Details of the Target

General Information of Target

Target ID LDTP11399
Target Name Pappalysin-2 (PAPPA2)
Gene Name PAPPA2
Gene ID 60676
Synonyms
PLAC3; Pappalysin-2; EC 3.4.24.-; Pregnancy-associated plasma protein A2; PAPP-A2; Pregnancy-associated plasma protein E1; PAPP-E
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGDSDDEYDRRRRDKFRRERSDYDRSRERDERRRGDDWNDREWDRGRERRSRGEYRDYDR
NRRERFSPPRHELSPPQKRMRRDWDEHSSDPYHSGYEMPYAGGGGGPTYGPPQPWGHPDV
HIMQHHVLPIQARLGSIAEIDLGVPPPVMKTFKEFLLSLDDSVDETEAVKRYNDYKLDFR
RQQMQDFFLAHKDEEWFRSKYHPDEVGKRRQEARGALQNRLRVFLSLMETGWFDNLLLDI
DKADAIVKMLDAAVIKMEGGTENDLRILEQEEEEEQAGKPGEPSKKEEGRAGAGLGDGER
KTNDKDEKKEDGKQAENDSSNDDKTKKSEGDGDKEEKKEDSEKEAKKSSKKRNRKHSGDD
SFDEGSVSESESESESGQAEEEKEEAEEALKEKEKPKEEEWEKPKDAAGLECKPRPLHKT
CSLFMRNIAPNISRAEIISLCKRYPGFMRVALSEPQPERRFFRRGWVTFDRSVNIKEICW
NLQNIRLRECELSPGVNRDLTRRVRNINGITQHKQIVRNDIKLAAKLIHTLDDRTQLWAS
EPGTPPLPTSLPSQNPILKNITDYLIEEVSAEEEELLGSSGGAPPEEPPKEGNPAEINVE
RDEKLIKVLDKLLLYLRIVHSLDYYNTCEYPNEDEMPNRCGIIHVRGPMPPNRISHGEVL
EWQKTFEEKLTPLLSVRESLSEEEAQKMGRKDPEQEVEKFVTSNTQELGKDKWLCPLSGK
KFKGPEFVRKHIFNKHAEKIEEVKKEVAFFNNFLTDAKRPALPEIKPAQPPGPAQILPPG
LTPGLPYPHQTPQGLMPYGQPRPPILGYGAGAVRPAVPTGGPPYPHAPYGAGRGNYDAFR
GQGGYPGKPRNRMVRGDPRAIVEYRDLDAPDDVDFF
Target Bioclass
Enzyme
Family
Peptidase M43B family
Subcellular location
Secreted
Function Metalloproteinase which specifically cleaves insulin-like growth factor binding protein (IGFBP)-5 at the '163-Ser-|-Lys-164' bond. Shows limited proteolysis toward IGFBP-3.
Uniprot ID
Q9BXP8
Ensemble ID
ENST00000367661.7
HGNC ID
HGNC:14615

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.N1344D .
ABC1 SNV: p.Q163R .
AN3CA SNV: p.A377V .
COLO792 SNV: p.E1443K
Substitution: p.P1469L		 .
CORL23 SNV: p.T1410I .
CORL88 SNV: p.S840R .
EFO21 SNV: p.D904N .
FTC133 SNV: p.M1417V .
HCC1143 SNV: p.R1783L .
HCT116 SNV: p.T1008A .
HCT15 SNV: p.R1388L .
HLF SNV: p.P786Q .
HT SNV: p.S234G .
IGR1 SNV: p.P134S .
IGR37 SNV: p.M1704I .
IGR39 SNV: p.M1704I .
IGROV1 SNV: p.K154Q .
KASUMI2 SNV: p.C632R .
KATOIII SNV: p.P81T .
MCC26 SNV: p.W1639Ter .
MDST8 SNV: p.N23Y .
MEWO SNV: p.G1153E .
MKN1 SNV: p.R196M .
MOLT4 SNV: p.A291V .
NALM6 Deletion: p.S1686VfsTer4 .
NCIH1993 SNV: p.S589G; p.V1594L .
NCIH358 SNV: p.C343F .
PANC0403 SNV: p.F639V .
RH30 SNV: p.E448D .
RKO SNV: p.P493H .
SNGM SNV: p.A1420D .
SNU1 Insertion: p.V1020GfsTer7 .
SUPT1 Insertion: p.R275AfsTer7 .
SW1116 SNV: p.A170G .
TE4 SNV: p.P1600T .
