摘要:
Molecules having covalent catalytic activity are identified by panning synthetic and semisynthetic combinatorial libraries on solid phase suicide substrates. In an alternative mode, mechanism-based inhibitors or affinity labels may substituted for the suicide substrate. Covalent catalysts within the combinatorial library form covalent conjugates with the suicide substrate, mechanism-based inhibitor, or affinity label. Covalent conjugates are immobilized by attachment to the suicide substrate to solid phase and are easily separated from unconjugated elements of the combinatorial library by stringent washing. Combinatorial libraries employing phagemid-display are particularly preferred since such phagemids include genetic material for identifying and amplifying conjugated catalysts. Covalent catalysts obtainable by this method include, inter alia, molecules having esterolytic activity, aldol condensation activity, .beta.-lactamase activity, glycosidase activity, RNase activity, and proteolytic activity.
摘要:
This invention provides small molecule Myc-inhibitors. Also provided in the invention are therapeutic applications of these compounds for treating Myc-driven cancer and other related methods.
摘要:
The present invention provides anti-ghrelin antibodies or antigen-binding molecules that are capable of sequestering ghrelin and inhibiting ghrelin-mediated cellular activities. Also provided in the invention are therapeutic applications of combinations of these antibodies, e.g., to treat or prevent obesity.
摘要:
The invention describes the display of exogenous polypeptides on filamentous phage using a fusion between the exogenous polypeptide and phage pVII or pIX proteins. In particular, phage particles and phagemid vectors are described for expression and display of heterodimeric proteins such as antibody Fv heterodimers in combinatorial libraries, and uses thereof.
摘要:
Immunoconjugates for impeding weight gain and treating obesity in a subject are disclosed. The immunoconjugates comprise a ghrelin mimetic polypeptide hapten, a spacer moiety comprising one of more polyethylene glycol (PEG) units, and a protein carrier moiety. Immunoconjugates optionally include a conjugation moiety for conjugating the polypeptide hapten with a linker moiety or the protein carrier moiety and a linker moiety for conjugating the conjugation moiety with the protein carrier moiety.
摘要:
The invention features immunoconjugates for impeding weight gain and treating obesity in a subject. The immuno-conjugates comprise particular ghrelin polypeptides and a suitable carrier moiety.
摘要:
The invention provides an immunogenic molecular entity and related vaccines that can be used to inhibit Gram-positive bacterial quorum sensing, prevent infection or development of a disease condition associated with a Gram-positive bacterial infection. The invention also provides methods of inhibiting Gram-positive bacterial quorum sensing, and methods of preventing infection or development of a disease condition associated with a Gram-positive bacterial infection.
摘要:
The invention provides an immunogenic molecular entity, a supramolecular assembly, and an antibody that can be used to inhibit Gram-positive bacterial quorum sensing, prevent infection or development of a disease condition associated with a Gram-positive bacterial infection. The invention also provides methods of inhibiting Gram-positive bacterial quorum sensing, and methods of preventing infection or development of a disease condition associated with a Gram-positive bacterial infection.
摘要:
The invention features immunoconjugates for impeding weight gain and treating obesity in a subject. The immuno-conjugates comprise particular ghrelin polypeptides and a suitable carrier moiety.
摘要:
A reaction cassette has been designed for the highly sensitive detection of the making and breaking of chemical bonds. The system may be employed as a companion device to be used in the search for antibody and other novel catalysts. The cassette also has important clinical applications in the design of diagnostic reagents. In its fully encoded format this methodology is capable of both detecting and decoding chemical events.