2BCJ: G Protein-Coupled Receptor Kinase 2

Crystal Structure of G Protein-Coupled Receptor Kinase 2 in Complex with Galpha-q and Gbetagamma Subunits. Determined by X-ray diffraction at 3.06 Å resolution. Released 20 Dec 2005.

Method: X-ray diffraction
Resolution: 3.06 Å
Organisms: Bos taurus, Rattus norvegicus, Mus musculus
Chains: 4
Atoms: 10,878
Mol. weight: 166.78 kDa
Ligands: GDP, ALF, MG
Released: 20 Dec 2005

Explore 2BCJ in 3D Show helices and sheets RCSB PDB PDBe

Secondary structure: helices and β-sheets

2BCJ contains 58 α-helices and 55 β-strands across 4 chains. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.

Chain A: 31 helices, 19 β-strands

Element	Residues	Length	Sheet
α-helix	37-39	3
α-helix	40-48	9
α-helix	55-60	6
α-helix	62-74	13
α-helix	80-93	14
α-helix	98-108	11
α-helix	109-114	6
α-helix	115-118	4
α-helix	126-137	12
α-helix	147-158	12
α-helix	160-167	8
α-helix	169-182	14
β-strand	191-198	8	1
β-strand	205-210	6	1
β-strand	216-223	8	1
α-helix	224-229	6
α-helix	233-247	15
β-strand	254	1	2
β-strand	257-262	6	1
β-strand	266-271	6	1
β-strand	278	1	2
α-helix	279-286	8
α-helix	291-309	19
β-strand	313-314	2	3
α-helix	320-322	3
β-strand	323-325	3	2
β-strand	331-333	3	2
α-helix	336-338	3
β-strand	340-341	2	3
α-helix	359-362	4
α-helix	371-386	16
α-helix	399-408	10
α-helix	409-411	3
α-helix	419-428	10
α-helix	444-449	6
α-helix	452-455	4
α-helix	458-462	5
α-helix	467-468	2
α-helix	500-505	6
β-strand	511-512	2	1
α-helix	514-522	9
α-helix	526-547	22
β-strand	561-567	7	4
β-strand	577-584	8	4
β-strand	587-591	5	4
β-strand	599-602	4	4
β-strand	606-613	8	4
β-strand	618-624	7	4
β-strand	628-633	6	4
α-helix	637-658	22

Chain B: 5 helices, 28 β-strands

Element	Residues	Length	Sheet
α-helix	3-23	21
α-helix	30-33	4
α-helix	38-39	2
β-strand	47-52	6	5
β-strand	58-63	6	6
β-strand	69-74	6	6
β-strand	78-83	6	6
β-strand	89-94	6	6
α-helix	95	1
β-strand	100-105	6	7
β-strand	111-116	6	7
β-strand	120-125	6	7
β-strand	134-140	7	7
β-strand	146-151	6	8
β-strand	156-161	6	8
β-strand	165-170	6	8
β-strand	175-181	7	8
β-strand	187-192	6	9
β-strand	198-203	6	9
β-strand	207-212	6	9
β-strand	218-223	6	9
β-strand	229-234	6	10
β-strand	240-245	6	10
β-strand	250-254	5	10
β-strand	259-264	6	10
α-helix	272	1
β-strand	273-278	6	11
β-strand	284-289	6	11
β-strand	295-298	4	11
β-strand	304-307	4	11
β-strand	317-320	4	5
β-strand	327-330	4	5
β-strand	335-339	5	5

Chain G: 3 helices, 0 β-strands

Element	Residues	Length
α-helix	5-23	19
α-helix	30-44	15
α-helix	53-55	3

Chain Q: 19 helices, 8 β-strands

Element	Residues	Length	Sheet
β-strand	39-46	8	12
α-helix	52-62	11
α-helix	69-74	6
α-helix	76-97	22
α-helix	99-101	3
α-helix	106-114	9
α-helix	126-137	12
α-helix	139-146	8
α-helix	157-161	5
α-helix	164-167	4
α-helix	176-181	6
β-strand	190-195	6	12
β-strand	200-205	6	12
α-helix	212-219	8
β-strand	225-231	7	12
α-helix	232-236	5
β-strand	238	1	13
β-strand	246	1	13
α-helix	247-260	14
α-helix	262-264	3
β-strand	268-274	7	12
α-helix	276-282	7
α-helix	288-291	4
α-helix	298	1
α-helix	302-314	13
β-strand	324-328	5	12
α-helix	334-352	19