TYKNU SNV: p.S1492Y DBIA    Probe Info 
WM793 SNV: p.S1678F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C656(1.24); C586(1.46)  LDD3380  [1]
BTD
 Probe Info  		C50(0.39)  LDD2089  [2]
W1
 Probe Info  		N.A.  LDD0236  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C1633(1.20)  LDD2112  [2]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C50(0.69)  LDD2130  [2]
 LDCM0215  AC10 HEK-293T C586(1.21)  LDD0813  [4]
 LDCM0226  AC11 HEK-293T C586(1.05)  LDD0824  [4]
 LDCM0237  AC12 HEK-293T C586(1.38)  LDD0835  [4]
 LDCM0259  AC14 HEK-293T C586(1.37)  LDD0857  [4]
 LDCM0270  AC15 HEK-293T C586(1.79)  LDD0868  [4]
 LDCM0276  AC17 HEK-293T C586(1.25)  LDD0874  [4]
 LDCM0277  AC18 HEK-293T C586(1.01)  LDD0875  [4]
 LDCM0278  AC19 HEK-293T C586(0.97)  LDD0876  [4]
 LDCM0280  AC20 HEK-293T C586(1.21)  LDD0878  [4]
 LDCM0281  AC21 HEK-293T C586(1.03)  LDD0879  [4]
 LDCM0282  AC22 HEK-293T C586(1.32)  LDD0880  [4]
 LDCM0283  AC23 HEK-293T C586(1.19)  LDD0881  [4]
 LDCM0284  AC24 HEK-293T C586(1.15)  LDD0882  [4]
 LDCM0320  AC57 HEK-293T C586(1.28)  LDD0918  [4]
 LDCM0321  AC58 HEK-293T C586(0.97)  LDD0919  [4]
 LDCM0322  AC59 HEK-293T C586(0.99)  LDD0920  [4]
 LDCM0323  AC6 HEK-293T C586(1.06)  LDD0921  [4]
 LDCM0324  AC60 HEK-293T C586(2.87)  LDD0922  [4]
 LDCM0325  AC61 HEK-293T C586(1.13)  LDD0923  [4]
 LDCM0326  AC62 HEK-293T C586(1.10)  LDD0924  [4]
 LDCM0327  AC63 HEK-293T C586(1.25)  LDD0925  [4]
 LDCM0328  AC64 HEK-293T C586(1.04)  LDD0926  [4]
 LDCM0329  AC65 HEK-293T C586(1.67)  LDD0927  [4]
 LDCM0330  AC66 HEK-293T C586(1.08)  LDD0928  [4]
 LDCM0331  AC67 HEK-293T C586(1.31)  LDD0929  [4]
 LDCM0334  AC7 HEK-293T C586(1.53)  LDD0932  [4]
 LDCM0345  AC8 HEK-293T C586(1.59)  LDD0943  [4]
 LDCM0248  AKOS034007472 HEK-293T C586(1.55)  LDD0846  [4]
 LDCM0356  AKOS034007680 HEK-293T C586(1.43)  LDD0954  [4]
 LDCM0275  AKOS034007705 HEK-293T C586(1.16)  LDD0873  [4]
 LDCM0498  BS-3668 MDA-MB-231 C50(0.29)  LDD2091  [2]
 LDCM0370  CL101 HEK-293T C586(1.33)  LDD0968  [4]
 LDCM0371  CL102 HEK-293T C586(1.43)  LDD0969  [4]
 LDCM0372  CL103 HEK-293T C586(1.25)  LDD0970  [4]
 LDCM0373  CL104 HEK-293T C586(1.67)  LDD0971  [4]
 LDCM0374  CL105 HEK-293T C586(1.10)  LDD0972  [4]
 LDCM0375  CL106 HEK-293T C586(1.00)  LDD0973  [4]
 LDCM0376  CL107 HEK-293T C586(1.03)  LDD0974  [4]
 LDCM0377  CL108 HEK-293T C586(1.12)  LDD0975  [4]
 LDCM0378  CL109 HEK-293T C586(0.92)  LDD0976  [4]
 LDCM0380  CL110 HEK-293T C586(1.12)  LDD0978  [4]
 LDCM0381  CL111 HEK-293T C586(0.99)  LDD0979  [4]
 LDCM0396  CL125 HEK-293T C586(0.97)  LDD0994  [4]
 LDCM0397  CL126 HEK-293T C586(1.07)  LDD0995  [4]
 LDCM0398  CL127 HEK-293T C586(0.92)  LDD0996  [4]
 LDCM0399  CL128 HEK-293T C586(0.70)  LDD0997  [4]
 LDCM0403  CL16 HEK-293T C586(1.10)  LDD1001  [4]
 LDCM0404  CL17 HEK-293T C586(1.01)  LDD1002  [4]
 LDCM0405  CL18 HEK-293T C586(1.07)  LDD1003  [4]
 LDCM0406  CL19 HEK-293T C586(1.28)  LDD1004  [4]
 LDCM0408  CL20 HEK-293T C586(1.14)  LDD1006  [4]
