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An investigation of protective formulations containing
An investigation of protective formulations containing

... Fig.   1   –   The   variation   in   the   energy   for   the   Many   pharmaceuticals   are   enzyme   stabilisation   of   the   transition   state   by   an   enzyme   is   inhibitors,   as   for   example   ibuprofen   (COX-­‐inhibitor). ...
Download CV
Download CV

... Thomas AJ, Olkowski JH, Vornov JJ, Slusher BS. “Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition.” Brain Research, 1999, 843, 48-52 Tiffany CW, Lapidus RG, Merion A, Calvin DC, Slusher BS. “Characterization of the enzymatic activity of PSM: Comparison with bra ...
Evaluation of different mycobacterial species for drug discovery and
Evaluation of different mycobacterial species for drug discovery and

... used for anti-Tb drug high-throughput screening (HTS), and to use this model to identify a novel candidate anti-tubercular drug and its cognate cellular target. A sensitive growth inhibition assay was set up with a GFP-labelled Tb vaccine strain, M. bovis BCG, using standard first and second line an ...
In Vivo Criteria To Differentiate Monoamine Reuptake Inhibitors from
In Vivo Criteria To Differentiate Monoamine Reuptake Inhibitors from

... al., 1995). It is unlikely that this would be a property of releasing agents, assuming that they produce depolarizationindependent release of 5-HT. 4) Because both reuptake inhibitors and releasing agents such as fenfluramine bind to the 5-HT carrier, pretreatment with reuptake inhibitors can attenu ...
Sequence and Structure Classification of Kinases
Sequence and Structure Classification of Kinases

... transfer reaction from a phosphate donor (usually ATP) to a receptor substrate. Although all kinases catalyze essentially the same phosphoryl transfer reaction, they display remarkable diversity in their substrate specificity, structure, and the pathways in which they participate. In order to learn ...
the PDF
the PDF

... applying knowledge, and changing preferences. It involves memory, attention, executive functions, perception, language, and psychomotor functions. The term nootropics was coined in 1972 when memory enhancing properties of piracetam were observed in clinical trials. In the meantime, hundreds of drugs ...
Irreversible Inhibitors of Serine, Cysteine, and Threonine Proteases
Irreversible Inhibitors of Serine, Cysteine, and Threonine Proteases

... With cysteine proteases, there is the papain/cathepsin B family of proteases and the caspase family. Both have quite different protein folds. Crystal structures are now available for several caspases and gingipain.22 Legumain, caspases, clostripain, separase, and gingipains have been shown to belong ...
BoNT_A Presentation UMass Dartmouth 081029
BoNT_A Presentation UMass Dartmouth 081029

... 5) Samples are run on SDS-PAGE gels and transferred to membranes for immunoblot analysis with rabbit anti-SNAP-25 and HRP-conjugated goat antirabbit IgG 6) Band intensities are read and normalized using scanning densitometry ...
NIH Public Access - The Scripps Research Institute
NIH Public Access - The Scripps Research Institute

... In 2002, the first X-ray crystal structure of FAAH was determined for the rat enzyme at 2.8 À resolution using ΔTM-rFAAH in complex with an irreversible inhibitor, methyl arachidonyl fluorophosphonate (MAFP) (52). FAAH crystallized as a dimeric enzyme, consistent with chemical cross-linking and anal ...


... antagonism, phosphodiesterase (PDE) inhibition and other actions have been advanced to explain its effectiveness in asthma. Cyclic adenosine monophosphate (AMP) and cyclic guanosine monophosphate (GMP) are involved in the regulation of smooth muscle tone, and the breakdown of these nucleotides is ca ...
C H A P
C H A P

... We have mentioned before (see General Introduction 3.4 and 4, and Chapter 3) that lipase inhibitors have a high pharmacological interest because they could help in the therapy of diseases in which lipases play an important role such as obesity or infective diseases produced by lipolytic microorganis ...
Synopsis of Some Recent Tactical Application of Bioisosteres in
Synopsis of Some Recent Tactical Application of Bioisosteres in

... drug candidates when incorported at sites relevant to metabolic modification and the first clinical studies with deuterated analogues of known drugs have recently been initiated.27-29 The KIE for D typically ranges from 1- to 7-fold, depending on the circumstance, although calculations suggest a 7- ...
PEDIATRIC PHARMACOTHERAPY
PEDIATRIC PHARMACOTHERAPY

