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Jiřina Stolařikova - One of the best experts on this subject based on the ideXlab platform.

  • structural basis for inhibition of mycobacterial and human adenosine kinase by 7 substituted 7 het aryl 7 deazaadenine ribonucleosides
    Journal of Medicinal Chemistry, 2014
    Co-Authors: Jan Snasel, Petr Naus, Jiři Dostal, Ales Hnizda, Jindřich Fanfrlik, Jiři Brynda, Aurelie Bourderioux, Michal Dusek, Hana Dvořakova, Jiřina Stolařikova
    Abstract:

    Adenosine kinase (ADK) from Mycobacterium tuberculosis (Mtb) was selected as a target for design of antimycobacterial nucleosides. Screening of 7-(het)aryl-7-deazaadenine ribonucleosides with Mtb and human (h) ADKs and testing with wild-type and drug-resistant Mtb strains identified specific inhibitors of Mtb ADK with micromolar antimycobacterial activity and low cytotoxicity. X-ray structures of complexes of Mtb and hADKs with 7-ethynyl-7-deazaadenosine showed differences in inhibitor interactions in the adenosine binding sites. 1D 1H STD NMR experiments revealed that these inhibitors are readily accommodated into the ATP and adenosine binding sites of Mtb ADK, whereas they bind preferentially into the adenosine site of hADK. Occupation of the Mtb ADK ATP site with inhibitors and formation of catalytically less competent semiopen conformation of MtbADK after inhibitor binding in the adenosine site explain the lack of phosphorylation of 7-substituted-7-deazaadenosines. Semiempirical quantum mechanical ana...

Wen Guo Jiang - One of the best experts on this subject based on the ideXlab platform.

  • interleukin 7 il 7 and il 7 receptor il 7r signalling complex in human solid tumours
    Histology and Histopathology, 2003
    Co-Authors: M A A Alrawi, R E Mansel, Wen Guo Jiang
    Abstract:

    Interleukin-7 (IL-7) plays an important role in the normal development and maintenance of the human immune system. Its effects are mediated via its receptor, IL-7R. Ligand-receptor engagement results in a cascade of phosphorylation events mediated by various molecules including the Janus kinases (Jak1 and Jak3), PI3-kinase, Stats (signal transducers and activators of transcription) and other molecules. The activation of IL- 7 signalling pathway results in survival, proliferation, differentiation and maturation of haematopoietic cells including B and T lymphocytes. Although the relationship of IL-7 with the development and differentiation of some haematological cancers like leukaemias and lymphomas is well recognised, little is known about it involvement with solid tumours. There are several studies that have revealed IL-7/IL-7R expression in epithelial systems and some human solid epithelial tumours. Furthermore, IL-7 can be produced by some human tumour cells and involved in tumour development and progression. In this review article we have summarised the main biological activities of IL-7 and its downstream signalling complex in relation to some human solid malignancies.

Jan Snasel - One of the best experts on this subject based on the ideXlab platform.

  • structural basis for inhibition of mycobacterial and human adenosine kinase by 7 substituted 7 het aryl 7 deazaadenine ribonucleosides
    Journal of Medicinal Chemistry, 2014
    Co-Authors: Jan Snasel, Petr Naus, Jiři Dostal, Ales Hnizda, Jindřich Fanfrlik, Jiři Brynda, Aurelie Bourderioux, Michal Dusek, Hana Dvořakova, Jiřina Stolařikova
    Abstract:

    Adenosine kinase (ADK) from Mycobacterium tuberculosis (Mtb) was selected as a target for design of antimycobacterial nucleosides. Screening of 7-(het)aryl-7-deazaadenine ribonucleosides with Mtb and human (h) ADKs and testing with wild-type and drug-resistant Mtb strains identified specific inhibitors of Mtb ADK with micromolar antimycobacterial activity and low cytotoxicity. X-ray structures of complexes of Mtb and hADKs with 7-ethynyl-7-deazaadenosine showed differences in inhibitor interactions in the adenosine binding sites. 1D 1H STD NMR experiments revealed that these inhibitors are readily accommodated into the ATP and adenosine binding sites of Mtb ADK, whereas they bind preferentially into the adenosine site of hADK. Occupation of the Mtb ADK ATP site with inhibitors and formation of catalytically less competent semiopen conformation of MtbADK after inhibitor binding in the adenosine site explain the lack of phosphorylation of 7-substituted-7-deazaadenosines. Semiempirical quantum mechanical ana...

Lisandra L. Martin - One of the best experts on this subject based on the ideXlab platform.

  • redox and acid base chemistry of 7 7 8 8 tetracyanoquinodimethane 7 7 8 8 tetracyanoquinodimethane radical anion 7 7 8 8 tetracyanoquinodimethane dianion and dihydro 7 7 8 8 tetracyanoquinodimethane in acetonitrile
    Analytical Chemistry, 2012
    Co-Authors: Ayman Nafady, Alan M. Bond, Lisandra L. Martin
    Abstract:

    The chemistry and electrochemistry of TCNQ (7,7,8,8-tetracyanoquinodimethane), TCNQ•–, TCNQ2–, and H2TCNQ in acetonitrile (0.1 M Bu4NPF6) solution containing trifluoroacetic acid (TFA) has been studied by transient and steady-state voltammetric methods with the interrelationship between the redox and the acid–base chemistry being supported by simulations of the cyclic voltammograms. In the absence of acid, TCNQ and its anions undergo two electrochemically and chemically reversible one-electron processes. However, in the presence of TFA, the voltammetry is considerably more complex. The TCNQ2– dianion is protonated to form HTCNQ–, which is oxidized to HTCNQ•, and H2TCNQ which is electroinactive over the potential range of −1.0 to +1.0 V versus Ag/Ag+. The monoreduced TCNQ•– radical anion is weakly protonated to give HTCNQ•, which disproportionates to TCNQ and H2TCNQ. In acetonitrile, H2TCNQ deprotonates slowly, whereas in N,N-dimethylformamide or tetrahydrofuran, rapid deprotonation occurs to yield HTCNQ– ...

M A A Alrawi - One of the best experts on this subject based on the ideXlab platform.

  • interleukin 7 il 7 and il 7 receptor il 7r signalling complex in human solid tumours
    Histology and Histopathology, 2003
    Co-Authors: M A A Alrawi, R E Mansel, Wen Guo Jiang
    Abstract:

    Interleukin-7 (IL-7) plays an important role in the normal development and maintenance of the human immune system. Its effects are mediated via its receptor, IL-7R. Ligand-receptor engagement results in a cascade of phosphorylation events mediated by various molecules including the Janus kinases (Jak1 and Jak3), PI3-kinase, Stats (signal transducers and activators of transcription) and other molecules. The activation of IL- 7 signalling pathway results in survival, proliferation, differentiation and maturation of haematopoietic cells including B and T lymphocytes. Although the relationship of IL-7 with the development and differentiation of some haematological cancers like leukaemias and lymphomas is well recognised, little is known about it involvement with solid tumours. There are several studies that have revealed IL-7/IL-7R expression in epithelial systems and some human solid epithelial tumours. Furthermore, IL-7 can be produced by some human tumour cells and involved in tumour development and progression. In this review article we have summarised the main biological activities of IL-7 and its downstream signalling complex in relation to some human solid malignancies.