however, that the substrate, which constitutes the red-cell surface receptor, has been identified. Many other macromolecular substances have been found which will bind on to the surface o ...
... that the influenza virus possesses a specific enzyme grouping on its surface. It is only comparatively recently, however, that the substrate, which constitutes the red-cell surface receptor, has been identified. Many other macromolecular substances have been found which will bind on to the surface o ...
Discovery of Entry Inhibitors for HIV-1: Predictions via a Novel De Novo Protein Design Framework and Experimental Validation
... acid sequences with the lowest energies by solving an integer programming sequence selection model [1]. The validation stage uses both fold specificity calculations and approximate binding affinity calculations to re-rank the sequences from stage one, validating the sequence’s fold and binding to a ...
... acid sequences with the lowest energies by solving an integer programming sequence selection model [1]. The validation stage uses both fold specificity calculations and approximate binding affinity calculations to re-rank the sequences from stage one, validating the sequence’s fold and binding to a ...
cover_article_1135_en_US
... via Ca2+/calmodulin (CaM)/signaling to human vacuolar protein sorting 34 (hVps34) due to AKT inhibition. DC120 also attenuated the inhibitory effect of AKT on C-Raf by decreasing the phosphorylation of C-Raf at Ser259 and activated the mitogen-activated protein kinase (MAPK) pathway. The activation ...
... via Ca2+/calmodulin (CaM)/signaling to human vacuolar protein sorting 34 (hVps34) due to AKT inhibition. DC120 also attenuated the inhibitory effect of AKT on C-Raf by decreasing the phosphorylation of C-Raf at Ser259 and activated the mitogen-activated protein kinase (MAPK) pathway. The activation ...
HPA Pharmacological treatment and prophylaxis of influenza
... zanamivir is preferred over inhaled zanamivir. 8. Immunocompromised patients should be given inhaled zanamivir therapy regardless of antiviral susceptibility. Therapy should be continued until viral shedding from the respiratory tract is not evident in sequential samples. 9. If oseltamivir resistanc ...
... zanamivir is preferred over inhaled zanamivir. 8. Immunocompromised patients should be given inhaled zanamivir therapy regardless of antiviral susceptibility. Therapy should be continued until viral shedding from the respiratory tract is not evident in sequential samples. 9. If oseltamivir resistanc ...
Characterization of 2 Influenza A(H3N2) Clinical Isolates with
... the R229I mutation was ∼4.4% for H3N2 isolates collected in the Province of Quebec from 1997–2000, whereas most (97.7%) of the isolates were 226V. The NA catalytic region, consisting of 8 framework and 10 functional residues [4], was conserved in all our isolates. Kinetics of virus binding. The bind ...
... the R229I mutation was ∼4.4% for H3N2 isolates collected in the Province of Quebec from 1997–2000, whereas most (97.7%) of the isolates were 226V. The NA catalytic region, consisting of 8 framework and 10 functional residues [4], was conserved in all our isolates. Kinetics of virus binding. The bind ...
VIRTUAL HIGH THROUGHPUT SCREENING FOR AVIAN
... the molecular docking with different conformations of the neuraminidase monomer. The ligands were drimene, faradiol, ochrolifuanine A, beta-amyrin and cycloartenol. In molecular docking with different conformations of the neuraminidase tetramer, drimene and ochrolifuanine A in addition to jacoumaric ...
... the molecular docking with different conformations of the neuraminidase monomer. The ligands were drimene, faradiol, ochrolifuanine A, beta-amyrin and cycloartenol. In molecular docking with different conformations of the neuraminidase tetramer, drimene and ochrolifuanine A in addition to jacoumaric ...
Chapter 8
... Tertiary - interactions between R groups • Ionic Bonds – positively and negatively charged aas bond • Disulfide bridges – covalent bonds of two cysteines (–SH) ...
... Tertiary - interactions between R groups • Ionic Bonds – positively and negatively charged aas bond • Disulfide bridges – covalent bonds of two cysteines (–SH) ...
LAB 8: ENZYMES AS DRUG TARGETS.
... What is the turnover number per active site of acetylcholine esterase? ...
... What is the turnover number per active site of acetylcholine esterase? ...
Control of Metabolic Pathways (2)
... • These compete with molecules of substrate for the active sites on an enzyme • Molecular structure similar to the substrate • Rate of reaction is reduced ...
... • These compete with molecules of substrate for the active sites on an enzyme • Molecular structure similar to the substrate • Rate of reaction is reduced ...
have
... • Viruses are among the smallest micro-organisms varying in size from 0.020.04μm and can be seen and identified by electron microscopes. • They are simply nucleic acid (either DNA or RNA), which constitutes the genetic material; surrounded by a protein shell (the whole structure is called the nucleo ...
... • Viruses are among the smallest micro-organisms varying in size from 0.020.04μm and can be seen and identified by electron microscopes. • They are simply nucleic acid (either DNA or RNA), which constitutes the genetic material; surrounded by a protein shell (the whole structure is called the nucleo ...
Antiviral Medications for H1N1 Flu Virus
... Certain antiviral medications can be used to treat influenza symptoms. The H1N1 flu virus can be treated by two prescription medications called oseltamivir (Tamiflu®) and zanamivir (Relenza®). Another antiviral medication, amantadine, does not work against the H1N1 flu virus. These medications stop ...
... Certain antiviral medications can be used to treat influenza symptoms. The H1N1 flu virus can be treated by two prescription medications called oseltamivir (Tamiflu®) and zanamivir (Relenza®). Another antiviral medication, amantadine, does not work against the H1N1 flu virus. These medications stop ...
Antiviral_07ho
... active against both influenza A and B inhibits influenza viral neuraminidase. Neuraminidase must cleave terminal sialic acid residues on receptors recognized by viral hemagglutinin. Without this cleavage, virus remains trapped on infected cells --no release of infectious particles ...
... active against both influenza A and B inhibits influenza viral neuraminidase. Neuraminidase must cleave terminal sialic acid residues on receptors recognized by viral hemagglutinin. Without this cleavage, virus remains trapped on infected cells --no release of infectious particles ...