Drug binding

Xem 1-20 trên 45 kết quả Drug binding
  • The role of the ATP-binding cassette ABCB1 in mediating the resistance to chemotherapy in many forms of cancer has been well established. The pro-tein is also endogenously expressed in numerous barrier and excretory tissues, thereby regulating or impacting on drug pharmacokinetic profiles.

    pdf10p mobifone23 18-01-2013 22 2   Download

  • Medicinal chemistry is a discipline at the intersection of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties, where they are involved with design, chemical synthesis and development for market of pharmaceutical agents (drugs). Compounds used in medical applications are most often organic compounds, which are often divided into the broad classes of small organic molecules and biologics, the latter of which are most often medicinal preparations of proteins. Inorganic and organometallic compounds are also useful as drugs.

    pdf418p wqwqwqwqwq 09-07-2012 100 46   Download

  • Proteins are the driving force for all cellular processes. They regulate several cellular events through binding to different partners in the cell. They are capable of binding to other proteins, peptides, DNA, and also RNA. These interactions are essential in the regulation of cell fates and could be important in drugs development. For example RNA interacting proteins regulate gene expression through the binding to different mRNAs. These mRNAs could be involved in important cellular processes such as cell survival or apoptosis.

    pdf214p xunu1311 02-11-2012 37 9   Download

  • Tham khảo sách 'drug stereochemistry analytical methods and f'hannacology second edition_1', y tế - sức khoẻ, y học thường thức phục vụ nhu cầu học tập, nghiên cứu và làm việc hiệu quả

    pdf201p mnemosyne75 02-02-2013 19 3   Download

  • One of the Holy Grails of ATP-binding cassette transporter research is a structural understanding of drug binding and transport in a eukaryotic multidrug resistance pump. These transporters are front-line mediators of drug resistance in cancers and represent an important therapeutic target in future chemotherapy.

    pdf14p mobifone23 18-01-2013 17 2   Download

  • The Protein Data Bank contains the description of approximately 27 000 protein–ligand binding sites. Most of the ligands at these sites are biologi-cally active small molecules, affecting the biological function of the protein. The classification of their binding sites may lead to relevant results in drug discovery and design.

    pdf9p mobifone23 18-01-2013 24 2   Download

  • ABCG2 confers resistance to cancer cells by mediating the ATP-dependent outward efflux of chemotherapeutic compounds. Recent studies have indi-cated that the protein contains a number of interconnected drug binding sites. The present investigation examines the coupling of drug binding to ATP hydrolysis.

    pdf9p galaxyss3 07-03-2013 22 2   Download

  • Describing the molecular details of the multidrug efflux process of ABCB1, in particular the interdomain communication associated with bioenergetic coupling, continues to prove difficult. A number of investigations to date have implicated transmembrane helix 12 (TM12) in mediating communica-tion between the transmembrane domains and nucleotide-binding domains (NBDs) of ABCB1.

    pdf12p viettel02 19-02-2013 6 1   Download

  • An homology model of human P-glycoprotein, based on the X-ray struc-ture of the recently resolved mouse P-glycoprotein, is presented. The model corresponds to the inward-facing conformation competent for drug binding. From the model, the residues involved in the protein-binding cav-ity are identified and compared with those in the outward-facing confor-mation of human P-glycoprotein developed previously based on the Sav1866 structure.

    pdf11p viettel02 20-02-2013 16 1   Download

  • Human serum albumin (HSA) has an extraordinary ligand-binding capac-ity, and transports Fe(III)heme and medium- and long-chain fatty acids. In human immunodeficiency virus-infected patients the administered drugs bind to HSA and act as allosteric effectors. Here, the binding of Fe(III)-heme to HSA in the presence of three representative anti-HIV drugs and myristate is investigated.

    pdf12p media19 04-03-2013 11 1   Download

  • The reality is more complex since the receptor binding profile of clozapine and the newer atypical antipsychotic agents suggests that D2-receptor blockade is not essential for antipsychotic effect. The atypical drugs act on numerous receptors and modulate several interacting transmitter systems. Clozapine is a highly effective antipsychotic. It has little affinity for the D2-receptor compared with classical drugs but binds more avidly to other dopamine subtypes (e.g. D1, D3 and D4). It blocks muscarinic acetylcholine receptors, as do certain classical agents (e.g.

