G proteins
AssigneeHeptares Therapeutics Limited
InventorsByron Carpenter, Andrew Leslie, Rony Nehmé, Christopher Gordon Tate, Antony Warne
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Abstract
The invention provides a mutant of a parent heterotrimeric G protein alpha (Gα) subunit, which mutant (i) lacks at least one helix of the helical domain of the parent Gα subunit; (ii) is capable of binding to a GPCR in the absence of a heterotrimeric G protein beta (Gβ) subunit and a heterotrimeric G protein gamma (Gγ) subunit; and (iii) has an amino acid sequence that contains one or more mutations compared to the amino acid sequence of the parent heterotrimeric Gα subunit, which mutations are selected from a deletion, a substitution and an insertion.
Claims22
A mutant of a human parent heterotrimeric G protein alpha (Gα) subunit, which mutant:
- lacks the amino acid sequence of at least one of helix A, helix B, helix C, helix D, helix E, or helix F of the helical domain of the naturally-occurring parent Gα subunit, corresponding to amino acid residues 85-113, 123-136, 144-154, 157-168, 174-186 and 194-199, respectively, according to the numbering of the long isoform of human Gα-s subunit of SEQ ID NO:92;
- is capable of binding to a GPCR in the absence of a heterotrimeric G protein beta (Gβ) subunit and a heterotrimeric G protein gamma (Gγ) subunit;
- and
- has an amino acid sequence that contains one or more mutations compared to the amino acid sequence of the parent heterotrimeric Gα subunit, which mutations are selected from a deletion, a substitution and an insertion.
Dependencies are inferred from the claim text.