Details of the Target

General Information of Target

Target ID LDTP11835
Target Name Diphthine methyl ester synthase (DPH5)
Gene Name DPH5
Gene ID 51611
Synonyms
Diphthine methyl ester synthase; EC 2.1.1.314; Diphthamide biosynthesis methyltransferase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MFQLPVNNLGSLRKARKTVKKILSDIGLEYCKEHIEDFKQFEPNDFYLKNTTWEDVGLWD
PSLTKNQDYRTKPFCCSACPFSSKFFSAYKSHFRNVHSEDFENRILLNCPYCTFNADKKT
LETHIKIFHAPNASAPSSSLSTFKDKNKNDGLKPKQADSVEQAVYYCKKCTYRDPLYEIV
RKHIYREHFQHVAAPYIAKAGEKSLNGAVPLGSNAREESSIHCKRCLFMPKSYEALVQHV
IEDHERIGYQVTAMIGHTNVVVPRSKPLMLIAPKPQDKKSMGLPPRIGSLASGNVRSLPS
QQMVNRLSIPKPNLNSTGVNMMSSVHLQQNNYGVKSVGQGYSVGQSMRLGLGGNAPVSIP
QQSQSVKQLLPSGNGRSYGLGSEQRSQAPARYSLQSANASSLSSGQLKSPSLSQSQASRV
LGQSSSKPAAAATGPPPGNTSSTQKWKICTICNELFPENVYSVHFEKEHKAEKVPAVANY
IMKIHNFTSKCLYCNRYLPTDTLLNHMLIHGLSCPYCRSTFNDVEKMAAHMRMVHIDEEM
GPKTDSTLSFDLTLQQGSHTNIHLLVTTYNLRDAPAESVAYHAQNNPPVPPKPQPKVQEK
ADIPVKSSPQAAVPYKKDVGKTLCPLCFSILKGPISDALAHHLRERHQVIQTVHPVEKKL
TYKCIHCLGVYTSNMTASTITLHLVHCRGVGKTQNGQDKTNAPSRLNQSPSLAPVKRTYE
QMEFPLLKKRKLDDDSDSPSFFEEKPEEPVVLALDPKGHEDDSYEARKSFLTKYFNKQPY
PTRREIEKLAASLWLWKSDIASHFSNKRKKCVRDCEKYKPGVLLGFNMKELNKVKHEMDF
DAEWLFENHDEKDSRVNASKTADKKLNLGKEDDSSSDSFENLEEESNESGSPFDPVFEVE
PKISNDNPEEHVLKVIPEDASESEEKLDQKEDGSKYETIHLTEEPTKLMHNASDSEVDQD
DVVEWKDGASPSESGPGSQQVSDFEDNTCEMKPGTWSDESSQSEDARSSKPAAKKKATMQ
GDREQLKWKNSSYGKVEGFWSKDQSQWKNASENDERLSNPQIEWQNSTIDSEDGEQFDNM
TDGVAEPMHGSLAGVKLSSQQA
Target Bioclass
Enzyme
Family
Diphthine synthase family
Function
S-adenosyl-L-methionine-dependent methyltransferase that catalyzes four methylations of the modified target histidine residue in translation elongation factor 2 (EF-2), to form an intermediate called diphthine methyl ester. The four successive methylation reactions represent the second step of diphthamide biosynthesis.
Uniprot ID
Q9H2P9
Ensemble ID
ENST00000342173.11
HGNC ID
HGNC:24270

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 SNV: p.G41E .