    pdf15p bigbaby87 03-09-2010 61 10   Download

  • “Epigenetics” as introduced by ConradWaddington in 1946, is defined as a set of interactions between genes and the surrounding environment, which determines the phenotype or physical traits in an organism, (Murrell et al., 2005;Waddington, 1942). Initial research focused on genomic regions such as heterochromatin and euchromatin based on dense and relatively loose DNA packing, since these were known to contain inactive and active genes respectively, (Yasuhara et al., 2005).

    pdf218p yeutinh98 22-09-2012 29 9   Download

  • It has been nearly 20 years since the last Humana Press book devoted to serotonin (5-hydroxytryptamine; 5-HT) receptors has appeared. Since then, the field of 5-HT receptors has undergone a revolution due to the discovery of many additional 5-HT receptors. Although 5-HT was chemically elucidated in 1948 by Page and colleagues (Rapport et al.

    pdf637p mnemosyne75 02-02-2013 33 5   Download

  • Pharmacokinetic Interactions Causing Decreased Drug Effects Gastrointestinal absorption can be reduced if a drug interaction results in drug binding in the gut, as with aluminum-containing antacids, kaolin-pectin suspensions, or bile acid sequestrants. Drugs such as histamine H 2 receptor antagonists or proton pump inhibitors that alter gastric pH may decrease the solubility and hence absorption of weak bases such as ketoconazole.

    pdf5p tubreakdance 26-11-2010 40 3   Download

  • The second section “HLA and non-MHC genes, Immune Response, and Gene Expression Studies” is dedicated to the molecular and immunological processes of AS. HLA- B*27 is a unique HLA Class I molecule: anchoring peptides in the binding grove of B pocket must have an arginine at the P2, and the free thiol Cys67 residue made B*27 easy to form homodimers in the extracellular domain. Twin studies suggest that the HLA-B*27 accounts for more than 50% of AS susceptibility. Until July 2011, 82 subtypes were described based on nucleotide differences.

    pdf170p wqwqwqwqwq 23-07-2012 33 3   Download

  • the beginning, medicinal therapy consisteodf concoctions coadministered with incantations. Little thought was given to dissecting out the contributions of the pharmacology of the concoction from the spiritual consequences of the incantations. Eventually, potions and extracts were recognized to have predictable activity that could be observed and described objectively. Then came the capacity to estimate potency,t o l eading concentration and purification.

    pdf242p mnemosyne75 02-02-2013 16 3   Download

  • Single-crystal X-ray structure determinations of the complex between the minor-groove binder distamycin and d(GGCCAATTGG) reveal two 1 : 1 binding modes which differ in the orientation of the drug molecule in the minor groove. The two crystals were grown from different crystallization conditions and found to diffract to 2.38 and ˚ 1.85 A, respectively. The structures were refined to completion using SHELXL-93, resulting in a residual R factor of ˚ 20.30% for the 2.38-A resolution structure (including 46 ˚ water molecules) and 19.74% for the 1.

    pdf10p system191 01-06-2013 13 3   Download

  • Multidrug resistance is a major challenge in the therapy of cancer and pathogenic fungal infections. More than three decades ago, P-glycoprotein was the first identified multidrug transporter. It has been studied exten-sively at the genetic and biochemical levels ever since. Pdr5, the most abun-dant ATP-binding cassette transporter in Saccharomyces cerevisiae,is highly homologous to azole-resistance-mediating multidrug transporters in fungal pathogens, and a focus of clinical drug resistance research. ...

    pdf10p mobifone23 18-01-2013 17 2   Download

  • Human P-glycoprotein (P-gp), which conveys multidrug resistance, is an ATP-dependent drug efflux pump that transports a wide variety of struc-turally unrelated compounds out of cells. P-gp possesses a ‘linker region’ of75 amino acids that connects two homologous halves, each of which contain a transmembrane domain followed by a nucleotide-binding domain.

    pdf13p viettel02 22-02-2013 12 2   Download

  • Thymidine kinase (TK) is the key enzyme in salvaging thymidine to pro-duce thymidine monophosphate. Owing to its ability to phosphorylate nucleoside analogue prodrugs, TK has gained attention as a rate-limiting drug activator.

    pdf11p galaxyss3 21-03-2013 25 2   Download


Đồng bộ tài khoản