P2Y12 receptor
AssigneePortola Pharmaceuticals, Inc.
InventorsPamela B. Conley, Hans-Michael Jantzen, Vanitha Ramakrishnan-DuBridge, David Jay Julius, Gunther Hollopeter
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Abstract
The present invention includes a novel subtype of the P2-purinergic receptor, referred to as the P2Y12 receptor. This receptor is expressed selectively in the platelets and brain, and couples to a pertussis toxin-sensitive G protein (Gi). Nucleic acids encoding the receptor and associated screening and therapeutic methods are also disclosed.
Claims57
An isolated nucleic acid molecule selected from the group consisting of:
- (a) an isolated nucleic acid molecule that encodes the amino acid sequence of SEQ ID NO:
- 2;
- (b) an isolated nucleic acid molecule which hybridizes to the complement of a nucleic acid molecule comprising SEQ ID NO:
- 1 under conditions of sufficient stringency to produce a clear signal;
- and (c) an isolated nucleic acid molecule which hybridizes to a nucleic acid molecule that encodes the amino acid sequence of SEQ ID NO:
- 2 under conditions of sufficient stringency to produce a clear signal.
An isolated receptor polypeptide comprising the amino acid sequence of SEQ ID NO:
- 2.
An isolated nucleic acid molecule that encodes the amino acid sequence of SEQ ID NO:
- 12.
An isolated receptor polypeptide comprising the amino acid sequence of SEQ ID NO:
- 12.
A method of identifying an agent which modulates the expression of a nucleic acid encoding a P2Y12 receptor comprising the steps of:
- (a) exposing cells which express the nucleic acid to the agent;
- and
- (b) determining whether the agent modulates expression of said nucleic acid, thereby identifying an agent which modulates the expression of a nucleic acid encoding the protein having the sequence of P2Y12 receptor.
A method of identifying an agent which modulates at least one activity of a P2Y12 receptor comprising the steps of:
- (a) exposing cells which express the protein to the agent;
- (b) determining whether the agent modulates at least one activity of said protein, thereby identifying an agent which modulates at least one activity of a P2Y12 receptor.
A method of identifying binding partners for a P2Y12 receptor protein comprising the steps of:
- (a) exposing said protein to a potential binding partner;
- and
- (b) determining if the potential binding partner binds to said protein, thereby identifying binding partners for a P2Y12 receptor protein.
A method of modulating the expression of a nucleic acid encoding a P2Y12 receptor protein comprising the step of:
- (a) administering an effective amount of an agent which modulates the expression of a nucleic acid encoding encoding a P2Y12 receptor protein.
A method of modulating at least one activity of a P2Y12 receptor protein comprising the step of:
- (a) administering an effective amount of an agent which modulates at least one activity of a P2Y12 receptor protein.
A non-human transgenic animal modified to contain a nucleic acid molecule which encodes a P2Y12 receptor or a truncation mutant of P2Y12 receptor.
A method of diagnosing a disease state in a subject, comprising the step of determining the level of expression of a nucleic acid molecule encoding a P2Y12 receptor.
A method of diagnosing a disease state in a subject, comprising the step of determining the level of expression of a P2Y12 receptor protein.
An isolated mutant P2Y12 receptor protein which is a naturally occurring truncation mutant, wherein said truncation is caused by a frame-shift mutation in the region of the gene encoding transmembrane domain six of the protein.
An isolated nucleic acid encoding a mutant P2Y12 receptor protein which is a naturally occurring truncation mutant, wherein said truncation is caused by a frame-shift mutation in the region of the gene encoding transmembrane domain six of the protein.
Dependencies are inferred from the claim text.