Molecules and chains

Molecule	Chains	Type	Length	Organism	UniProt
G-protein-coupled receptor kinase 2	A	protein	689	Bos taurus	P21146 (AlphaFold model)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1	B	protein	340	Bos taurus	P62871 (AlphaFold model)
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2	G	protein	71	Bos taurus	P63212 (AlphaFold model)
Guanine nucleotide-binding protein G(i) subunit alpha-1, Guanine nucleotide-binding protein G(q)…	Q	protein	353	Rattus norvegicus, Mus musculus	P10824 (AlphaFold model), P21279

Sequence of entity 1 (A), FASTA

>2BCJ_1 G-protein-coupled receptor kinase 2 (chains A)
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLKHLEEAKPLVEFYEEIKKYEKLETEEERLVCSREIFDTYIMKELLAC
SHPFSKSAIEHVQGHLVKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KTKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFVLQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRAPVVELSKVPLIQRGSANGL

Sequence of entity 2 (B), FASTA

>2BCJ_2 Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 (chains B)
XSELDQLRQEAEQLKNQIRDARKACADATLSQITNNIDPVGRIQMRTRRTLRGHLAKIYA
MHWGTDSRLLVSASQDGKLIIWDSYTTNKVHAIPLRSSWVMTCAYAPSGNYVACGGLDNI
CSIYNLKTREGNVRVSRELAGHTGYLSCCRFLDDNQIVTSSGDTTCALWDIETGQQTTTF
TGHTGDVMSLSLAPDTRLFVSGACDASAKLWDVREGMCRQTFTGHESDINAICFFPNGNA
FATGSDDATCRLFDLRADQELMTYSHDNIICGITSVSFSKSGRLLLAGYDDFNCNVWDAL
KADRAGVLAGHDNRVSCLGVTDDGMAVATGSWDSFLKIWN

Sequence of entity 3 (G), FASTA

>2BCJ_3 Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 (chains G)
MASNNTASIAQARKLVEQLKMEANIDRIKVSKAAADLMAYCEAHAKEDPLLTPVPASENP
FREKKFFSAIL

Sequence of entity 4 (Q), FASTA

>2BCJ_4 Guanine nucleotide-binding protein G(i) subunit alpha-1, Guanine nucleotide-binding protein G(q) subunit alpha chimera (chains Q)
MGCTLSAEDKAAVERSKMIDRNLREDGERSRRELKLLLLGTGESGKSTFIKQMRIIHGSG
YSDEDKRGFTKLVYQNIFTAMQAMIRAMDTLKIPYKYEHNKAHAQLVREVDVEKVSAFEN
PYVDAIKSLWNDPGIQECYDRRREYQLSDSTKYYLNDLDRVADPSYLPTQQDVLRVRVPT
TGIIEYPFDLQSVIFRMVDVGGQRSERRKWIHCFENVTSIMFLVALSEYDQVLVESDNEN
RMEESKALFRTIITYPWFQNSSVILFLNKKDLLEEKIMYSHLVDYFPEYDGPQRDAQAAR
EFILKMFVDLNPDSDKIIYSHFTCATDTENIRFVFAAVKDTILQLNLKEYNLV

Ligands and cofactors

ID	Name	Formula	Copies
GDP	Guanosine-5'-diphosphate	C10 H15 N5 O11 P2	1
ALF	Tetrafluoroaluminate ion	Al F4	1
MG	Magnesium ion	Mg	1

Primary citation

Snapshot of Activated G Proteins at the Membrane: The Gq-GRK2-G Complex. Tesmer, V.M., Kawano, T., Shankaranarayanan, A. et al. Science (2005) 310:1686-1690. DOI 10.1126/science.1118890 · PubMed

Other PDB entries of the same protein (UniProt P21146 (AlphaFold model), which also has an AlphaFold model), best resolution first:

3PVU 2.48 Å, Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor (CMPD101)
3PVW 2.49 Å, Bovine GRK2 in complex with Gbetagamma subunits and a selective kinase inhibitor…
1OMW 2.5 Å, Crystal Structure of the complex between G Protein-Coupled Receptor Kinase 2 and…
5HE0 2.56 Å, Bovine GRK2 in complex with Gbetagamma subunits and CCG215022
3PSC 2.67 Å, Bovine GRK2 in complex with Gbetagamma subunits
5HE3 2.74 Å, Bovine GRK2 in complex with Gbetagamma subunits and CCG224411
5HE2 2.79 Å, Bovine GRK2 in complex with Gbetagamma subunits and CCG224406
8JPD 2.81 Å, Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes
5UKM 3.03 Å, bovine GRK2 in complex with human Gbetagamma subunits and CCG258208 (14as)
8JPB 3.07 Å, cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1
8JPC 3.07 Å, cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 2
3UZT 3.51 Å, Structure of the C13.18 RNA Aptamer in Complex with G Protein-Coupled Receptor Kinase 2

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