Details of the Target

General Information of Target

Target ID LDTP05566
Target Name 3',5'-cyclic-AMP phosphodiesterase 4D (PDE4D)
Gene Name PDE4D
Gene ID 5144
Synonyms
DPDE3; 3',5'-cyclic-AMP phosphodiesterase 4D; EC 3.1.4.53; DPDE3; PDE43; cAMP-specific phosphodiesterase 4D
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEAEGSSAPARAGSGEGSDSAGGATLKAPKHLWRHEQHHQYPLRQPQFRLLHPHHHLPPP
PPPSPQPQPQCPLQPPPPPPLPPPPPPPGAARGRYASSGATGRVRHRGYSDTERYLYCRA
MDRTSYAVETGHRPGLKKSRMSWPSSFQGLRRFDVDNGTSAGRSPLDPMTSPGSGLILQA
NFVHSQRRESFLYRSDSDYDLSPKSMSRNSSIASDIHGDDLIVTPFAQVLASLRTVRNNF
AALTNLQDRAPSKRSPMCNQPSINKATITEEAYQKLASETLEELDWCLDQLETLQTRHSV
SEMASNKFKRMLNRELTHLSEMSRSGNQVSEFISNTFLDKQHEVEIPSPTQKEKEKKKRP
MSQISGVKKLMHSSSLTNSSIPRFGVKTEQEDVLAKELEDVNKWGLHVFRIAELSGNRPL
TVIMHTIFQERDLLKTFKIPVDTLITYLMTLEDHYHADVAYHNNIHAADVVQSTHVLLST
PALEAVFTDLEILAAIFASAIHDVDHPGVSNQFLINTNSELALMYNDSSVLENHHLAVGF
KLLQEENCDIFQNLTKKQRQSLRKMVIDIVLATDMSKHMNLLADLKTMVETKKVTSSGVL
LLDNYSDRIQVLQNMVHCADLSNPTKPLQLYRQWTDRIMEEFFRQGDRERERGMEISPMC
DKHNASVEKSQVGFIDYIVHPLWETWADLVHPDAQDILDTLEDNREWYQSTIPQSPSPAP
DDPEEGRQGQTEKFQFELTLEEDGESDTEKDSGSQVEEDTSCSDSKTLCTQDSESTEIPL
DEQVEEEAVGEEEESQPEACVIDDRSPDT
Target Type
Successful
Target Bioclass
Enzyme
Family
Cyclic nucleotide phosphodiesterase family, PDE4 subfamily
Subcellular location
Apical cell membrane
Function Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
TTD ID
T02001
Uniprot ID
Q08499
DrugMap ID
TTSKMI8
Ensemble ID
ENST00000309641.10
HGNC ID
HGNC:8783
ChEMBL ID
CHEMBL288

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.W286Ter .
A549 SNV: p.E532Ter DBIA    Probe Info 
AN3CA SNV: p.V223A .
COLO792 SNV: p.Q260Ter .
EFO27 Deletion: p.L81AfsTer73 .
HCT15 SNV: p.D759V DBIA    Probe Info 
HT115 SNV: p.R237Q DBIA    Probe Info 
IGROV1 SNV: p.A500V .
LOXIMVI SNV: p.Y41C .
NCIH2286 SNV: p.S6R
Substitution: p.P53H		 DBIA    Probe Info 
NCIH2291 SNV: p.I346M .
OPM2 SNV: p.I212T .
OV90 Deletion: p.P84LfsTer60 DBIA    Probe Info 
P31FUJ SNV: p.S596G .
PF382 SNV: p.R92H .
REH SNV: p.V183A .
SW1271 SNV: p.S754G .
SW620 SNV: p.S301N DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C53(3.20)  LDD3318  [1]
5E-2FA
 Probe Info  		N.A.  LDD2235  [2]
IA-alkyne
 Probe Info  		C660(0.00); C618(0.00)  LDD0162  [3]
BTD
 Probe Info  		N.A.  LDD0004  [4]
IPM
 Probe Info  		N.A.  LDD0025  [5]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [5]
TFBX
 Probe Info  		N.A.  LDD0027  [5]
Acrolein
 Probe Info  		C548(0.00); H298(0.00); C258(0.00)  LDD0217  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa C548(0.00); H298(0.00)  LDD0222  [6]
 LDCM0107  IAA HeLa C548(0.00); H298(0.00); H578(0.00)  LDD0221  [6]
 LDCM0022  KB02 22RV1 C53(3.72)  LDD2243  [1]
 LDCM0023  KB03 22RV1 C53(3.35)  LDD2660  [1]
 LDCM0024  KB05 MELHO C53(3.20)  LDD3318  [1]
 LDCM0109  NEM HeLa N.A.  LDD0223  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Palmitoyltransferase ZDHHC17 (ZDHHC17) DHHC palmitoyltransferase family Q8IUH5
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Beta-arrestin-2 (ARRB2) Arrestin family P32121
Optineurin (OPTN) . Q96CV9
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Coilin (COIL) Coilin family P38432
. GOLGA8 family Q08AF8
Putative golgin subfamily A member 8D (GOLGA8DP) GOLGA8 family Q0D2H9
Melanoma-associated antigen 6 (MAGEA6) . P43360
TNF receptor-associated factor 1 (TRAF1) . Q13077