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  		C231(1.26)  LDD3325  [1]
Acrolein
 Probe Info  		N.A.  LDD0222  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [4]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [4]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [5]
TFBX
 Probe Info  		N.A.  LDD0027  [5]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C269
 Probe Info  		25.28  LDD1939  [6]
VE-P
 Probe Info  		N.A.  LDD0396  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C219(0.97)  LDD1508  [8]
 LDCM0226  AC11 HEK-293T C26(1.07); C161(1.09)  LDD1509  [8]
 LDCM0237  AC12 HEK-293T C219(1.02)  LDD1510  [8]
 LDCM0270  AC15 HEK-293T C219(1.14)  LDD1513  [8]
 LDCM0277  AC18 HEK-293T C219(0.98)  LDD1516  [8]
 LDCM0278  AC19 HEK-293T C26(1.06); C161(0.77)  LDD1517  [8]
 LDCM0279  AC2 HEK-293T C219(0.76)  LDD1518  [8]
 LDCM0280  AC20 HEK-293T C219(0.99)  LDD1519  [8]
 LDCM0283  AC23 HEK-293T C219(1.11)  LDD1522  [8]
 LDCM0284  AC24 HEK-293T C26(1.83)  LDD1523  [8]
 LDCM0286  AC26 HEK-293T C219(1.01)  LDD1525  [8]
 LDCM0287  AC27 HEK-293T C26(0.89); C161(1.00)  LDD1526  [8]
 LDCM0288  AC28 HEK-293T C219(1.11)  LDD1527  [8]
 LDCM0290  AC3 HEK-293T C26(0.66); C161(1.10)  LDD1529  [8]
 LDCM0292  AC31 HEK-293T C219(1.12)  LDD1531  [8]
 LDCM0293  AC32 HEK-293T C26(1.36)  LDD1532  [8]
 LDCM0295  AC34 HEK-293T C219(1.09)  LDD1534  [8]
 LDCM0296  AC35 HEK-293T C26(1.39); C161(1.03)  LDD1535  [8]
 LDCM0297  AC36 HEK-293T C219(1.12)  LDD1536  [8]
 LDCM0300  AC39 HEK-293T C219(1.41)  LDD1539  [8]
 LDCM0301  AC4 HEK-293T C219(1.29)  LDD1540  [8]
 LDCM0302  AC40 HEK-293T C26(1.87)  LDD1541  [8]
 LDCM0304  AC42 HEK-293T C219(0.93)  LDD1543  [8]
 LDCM0305  AC43 HEK-293T C26(1.51); C161(1.09)  LDD1544  [8]
 LDCM0306  AC44 HEK-293T C219(1.15)  LDD1545  [8]
 LDCM0309  AC47 HEK-293T C219(1.06)  LDD1548  [8]
 LDCM0310  AC48 HEK-293T C26(1.79)  LDD1549  [8]
 LDCM0313  AC50 HEK-293T C219(1.03)  LDD1552  [8]
 LDCM0314  AC51 HEK-293T C26(1.04); C161(1.02)  LDD1553  [8]
 LDCM0315  AC52 HEK-293T C219(0.93)  LDD1554  [8]
 LDCM0318  AC55 HEK-293T C219(1.08)  LDD1557  [8]
 LDCM0319  AC56 HEK-293T C26(1.65)  LDD1558  [8]
 LDCM0321  AC58 HEK-293T C219(1.05)  LDD1560  [8]
 LDCM0322  AC59 HEK-293T C26(1.04); C161(1.10)  LDD1561  [8]
 LDCM0324  AC60 HEK-293T C219(1.16)  LDD1563  [8]
 LDCM0327  AC63 HEK-293T C219(1.35)  LDD1566  [8]
 LDCM0328  AC64 HEK-293T C26(1.14)  LDD1567  [8]
 LDCM0334  AC7 HEK-293T C219(1.01)  LDD1568  [8]
 LDCM0345  AC8 HEK-293T C26(0.92)  LDD1569  [8]
 LDCM0275  AKOS034007705 HEK-293T C26(1.24)  LDD1514  [8]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [2]
 LDCM0369  CL100 HEK-293T C219(1.05)  LDD1573  [8]
 LDCM0371  CL102 HEK-293T C219(1.01)  LDD1575  [8]
 LDCM0373  CL104 HEK-293T C219(1.13)  LDD1577  [8]
 LDCM0375  CL106 HEK-293T C219(1.03)  LDD1579  [8]
 LDCM0377  CL108 HEK-293T C219(1.01)  LDD1581  [8]
 LDCM0379  CL11 HEK-293T C219(0.97)  LDD1583  [8]
 LDCM0380  CL110 HEK-293T C219(0.94)  LDD1584  [8]
 LDCM0382  CL112 HEK-293T C219(1.06)  LDD1586  [8]
 LDCM0384  CL114 HEK-293T C219(1.01)  LDD1588  [8]
 LDCM0386  CL116 HEK-293T C219(0.96)  LDD1590  [8]
 LDCM0388  CL118 HEK-293T C219(1.19)  LDD1592  [8]
 LDCM0390  CL12 HEK-293T C26(1.29)  LDD1594  [8]
 LDCM0391  CL120 HEK-293T C219(1.06)  LDD1595  [8]
 LDCM0393  CL122 HEK-293T C219(1.09)  LDD1597  [8]
 LDCM0395  CL124 HEK-293T C219(1.22)  LDD1599  [8]
 LDCM0397  CL126 HEK-293T C219(1.13)  LDD1601  [8]
 LDCM0399  CL128 HEK-293T C219(1.28)  LDD1603  [8]
