Of drug metabolism

Biotherapeutics (BTs), one of the fastest growing classes of drug molecules, offer several advantages over the traditional small molecule pharmaceuticals because of their relatively high specificity, low off-target effects, and biocompatible metabolism, in addition to legal and logistic advantages. However, their clinical utility is limited, among other things, by their high immunogenic potential and/or variable therapeutic efficacy in different patient populations.

7p caothientrangnguyen 09-05-2020 23 1   Download

Quantifying the multiple processes which control and modulate the extent of oral bioavailability for drug candidates is critical to accurate projection of human pharmacokinetics (PK). Understanding how gut wall metabolism and hepatic elimination factor into first-pass clearance of drugs has improved enormously. Typically, the cytochrome P450s, uridine 5′- diphosphate-glucuronosyltransferases and sulfotransferases, are the main enzyme classes responsible for drug metabolism. Knowledge of the isoforms functionally expressed within organs of first-pass clearance, their anatomical topology (e.

16p caothientrangnguyen 09-05-2020 19 1   Download

The cytochrome P450 family of enzymes has long been known tometabolize a wide range of compounds, including many of today’s most common drugs. A novel nuclear receptor called PXR has been established as an activator of several of the cytochrome P450 genes, including CYP3A4. This enzyme is believed to account for the metabolism of more than 50% of all prescription drugs. PXR is therefore used as a negative selector target and discriminatory filter in preclinical drug development.

9p research12 29-04-2013 44 3   Download

Liver microsomal preparations are routinely used to predict drug interactions that can occurin vivo as a result of inhi-bition of cytochrome P450 (CYP)-mediated metabolism. However, the concentration of free drug (substrate and inhibitor)at its intrahepatic site of action, a variable that cannot be directly measured, may be significantly different from that in microsomal incubation systems.

10p tumor12 20-04-2013 47 4   Download

Malaria remains a major health problem especially in trop-ical and subtropical regions of the world, and therefore developing new antimalarial drugs constitutes an urgent challenge. Lipid metabolism has been attracting a lot of attention as an application for malarial chemotherapeutic purposes in recent years. However, little is known about glycosphingolipid biosynthesis inPlasmodium falciparum. In this report we describe for the first time the presence of an active glucosylceramide synthase in the intraerythrocytic stages of the parasite....

11p dell39 03-04-2013 31 4   Download

Prolonged exposure of pancreatic beta cells to the sulfonylureas glibenca-mide and tolbutamide induces subsequent desensitization to the actions of these drugs. The precise mechanisms underlying this desensitization remain unknown, prompting the present study, which investigated the impact of prolonged sulfonylurea exposure on glucose and energy metabolism using clonal pancreatic BRIN-BD11 beta cells.

9p inspiron33 23-03-2013 42 4   Download

In the search for new drug targets in the human parasite Entamoeba histolytica, metabolic control analysis was applied to determine, experimen-tally, flux control distribution of amebal glycolysis. The first (hexokinase, hexose-6-phosphate isomerase, pyrophosphate-dependent phosphofructo-

16p galaxyss3 07-03-2013 52 4   Download

Branched-chain lipids are important components of the human diet and are used as drug molecules, e.g. ibuprofen. Owing to the presence of methyl groups on their carbon chains, they cannot be metabolized in mitochon-dria, and instead are processed and degraded in peroxisomes. Several dif-ferent oxidative degradation pathways for these lipids are known, including a-oxidation, b-oxidation, and x-oxidation.

14p media19 06-03-2013 39 3   Download

Constitutively expressed human cytochrome P450 2D6 (CYP2D6; EC 1.14.14.1) is responsible for the metabolism of approximately 25% of drugs in common clinical use. It is widely accepted that CYP2D6 is localized in the endoplasmic reticulum of cells; however, we have identified this enzyme in the mitochondria of human liver samples and found that extensive inter-individual variability exists with respect to the level of the mitochondrial enzyme.

14p viettel02 22-02-2013 44 4   Download

The present study aimed to determine the role of Kupffer cells (KCs) in cytochrome P450 (CYP) isozyme activity and the expression of its gene during polymicrobial sepsis. For ablation of KCs, rats were pretreated with gadolinium chloride (GdCl3 ) at 48 and 24 h before cecal ligation and punc-ture (CLP). The depletion of KCs was confirmed by measuring the mRNA level of the KC marker gene CD163.

11p cosis54 05-01-2013 42 4   Download

Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Drug metabolizing enzyme activities versus genetic variances for drug of clinical pharmacogenomic relevance...

9p thulanh17 27-10-2011 38 2   Download

Thyroiditis is the inflammation of the thyroid gland. The thyroid gland is located on the front of the neck below the laryngeal prominence, and makes hormones that control metabolism. There are many different types of thyroiditis, with the most common being Hashimoto's thyroiditis. Other forms of the disease are postpartum thyroiditis, subacute thyroiditis, silent thyroiditis, drug-induced thyroiditis, radiation-induced Association, 2008).

4p truongthiuyen2 10-06-2011 91 3   Download