摘要:
The invention features compounds of the general formula (VIa) in which the variable groups are as defined herein, and to their preparation and use.
摘要:
Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein.
摘要:
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
摘要:
Single AAV vector constructs for regulated expression of an immunoglobulin molecule or fragment thereof and methods of making and using the same are described. The AAV vectors comprise a regulated promoter operably linked to the coding sequence for a first and second immunoglobulin coding sequence, a sequence encoding a self-processing cleavage site between the coding sequence for the first and second immunoglobulin coding sequence and a additional proteolytic cleavage site, which provides a means to remove the self processing peptide sequenc from an expressed immunoglobulin molecule or fragment thereof. The vector constructs find utility in enhanced production of biologically active immunoglobulins or fragments thereof in vitro and in vivo.
摘要:
This invention relates to compounds of the general formula (I), in which R?A, RB, RC, RD¿, and z are as defined herein, and to their preparation and use.
摘要:
An in vitro assay method permits the identification of a test substance which inhibits the mutual association of a pair of proteins. The method includes the steps of providing a pair of proteins capable of mutual association, one of said proteins bearing a covalently linked fluorophore; preparing a mixture containing the two proteins and at least one test substance; irradiating the mixture with polarized light of a suitable wavelength permitting excitation of the fluorophore as indicated by emission of polarized light; measuring the degree of polarization of the emission, and determining the effect of the presence or concentration of the test substance in decreasing the observed emission polarization of a mixture of the two proteins alone. Inhibitory activity of in the test substance correlates with decreased depolarization values.
摘要:
The invention relates to human ZAP-70, and in particular, to the region of ZAP-70 containing the tandem Src homology-2 ('SH2') domains, to crystalline forms thereof, liganded or unliganded, which are particularly useful for the determination of the three-dimensional structure of the protein. The three-dimensional structure of the tandem SH2 region of ZAP provides information useful for the design of pharmaceutical compositions which inhibit the biological function of ZAP and other members of the ZAP family of SH2 domain-containing proteins, particularly those biological functions mediated by molecular interactions involving one or both SH2 domains.