Rigel Pharmaceuticals, Incorporated

Jakob Maria Bogenberger

David C Anderson

Beau R Peelle

James B Lorens

Weiduan Xu

Sacha Holland

James Bradley Lorens

Susan E Swift

Robert E Atchison

The present invention relates to regulation of angiogenesis. More particularly, the present invention is directed to nucleic acids encoding 'angiogenesis regulatory proteins and nucleic acids' which are involved in modulation of angiogenesis. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, RNAi, and ribozymes, that modulate angiogenesis via modulation of angiogenesis regulatory proteins and nucleic acids; as well as to the use of expression profiles and compositions in diagnosis and therapy of diseases related to angiogenesis.

Modulators of angiogenesis

The invention relates to the use of scaffold proteins, particularly green fluorescent protein (GFP), in fusion constructs with random and defined peptides and peptide libraries, to increase the cellular expression levels, decrease the cellular catabolism, increase the conformational stability relative to linear peptides, and to increase the steady state concentrations of the library peptides and peptide library members expressed in cells for the purpose of detecting the presence of the peptides and screening peptide libraries. N-terminal, C-terminal, dual N- and C-terminal and one or more internal fusions are all contemplated. Novel fusions utilizing self-binding peptides to create a conformationally stabilized fusion domain are also contemplated.

Structurally biased random peptide libraries based on different scaffolds

The present invention relates to regulation of angiogenesis. More particularly, the present invention is directed to nucleic acids encoding C1-angiogenesis protein, also called integrin-linked kinase associated protein ('ILKAP') and ILKAP protein, which is involved in modulation of angiogenesis. The invention further relates to methods for identifying and using agents, including small organic molecules, antibodies, peptides, cyclic peptides, nucleic acids, antisense nucleic acids, and ribozymes, that modulate angiogenesis via modulation of ILKAP and ILKAP-related cascades; as well as to the use of expression profiles and compositions in diagnosis and therapy of angiogenesis.

The present invention provides random cDNA expression vector libraries, comprising expression vectors which comprise random cDNAs positioned in sense and antisense orientation, which are useful for the delivery and expression of a combination of genetic effector types to host cells. Methods for producing these libraries through bi-directional cloning of random cDNAs are also provided. Also provided herein are methods of using these libraries to screen for agents capable of modulating cell phenotype in desirable ways.

Bi-directionally cloned random cDNA expression vector libraries, compositions and methods of use

The present invention relates to the field of immunology, and more particularly to the regulation of antibody idiotypes. Provided are compositions and methods for determining and quantitating immunoglobulin germline transcript expression. As disclosed herein, these methods can be used to screen a plurality of candidate agents to identify a candidate agent capable of modulating an immunoglobulin germline transcript. Further, these methods can be used to identify a candidate agent having different modulatory effects on distinct immunoglobulin germline transcripts.

RNAse probe protection assays in screening for modulators of immunoglobulin germline transcription

The invention relates to the use of fluorescent proteins, particularly green fluorescent protein (GFP), in fusion constructs with random and defined peptides and peptide libraries, to increase the cellular expression levels, decrease the cellular catabolism, increase the conformational stability relative to linear peptides, and to increase the steady state concentrations of the random peptides and random peptide library members expressed in cells for the purpose of detecting the presence of the peptides and screening random peptide libraries. N-terminal, C-terminal, dual N- and C-terminal and one or more internal fusions are all contemplated. Novel fusions utilizing self-binding peptides to create a conformationally stabilized fusion domain are also contemplated.

Green fluorescent protein fusions with random peptides

The invention relates to the use of scaffold proteins, particularly green fluorescent protein (GFP), in fusion constructs with random and defined peptides and peptide libraries, to increase the cellular expression levels, decrease the cellular catabolism, increase the conformational stability relative to linear peptides, and to increase the steady state concentrations of the random peptides and random peptide library members expressed in cells for the purpose of detecting the presence of the peptides and screening random peptide libraries. N-terminal, C-terminal, dual N- and C-terminal and one or more internal fusions are all contemplated. Novel fusions utilizing self-binding peptides to create a conformationally stabilized fusion domain are also contemplated.

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San Mateo, CA, United States of America

Jakob Maria Bogenberger