 LDCM0401  CL14 HEK-293T C219(1.00)  LDD1605  [8]
 LDCM0403  CL16 HEK-293T C219(1.10)  LDD1607  [8]
 LDCM0405  CL18 HEK-293T C219(0.96)  LDD1609  [8]
 LDCM0406  CL19 HEK-293T C26(1.14); C161(0.92)  LDD1610  [8]
 LDCM0407  CL2 HEK-293T C219(1.09)  LDD1611  [8]
 LDCM0408  CL20 HEK-293T C219(1.15)  LDD1612  [8]
 LDCM0411  CL23 HEK-293T C219(1.05)  LDD1615  [8]
 LDCM0412  CL24 HEK-293T C26(1.32)  LDD1616  [8]
 LDCM0414  CL26 HEK-293T C219(1.09)  LDD1618  [8]
 LDCM0416  CL28 HEK-293T C219(1.10)  LDD1620  [8]
 LDCM0419  CL30 HEK-293T C219(0.99)  LDD1623  [8]
 LDCM0420  CL31 HEK-293T C26(1.05); C161(0.84)  LDD1624  [8]
 LDCM0421  CL32 HEK-293T C219(1.08)  LDD1625  [8]
 LDCM0424  CL35 HEK-293T C219(1.01)  LDD1628  [8]
 LDCM0425  CL36 HEK-293T C26(1.74)  LDD1629  [8]
 LDCM0429  CL4 HEK-293T C219(1.06)  LDD1633  [8]
 LDCM0430  CL40 HEK-293T C219(1.03)  LDD1634  [8]
 LDCM0432  CL42 HEK-293T C219(1.05)  LDD1636  [8]
 LDCM0433  CL43 HEK-293T C26(0.99); C161(0.96)  LDD1637  [8]
 LDCM0434  CL44 HEK-293T C219(1.01)  LDD1638  [8]
 LDCM0437  CL47 HEK-293T C219(1.04)  LDD1641  [8]
 LDCM0438  CL48 HEK-293T C26(2.05)  LDD1642  [8]
 LDCM0441  CL50 HEK-293T C219(1.19)  LDD1645  [8]
 LDCM0443  CL52 HEK-293T C219(1.14)  LDD1646  [8]
 LDCM0445  CL54 HEK-293T C219(1.02)  LDD1648  [8]
 LDCM0446  CL55 HEK-293T C26(1.14); C161(0.99)  LDD1649  [8]
 LDCM0447  CL56 HEK-293T C219(1.25)  LDD1650  [8]
 LDCM0450  CL59 HEK-293T C219(1.04)  LDD1653  [8]
 LDCM0451  CL6 HEK-293T C219(1.02)  LDD1654  [8]
 LDCM0452  CL60 HEK-293T C26(2.39)  LDD1655  [8]
 LDCM0454  CL62 HEK-293T C219(1.05)  LDD1657  [8]
 LDCM0456  CL64 HEK-293T C219(1.07)  LDD1659  [8]
 LDCM0458  CL66 HEK-293T C219(0.97)  LDD1661  [8]
 LDCM0459  CL67 HEK-293T C26(1.05); C161(0.93)  LDD1662  [8]
 LDCM0460  CL68 HEK-293T C219(1.03)  LDD1663  [8]
 LDCM0462  CL7 HEK-293T C26(0.78); C161(0.91)  LDD1665  [8]
 LDCM0464  CL71 HEK-293T C219(1.06)  LDD1667  [8]
 LDCM0465  CL72 HEK-293T C26(2.93)  LDD1668  [8]
 LDCM0467  CL74 HEK-293T C219(1.07)  LDD1670  [8]
 LDCM0469  CL76 HEK-293T C219(1.05)  LDD1672  [8]
 LDCM0471  CL78 HEK-293T C219(1.09)  LDD1674  [8]
 LDCM0472  CL79 HEK-293T C26(0.78); C161(0.90)  LDD1675  [8]
 LDCM0473  CL8 HEK-293T C219(0.94)  LDD1676  [8]
 LDCM0474  CL80 HEK-293T C219(1.21)  LDD1677  [8]
 LDCM0477  CL83 HEK-293T C219(1.14)  LDD1680  [8]
 LDCM0478  CL84 HEK-293T C26(1.18)  LDD1681  [8]
 LDCM0480  CL86 HEK-293T C219(1.12)  LDD1683  [8]
 LDCM0482  CL88 HEK-293T C219(1.21)  LDD1685  [8]
 LDCM0485  CL90 HEK-293T C219(0.92)  LDD1688  [8]
 LDCM0486  CL91 HEK-293T C26(1.09); C161(1.07)  LDD1689  [8]
 LDCM0487  CL92 HEK-293T C219(1.09)  LDD1690  [8]
 LDCM0490  CL95 HEK-293T C219(0.98)  LDD1693  [8]
 LDCM0491  CL96 HEK-293T C26(1.36)  LDD1694  [8]
 LDCM0493  CL98 HEK-293T C219(1.05)  LDD1696  [8]
 LDCM0427  Fragment51 HEK-293T C219(1.08)  LDD1631  [8]
 LDCM0022  KB02 HEK-293T C219(1.01)  LDD1492  [8]
 LDCM0023  KB03 HEK-293T C219(1.06)  LDD1497  [8]
 LDCM0024  KB05 UACC257 C231(1.26)  LDD3325  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
S-adenosyl-l-homocysteine Small molecular drug DB01752

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 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.
3 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
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 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
7 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
8 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402