Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T08813 Target Info
Target Name cAMP-dependent protein kinase A type I (PRKAR1A)
Synonyms cAMP-dependent protein kinase type I-alpha regulatory subunit; Tissue-specific extinguisher 1; TSE1; PRKAR1; PKR1
Target Type Literature-reported Target
Gene Name PRKAR1A
Biochemical Class Kinase
UniProt ID
KAP0_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: Cyclic Guanosine Monophosphate Ligand Info
Structure Description Co-crystal structure of PKA RI alpha CNB-B mutant (G316R/A336T) with cGMP PDB:5KJZ
Method X-ray diffraction Resolution 1.35 Å Mutation Yes [1]
PDB Sequence
SILMGSTLRK
242
RKMYEEFLSK
252
VSILESLDKW
262
ERLTVADALE
272
PVQFEDGQKI
282

VVQGEPGDEF
292
FIILEGSAAV
302
LQRRSENEEF
312
VEVRRLGPSD
322
YFGEIALLMN
332

RPRTATVVAR
342
GPLKCVKLDR
352
PRFERVLGPC
362
SDILKRNIQQ
372
YNSFVSLSV
Residue
Distance (Å)
VAL283
3.933
VAL302
3.758
GLN304
3.439
VAL315
3.552
ARG316
2.895
LEU318
4.765
TYR323
4.485
PHE324
3.198
GLY325
2.869
GLU326
2.593
Residue
Distance (Å)
ILE327
3.449
ALA328
2.945
LEU329
4.983
PRO334
4.739
ARG335
2.862
THR336
2.685
ALA337
3.382
VAL339
3.735
TYR373
3.427
ASN374
4.861
Ligand Name: [3H]cAMP Ligand Info
Structure Description Co-crystal Structure of PKA RI alpha CNB-B domain with cAMP PDB:5KJX
Method X-ray diffraction Resolution 1.90 Å Mutation No [1]
PDB Sequence
RKRKMYEEFL
250
SKVSILESLD
260
KWERLTVADA
270
LEPVQFEDGQ
280
KIVVQGEPGD
290

EFFIILEGSA
300
AVLQRRSENE
310
EFVEVGRLGP
320
SDYFGEIALL
330
MNRPRAATVV
340

ARGPLKCVKL
350
DRPRFERVLG
360
PCSDILKRNI
370
QQYNSFVSLS
380
V
Residue
Distance (Å)
VAL283
3.849
VAL302
3.701
GLN304
3.618
VAL315
4.235
LEU318
4.914
TYR323
4.479
PHE324
3.215
GLY325
2.974
GLU326
2.574
ILE327
3.216
Residue
Distance (Å)
ALA328
3.075
PRO334
4.502
ARG335
2.920
ALA336
2.738
ALA337
3.354
VAL339
3.672
TYR373
3.249
ASN374
2.969
SER375
3.561
LEU379
4.407
Click to View More Binding Site Information of This Target and Ligand Pair
References  Top
REF 1 Mutations of PKA cyclic nucleotide-binding domains reveal novel aspects of cyclic nucleotide selectivity. Biochem J. 2017 Jul 6;474(14):2389-2403.

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