Cadus Technologies, Inc.

Cadus Pharmaceutical Corp.

Jeremy I Paul

Joshua Trueheart

Christine A Klein

Dana M Fowlkes

John P Manfredi

Andrew J Murphy

James R Broach

Jim Broach

Andrew J M Murphy

Hans A Fuernkranz

Scott Holmes

Debra Nathan

Yeast cells are engineered to express both a surrogate of a pheromone system protein (e.g., enzymes involved in maturation of &#x3b1;-factor, transporters of a-factor, pheromone receptors, etc.) and a potential peptide modulator of the surrogate, in such a manner that the inhibition or activation of the surrogate affects a screenable or selectable trait of the yeast cells. Various additional features improve the signal-to-noise ratio of the screening/selection system.

Yeast cells engineered to produce pheromone system protein surrogates, and uses therefor

The present invention pertains to novel yeast cells which are useful for the expression of heterologous G protein coupled receptors. The yeast cells of the present invention can be used in screening assays which can be used to screen for modulators of G protein coupled receptors. Specifically, the invention provides novel yeast cells which express a heterologous G protein coupled receptor and mutant and/or chimeric G protein subunit molecules which serve to functionally integrate the heterologous into the pheromone signaling pathway of the yeast cell. The invention also provides for the expression of heterologous G protein coupled receptors which are functionally integrated into the yeast cell membrane using a yeast &#x3b1; factor leader sequence. Drug discovery assays using the subject yeast cells are also provided.

Yeast cells expressing modified G proteins and methods of use therefor

The present invention makes available rapid, effective assays for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assays enable rapid screening of large numbers of polypeptides in a library to identify those polypeptides which induce or antagonize receptor bioactivity. The subject assays are particularly amenable for identifying agonists and antagonists for orphan receptors. In particular the present invention makes available novel ligand agonists of human formyl peptide receptor like-1 (FPRL-1) receptors. These novel ligand agonists are used in the assays of the invention to identify modulators of FPRL-1 receptor.

Methods and compositions for identifying receptor effectors

The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.

Yeast cells engineered to produce pheromone system protein surrogates and uses therefor

The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assay enables rapid screening of large numbers of polypeptides in a yeast expression library to identifying those polypeptides which induce or antagonize receptor bioactivity. The subject assay is particularly amenable for identifying surrogate ligands for orphan receptors.

Methods for identifying G protein coupled receptor effectors

The present invention makes available a rapid, effective assay for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular protein, e.g., a receptor or ion channel. The subject assay enables rapid screening of large numbers of compounds to identify those which act as an agonist or antagonist to the bioactivity of the cellular protein. The subject assay is particularly amenable for identifying surrogate ligands for receptors especially from small molecule or peptide libraries or from peptides produced by an autocrine system.

Recombinant yeast cells for identifying receptor effectors

Yeast cells are engineered to express both a surrogate of a pheromone system protein (e.g., enzymes involved in maturation of .alpha.-factor, transporters of a-factor, pheromone receptors, etc.) and a potential peptide modulator of the surrogate, in such a manner that the inhibition or activation of the surrogate affects a screenable or selectable trait of the yeast cells. Various additional features improve the signal-to-noise ratio of the screening/selection system.

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Nyack, NY, United States of America

Jeremy I Paul