Structure of PDB 8exv Chain A

Receptor sequence
>8exvA (length=895) Species: 9606 (Homo sapiens) [Search protein sequence]
NREEKILNREIGFAIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDL
NSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSDKQKYTL
KINHDCVPEQVIAEAIRKKTRSMYQGKYILKVCGCDEYFLEKYPLSQYKY
IRSCIMLGRMPNLMLMAKESLYSQLPMDCFTMPSYSRRTSTKSLWVINSA
LRIKILCATYVNVNIIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNE
WLNYDIYIPDLPRAARLCLSICSVEEHCPLAWGNINLFDYTDTLVSGKMA
LNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVI
EEHANWSVSREAGFSYSHAGLSNRLARDNELRENDKEQLKAISTRDPLSE
ITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPP
IKPEQAMELLDCNYPDPMVRGFAVRCLEKYLTDDKLSQYLIQLVQVLKYE
QYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYC
RACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRRP
DFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSEL
LFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIG
DCVGLIEVVRNSHTIMQIQCKFNSHTLHQWLKDKNKGEIYDAAIDLFTRS
CAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKRERVPFVL
TQDFLIVISKGAQECTKTREFERFQEMCYKAYLAIRQHANLFINLFSMML
GSGMPELQSFDDIAYIRKTLALDKTEQEALEYFMKQMNDAHHGGW
3D structure
PDB8exv Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3K alpha.
ChainA
Resolution2.48 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.7.11.1: non-specific serine/threonine protein kinase.
2.7.1.137: phosphatidylinositol 3-kinase.
2.7.1.153: phosphatidylinositol-4,5-bisphosphate 3-kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 X3N A S774 W780 I800 Y836 I848 V851 S854 Q859 M922 I932 D933 S632 W638 I658 Y694 I706 V709 S712 Q717 M772 I782 D783
Gene Ontology
Molecular Function
GO:0016301 kinase activity
Biological Process
GO:0046854 phosphatidylinositol phosphate biosynthetic process

View graph for
Molecular Function
View graph for
Biological Process
External links
PDB RCSB:8exv, PDBe:8exv, PDBj:8exv
PDBsum8exv
PubMed36455032
UniProtP42336|PK3CA_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Gene Name=PIK3CA)

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