... Pharmacotherapy will review these papers and the potential role of sirolimus in the pediatric transplant population. Mechanism of Action Sirolimus, initially known as rapamycin, is a macrolide immunosuppressive agent with a unique mechanism of action. It is a fermentation product isolated from a str ...
Mechanism of endothelial nitric oxide synthase
Mechanism of endothelial nitric oxide synthase

... years, it was reported that protein hydrolysates derived from several marine organisms, such as cod (Kim et al., 2000), salmon (Ono et al., 2006), sea cucumber collagen (Zhao et al., 2009), shrimp (Zhang et al., 2009), sesame (Biswas, Dhar & Ghosh, 2010), squid skin (Lin, Shun & Li, 2011), and jelly ...
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 ...
The challenge of selecting protein kinase assays
The challenge of selecting protein kinase assays

... development [3]. Since 2001, the FDA has approved nine kinase inhibitors for oncology targets (Table 1), and many more are now in clinical trials for the treatment of such diseases as cancer and cardiovascular and inflammatory diseases [4]. At present, ∼ 24% of all research spending on drug discover ...
Isolation and Characterization of Protease Inhibitors from Animal
Isolation and Characterization of Protease Inhibitors from Animal

... Protease inhibitors (PIs) are ubiquitous in nature and are produced by diverse animals as well as plants. There are different types of proteases such as cysteine proteases (such as papain from papayas), metalloproteases (such as thermolysin from bacteria), serine proteases (such as trypsin, chymotry ...
Structural and Functional Basis of
Structural and Functional Basis of

... heterocycle inhibitors celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] and rofecoxib (4-[4-(methylsulfonyl)phenyl]-3-phenyl-2(5H)-furanone).13,14 In addition to their reduced gastrointestinal toxicity profiles, several in vitro, in vivo, and clinical studies have demonstrated t ...
Synthesis and Pharmacological Evaluation of
Synthesis and Pharmacological Evaluation of

... Cancer, a disease of worldwide importance, is a group of diseases characterized by uncontrolled growth and spread of abnormal cells. It is now generally accepted that a neoplastic transformation is related to genes alteration or oncogene activation, allowing progress in the development of new treatm ...
Cytochrome P450 Inhibition
Cytochrome P450 Inhibition

... Overview ...
Progesterone-stimulated intracellular calcium increase in human
Progesterone-stimulated intracellular calcium increase in human

... Physiological inducers of the sperm acrosome reaction include progesterone, which can increase intracellular calcium ([Ca21]i), tyrosine phosphorylation of proteins and chloride efflux in human spermatozoa. PKC may be involved in progesterone-stimulated acrosome reaction, although controversial resu ...
drug interactions with calcium channel blockers: possible
drug interactions with calcium channel blockers: possible

... 1). In fact, a decreased inhibition was observed (⬃3-fold, Table 1). This was consistent with the fact that ketoconazole is a substrate for CYP3A. Also as expected, the quasi-irreversible inhibitor TAO showed increased inhibitory potency when preincubated in the presence of NADPH (Fig. 2, A and B; T ...
Defining the Schistosoma haematobium kinome enables the
Defining the Schistosoma haematobium kinome enables the

... focused on protein kinases13,14, because they are involved in signalling cascades of essential regulatory and developmental processes15–17, particular kinase groups have relatively conserved structures18, and also because drugs targeting these enzymes in humans have shown particular potential for th ...
Recent Advances Towards New Anti-Infective Agents that Inhibit
Recent Advances Towards New Anti-Infective Agents that Inhibit

... During the anchoring reaction SrtA recognizes two substrates, the LPXTG sorting signal within the CWS of its protein substrate, and the (Gly)5 cross-bridge peptide located within lipid II (Fig. (2)). SrtA is highly specific for the LPXTG-motif, since only the central ‘X’ residue can be altered witho ...
Macrocycles in new drug discovery
Macrocycles in new drug discovery

... representing retention of activity with respect to the acyclic parent compound. However, com­ pound 3 was observed to form an ionic inter­ action between the tertiary amine and the acid Glu91 within the ribose pocket, while 4 has an undecorated alkyl chain and so cannot make this interaction. This c ...
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