摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要:
The present invention describes a direct interaction between myosin and the cytoplasmic domain of membrane proteins, particularly the phosphorylated cytoplasmic domains of the β-subunit of integrins. The invention provides methods of identifying agents which block integrin binding to myosin, methods of using agents which block integrin binding to myosin to modulate biological and pathological processes, and provides agents that block integrin mediated binding to myosin and thereby modulate related cellular or cellular component movement.
摘要:
The present invention provides the amino acid and nucleotide sequence of a protein that binds to β3 integrins, αIIb and Src kinase and is involved in integrin mediated signaling. Based on this disclosure, the present invention provides methods for identifying agents that block integrin mediated signaling, methods of using agents that block integrin mediated signaling to modulate biological and pathological processes, and agents that block integrin mediated signaling.
摘要:
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要:
The DNA encoding the C140 cell surface receptor has been cloned and sequenced. The availability of this DNA permits the recombinant production of the C140 receptor which can be produced at cell or oocyte surfaces and is useful in assay systems both for the detection of substances which affect its activity, including agonists and antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in these assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with the receptor per se or with specific regions thereof.
摘要:
An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formula R12 N(CH2)4CHNHCO- wherein each R1 is independently H, alkyl(1-6C) or at most one R?1 is R2-C=NR3¿ wherein R2 is H, alkyl(1-6C), phenyl or benzyl, or is NR4 in which each R4 is independently H or alkyl(1-6C) and R3 is H, alkyl(1-6C), phenyl or benzyl, or R2-C=NR3 is a radical selected from the group consisting of (a), (b), (c) and (d) where m is an integer of 2-3, and each R5 is independently H or alkyl(1-6C); and wherein one or two (CH¿2?) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
摘要:
Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an α2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.
摘要:
On décrit des produits de recombinaison de polypeptides modifiés récepteurs du facteur de croissance dérivé de plaquettes humaines. Des structures de domaines des régions extracellulaires sont identifiées et des réagencements combinatoires des segments récepteurs sont décrits. Des formes solubles ainsi que des formes à liaison cellulaire de segments modifiés sont disponibles, ainsi que des procédés de titrage les utilisant, permettant la détection d'analogues de ligand.