 LDCM0409  CL21 HEK-293T C586(1.31)  LDD1007  [4]
 LDCM0410  CL22 HEK-293T C586(0.97)  LDD1008  [4]
 LDCM0411  CL23 HEK-293T C586(0.86)  LDD1009  [4]
 LDCM0412  CL24 HEK-293T C586(1.01)  LDD1010  [4]
 LDCM0413  CL25 HEK-293T C586(1.03)  LDD1011  [4]
 LDCM0414  CL26 HEK-293T C586(1.02)  LDD1012  [4]
 LDCM0415  CL27 HEK-293T C586(0.96)  LDD1013  [4]
 LDCM0416  CL28 HEK-293T C586(0.92)  LDD1014  [4]
 LDCM0417  CL29 HEK-293T C586(1.02)  LDD1015  [4]
 LDCM0419  CL30 HEK-293T C586(1.22)  LDD1017  [4]
 LDCM0420  CL31 HEK-293T C586(1.32)  LDD1018  [4]
 LDCM0421  CL32 HEK-293T C586(1.29)  LDD1019  [4]
 LDCM0422  CL33 HEK-293T C586(1.05)  LDD1020  [4]
 LDCM0423  CL34 HEK-293T C586(1.16)  LDD1021  [4]
 LDCM0424  CL35 HEK-293T C586(1.17)  LDD1022  [4]
 LDCM0425  CL36 HEK-293T C586(1.25)  LDD1023  [4]
 LDCM0426  CL37 HEK-293T C586(1.10)  LDD1024  [4]
 LDCM0428  CL39 HEK-293T C586(1.41)  LDD1026  [4]
 LDCM0430  CL40 HEK-293T C586(1.14)  LDD1028  [4]
 LDCM0431  CL41 HEK-293T C586(1.55)  LDD1029  [4]
 LDCM0432  CL42 HEK-293T C586(1.52)  LDD1030  [4]
 LDCM0433  CL43 HEK-293T C586(1.54)  LDD1031  [4]
 LDCM0434  CL44 HEK-293T C586(1.15)  LDD1032  [4]
 LDCM0435  CL45 HEK-293T C586(1.46)  LDD1033  [4]
 LDCM0436  CL46 HEK-293T C586(1.28)  LDD1034  [4]
 LDCM0437  CL47 HEK-293T C586(1.30)  LDD1035  [4]
 LDCM0438  CL48 HEK-293T C586(1.03)  LDD1036  [4]
 LDCM0439  CL49 HEK-293T C586(1.11)  LDD1037  [4]
 LDCM0441  CL50 HEK-293T C586(1.47)  LDD1039  [4]
 LDCM0442  CL51 HEK-293T C586(1.20)  LDD1040  [4]
 LDCM0443  CL52 HEK-293T C586(0.82)  LDD1041  [4]
 LDCM0444  CL53 HEK-293T C586(0.99)  LDD1042  [4]
 LDCM0445  CL54 HEK-293T C586(1.17)  LDD1043  [4]
 LDCM0446  CL55 HEK-293T C586(1.30)  LDD1044  [4]
 LDCM0447  CL56 HEK-293T C586(1.00)  LDD1045  [4]
 LDCM0448  CL57 HEK-293T C586(1.25)  LDD1046  [4]
 LDCM0449  CL58 HEK-293T C586(1.17)  LDD1047  [4]
 LDCM0450  CL59 HEK-293T C586(1.36)  LDD1048  [4]
 LDCM0452  CL60 HEK-293T C586(1.85)  LDD1050  [4]
 LDCM0427  Fragment51 HEK-293T C586(1.13)  LDD1025  [4]
 LDCM0022  KB02 A2780 C586(1.30)  LDD2254  [1]
 LDCM0023  KB03 A2780 C656(2.51); C586(1.73)  LDD2671  [1]
 LDCM0024  KB05 OV-90 C656(1.24); C586(1.46)  LDD3380  [1]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C50(0.39)  LDD2089  [2]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C1633(0.46)  LDD2114  [2]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C50(0.57)  LDD2116  [2]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C50(0.83)  LDD2120  [2]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C50(1.08)  LDD2128  [2]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C50(3.29)  LDD2147  [2]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C50(0.36)  LDD2150  [2]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C50(0.47)  LDD2151  [2]

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 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
3 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
4 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.