초록 ▼

The invention relates to a general process by which recombinantly derived variable domains of antibodies encompassing either or both light and heavy variable regions with or without respective constant regions are engineered and selected for identification of unique surface domains of pharmaceutical

The invention relates to a general process by which recombinantly derived variable domains of antibodies encompassing either or both light and heavy variable regions with or without respective constant regions are engineered and selected for identification of unique surface domains of pharmaceutical targets or parts thereof which regulate target function. The recombinant antibodies are useful as reagents for high volume, rapid screening of occupation of the active surface domains by natural or synthetic entities. This invention is also directed to elucidating the three dimensional conformation of the antibodies, or parts thereof, which bind to the pharmaceutical targets and confers activity. Methods for creating high resolution molecular models which can direct the synthesis of biologically active small organic molecules useful as viable discovery drug leads are also provided.

대표청구항 ▼

[ I claim:] [1.] A method of identifying a potential drug candidate capable of binding to at least one site of a biologically active target, which site is capable of conferring a biological response, and wherein said potential drug candidate exhibits either agonist or antagonist activity at the targ

[ I claim:] [1.] A method of identifying a potential drug candidate capable of binding to at least one site of a biologically active target, which site is capable of conferring a biological response, and wherein said potential drug candidate exhibits either agonist or antagonist activity at the target, the method comprising:a) providing at least one detectable reporter of binding of said potential drug candidate to the biologically active target, wherein said reporter possesses agonist or antagonist activity at said target and wherein said reporter is selected from a recombinant library of antibodies comprising at least one variable region;b) screening potential drug candidates by assaying for the ability of the potential drug candidates to compete with the reporter for binding to the target; andc) selecting potential drug candidates possessing agonist or antagonist activity, which compete with the reporter for binding to the target.