The Drug(s) Related To This Target

Approved
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adenosine Phosphate Small molecular drug DB00131
Amrinone Small molecular drug DB01427
Caffeine Small molecular drug DB00201
Crisaborole Small molecular drug DB05219
Dyphylline Small molecular drug DB00651
Iloprost Small molecular drug DB01088
Papaverine Small molecular drug D0NJ3V
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Denbufylline Small molecular drug D01XHG
Sotb07 . D06VFP
Phase 2
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Awd-12-281 Small molecular drug D0F4TV
Cc-1088 Small molecular drug D0U2DH
Ht-0712 Small molecular drug D07OCV
Lirimilast Small molecular drug D0F5IY
Mk-0873 Small molecular drug D0M7CB
Oglemilast Small molecular drug D0L8KJ
Piclamilast Small molecular drug D0Z2FB
Revamilast Small molecular drug D0X0PW
Tofimilast Small molecular drug D09TFB
An-2898 . D00JED
Bpn14770 . D0IZ8X
Gpd-1116 . D01XFZ
Ox-914 . D0RJ1W
Ta-7906 . D02POH
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk-356278 Small molecular drug D0K9DI
Ronomilast Small molecular drug D0O8JW
Ave-8112 . D01WZL
Mem-1414 . D03CWX
Investigative
Click To Hide/Show 35 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(R)-rolipram Small molecular drug DB04149
(S)-rolipram Small molecular drug DB03606
1-butyl-3-methyl-3,7-dihydro-purine-2,6-dione Small molecular drug D00JBC
1-methyl-3-propyl-3,7-dihydro-purine-2,6-dione Small molecular drug D00TQR
3-isobutyl-1-methyl-7h-xanthine Small molecular drug DB07954
Cilomilast Small molecular drug DB03849
Exisulind Small molecular drug DB06246
Ibudilast Small molecular drug DB05266
Isobutylmethylxanthine Small molecular drug D0R6MT
Kf-66490 Small molecular drug D0E5VP
L-454560 Small molecular drug D0JD4C
L-869298 Small molecular drug D0W7WV
Rolipram Small molecular drug D0T5PO
Rolipram Small molecular drug DB01954
Rs-25344 Small molecular drug D0P2HX
Trapidil Small molecular drug DB09283
Ucb-101333-3 Small molecular drug D02ZPV
Zardaverine Small molecular drug DB02918
(4r)-4-(3-butoxy-4-methoxybenzyl)Imidazolidin-2-one . DB06842
1-(4-aminophenyl)-35-dimethyl-1h-pyrazole-4-carboxylic Acid Ethyl Ester . DB03183
1-(4-methoxyphenyl)-35-dimethyl-1h-pyrazole-4-carboxylic Acid Ethyl Ester . DB04469
2-[3-(2-hydroxy-11-dihydroxymethyl-ethylamino)-propylamino]-2-hydroxymethyl-propane-13-diol . DB02676
35-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic Acid Ethyl Ester . DB01959
35-dimethyl-1-phenyl-1h-pyrazole-4-carboxylic Acid Ethyl Ester . DB07051
35-dimethyl-1h-pyrazole-4-carboxylic Acid Ethyl Ester . DB04271
4-[8-(3-nitrophenyl)-17-naphthyridin-6-yl]Benzoic Acid . DB08299
Al-59640 . D04BMR
Asp-3258 . D0N7HS
Cd-160130 . D0U4SS
Ch-3697 . D05YEL
Chf-5480 . D0K9PS
Ocid-2987 . D0S6MA
Tas-203 . D0S1HX
Tetomilast . DB05298
Zl-n-91 . D04JNC
Discontinued
Click To Hide/Show 15 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cdp840 Small molecular drug D0UG4T
Ci-1018 Small molecular drug D00DBE
D-22888 Small molecular drug D0R1QJ
D-4418 Small molecular drug D0K1OA
Sch-351591 Small molecular drug D01FXD
Torbafylline Small molecular drug D0F7TV
Ym-976 Small molecular drug D0C7JT
Zaprinast Small molecular drug D00YPW
Daxalipram . D0I0GM
Gw-3600 . D01QUF
Kw-4490 . D03ZVD
Las-37779 . D0V2CN
Nik-616 . D07UHY
Tjn-598 . D01OUA
V-11294a . D08SNX

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
5 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
6 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.