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... atom and replacing it by the side chain of the new amino acid. In some studies, the atom is also kept intact for mutations between amino acids R, K and Q, as these are relatively large amino acids and normally located at the protein surface [9]. The mutant structure is then optimized by conformation ...
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Antimicrobial resistance

... Virginiamycin Arsenical compounds Nitrofurans Sulfonamides Streptomycin Roxarsone Carbadox ...
$doc.title

... therapeu6c  poten6al  for  inflammatory  condi6ons  where  excessive  or   deregulated  IL-­‐36  signalling  may  have  a  func6on  in  disease  pathology,  such  as   psoriasis.  Specifically,  direct  therapeu6c  u6lity  as  inhibitors  of  neu ...
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- The University of Liverpool Repository

... and evaluation of this novel antifungal in Phase 1 oral and intravenous single and repeat dose trials*. ...
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... some cases the nuclear apparatus of the host cells. The chemicals that interfere with the virus growth also interact with the normal functions of the host cells. So, the earlier inhibitory drugs used in infection control showed no preferential action on the virus-controlled synthesis compared to hos ...
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... hormones (TRH, vasopressin, insulin, gastrin). * The peptide bonds in proteins are metastable (i.e. in water, they break spontaneously, in living organisms, the process is facilitated by enzymes (protease/peptidase) ...
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Antimycobacterium

... the concurrent administration of pyridoxine (vitamin B6) prevents the occurrence of peripheral neuritis. INH is metabolized by acetylation. Nearly half of the population are fast acylators of INH and the other half are slow acylators of INH. Slow acylators (including middle easterns) are genetically ...
Valganciclovir Inhibits Human Adenovirus Replication and
Valganciclovir Inhibits Human Adenovirus Replication and

... etc., that form seven species (A–G). Many Ad types are ubiquitous and quite benign, but under certain circumstances Ads can cause serious infections of the respiratory and gastrointestinal tracts, the eye, and other organs, and Ads can be very dangerous in immunocompromised patients (reviewed in [1, ...
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Antipsychotics in the Pipeline

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Considerations for Target Selection in CNS Drug Discovery Programs

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Screening of pancreatic cancer cell lines with oncolytic

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... multiple clinical programs.  This presentation will highlight select case study examples of clinical  failures  due  to  poor  oral  drug  exposure  and  unexpected  toxicology,  as  well  as  the  many  confounding factors associated with confirming a role for AO in the metabolism of a candidate  d ...
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... inhibitor, and cross-resistance between rifampin and rifapentine is complete. Rifapentine is a potent inducer of cytochrome P450 enzymes, and it has the same drug interaction profile. Toxicity is similar to that of rifampin. Rifapentine 600 mg (10 mg/kg) once weekly is indicated for treatment of tub ...
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Antiprotozoal Drugs - IHMC Public Cmaps (3)

... affected. Sulfonamides are broad spectrum (including protozoa) and bacteriostatic. (3) Therapeutic uses. These drugs are used for both the prevention and treatment of ...
ANTI MYCOBACTERIAL DRUGS
ANTI MYCOBACTERIAL DRUGS

... The lipid rich mycobacterial cell wall is impermeable to many agents(e.g. drugs).  Mycobacterial species are intracellular pathogens, and organisms residing within macrophages are inaccessible to drugs that penetrate these cells poorly.  Finally,mycobacteria are notorius for their ability to devel ...
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Print this article - Journal of Applied Pharmaceutical Research

... Columbia Institute of Pharmacy, Tekari, Near Vidhan Sabha, Raipur, C.G., 493111, India The important therapeutic approach for treating type 2 diabetes mellitus is to decrease the post-prandial glucose levels which could be done by decreasing the absorption of glucose through the inhibition of the ca ...
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Antimalarial Drugs

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CHF Drugs

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... endogenous cathecolamines epinephrine and norepinephrine. In the central nervous system they modulate a wide variety of physiological functions such as arousal, attention, learning and memory. Historically, the adrenergic receptor family has been divided to α1-adrenoceptors, α2adrenoceptors and β1-a ...
Psychopharmacology of Mood Disorders
Psychopharmacology of Mood Disorders

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Relative Potency of Protease Inhibitors in Monocytes/Macrophages
Relative Potency of Protease Inhibitors in Monocytes/Macrophages

... late stages of replication, and such combinations have proven highly effective in a number of clinical trials, with plasma HIV-1 frequently becoming undetectable by RNA polymerase chain reaction [11, 12, 19, 20]. Such potent inhibition of HIV1 replication has also been found to be associated with a ...
Structure-based drug design - Biomolecular Structure Center
Structure-based drug design - Biomolecular Structure Center

... worldwide at that time. Yet at a meeting a few months ago, Alex Wlodawer showed a slide listing close to 200 structure determinations that have been performed worldwide on a single protein, HIV protease, complexed with a large variety of inhibitors; the number may have risen even further since then ...
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Chapter 10 Pharmacology

...  H2 Antagonists  Bind to H2 receptors, found only in the stomach, to decrease the amount of hydrochloric acid produced.  Representative drugs: ...
Toxicological Relationships Between Proteins Obtained From a
Toxicological Relationships Between Proteins Obtained From a

... • Selection of 233 classes from the MDL Drug Data Report • ~90,000 molecules • 15 independent 50%/50% splits into training/test set ...
< 1 ... 33 34 35 36 37 38 39 40 41 ... 66 >

Discovery and development of integrase inhibitors

The first human immunodeficiency virus (HIV) case was reported in the United States in the early 1980s. Many drugs have been discovered to treat the disease but mutations in the virus and resistance to the drugs make development difficult. Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. Integrase inhibitors are a new class of drugs used in the treatment of HIV. The first integrase inhibitor, raltegravir, was approved in 2007 and other drugs were in clinical trials in 2011.
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