Details of the Target

General Information of Target

Target ID LDTP02509
Target Name Microtubule-associated protein tau (MAPT)
Gene Name MAPT
Gene ID 4137
Synonyms
MAPTL; MTBT1; TAU; Microtubule-associated protein tau; Neurofibrillary tangle protein; Paired helical filament-tau; PHF-tau
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAEPRQEFEVMEDHAGTYGLGDRKDQGGYTMHQDQEGDTDAGLKESPLQTPTEDGSEEPG
SETSDAKSTPTAEDVTAPLVDEGAPGKQAAAQPHTEIPEGTTAEEAGIGDTPSLEDEAAG
HVTQEPESGKVVQEGFLREPGPPGLSHQLMSGMPGAPLLPEGPREATRQPSGTGPEDTEG
GRHAPELLKHQLLGDLHQEGPPLKGAGGKERPGSKEEVDEDRDVDESSPQDSPPSKASPA
QDGRPPQTAAREATSIPGFPAEGAIPLPVDFLSKVSTEIPASEPDGPSVGRAKGQDAPLE
FTFHVEITPNVQKEQAHSEEHLGRAAFPGAPGEGPEARGPSLGEDTKEADLPEPSEKQPA
AAPRGKPVSRVPQLKARMVSKSKDGTGSDDKKAKTSTRSSAKTLKNRPCLSPKHPTPGSS
DPLIQPSSPAVCPEPPSSPKYVSSVTSRTGSSGAKEMKLKGADGKTKIATPRGAAPPGQK
GQANATRIPAKTPPAPKTPPSSGEPPKSGDRSGYSSPGSPGTPGSRSRTPSLPTPPTREP
KKVAVVRTPPKSPSSAKSRLQTAPVPMPDLKNVKSKIGSTENLKHQPGGGKVQIINKKLD
LSNVQSKCGSKDNIKHVPGGGSVQIVYKPVDLSKVTSKCGSLGNIHHKPGGGQVEVKSEK
LDFKDRVQSKIGSLDNITHVPGGGNKKIETHKLTFRENAKAKTDHGAEIVYKSPVVSGDT
SPRHLSNVSSTGSIDMVDSPQLATLADEVSASLAKQGL
Target Type
Clinical trial
Target Bioclass
Other
Subcellular location
Cytoplasm, cytosol
Function
Promotes microtubule assembly and stability, and might be involved in the establishment and maintenance of neuronal polarity. The C-terminus binds axonal microtubules while the N-terminus binds neural plasma membrane components, suggesting that tau functions as a linker protein between both. Axonal polarity is predetermined by TAU/MAPT localization (in the neuronal cell) in the domain of the cell body defined by the centrosome. The short isoforms allow plasticity of the cytoskeleton whereas the longer isoforms may preferentially play a role in its stabilization.
TTD ID
T45593
Uniprot ID
P10636
DrugMap ID
TTXZCO0
Ensemble ID
ENST00000334239.12
HGNC ID
HGNC:6893
ChEMBL ID
CHEMBL1293224

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info  		Y29(25.12); Y514(24.07)  LDD3495  [1]
DBIA
 Probe Info  		C657(3.65)  LDD3423  [2]
HHS-465
 Probe Info  		Y711(4.27)  LDD2237  [3]
5E-2FA
 Probe Info  		H679(0.00); H585(0.00)  LDD2235  [4]
m-APA
 Probe Info  		N.A.  LDD2231  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [5]
IPM
 Probe Info  		N.A.  LDD0005  [6]
Phosphinate-6
 Probe Info  		C608(0.00); C639(0.00)  LDD0018  [7]
AOyne
 Probe Info  		15.00  LDD0443  [8]
NAIA_5
 Probe Info  		C608(0.00); C639(0.00)  LDD2223  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C639(1.35)  LDD1507  [10]
 LDCM0226  AC11 HEK-293T C409(1.06)  LDD1509  [10]
 LDCM0237  AC12 HEK-293T C409(1.07)  LDD1510  [10]
 LDCM0270  AC15 HEK-293T C639(1.15); C409(1.06)  LDD1513  [10]
 LDCM0276  AC17 HEK-293T C639(1.31)  LDD1515  [10]
 LDCM0278  AC19 HEK-293T C409(2.82)  LDD1517  [10]
 LDCM0280  AC20 HEK-293T C409(1.10)  LDD1519  [10]
 LDCM0281  AC21 HEK-293T C639(1.10); C409(1.01)  LDD1520  [10]
 LDCM0283  AC23 HEK-293T C639(1.07); C409(0.95)  LDD1522  [10]
 LDCM0284  AC24 HEK-293T C409(0.95)  LDD1523  [10]
 LDCM0285  AC25 HEK-293T C639(1.26)  LDD1524  [10]
 LDCM0287  AC27 HEK-293T C409(1.06)  LDD1526  [10]
 LDCM0288  AC28 HEK-293T C409(1.05)  LDD1527  [10]
 LDCM0289  AC29 HEK-293T C639(1.07); C409(1.05)  LDD1528  [10]
 LDCM0290  AC3 HEK-293T C409(0.99)  LDD1529  [10]
 LDCM0292  AC31 HEK-293T C639(0.97); C409(1.01)  LDD1531  [10]
 LDCM0293  AC32 HEK-293T C409(0.98)  LDD1532  [10]
 LDCM0294  AC33 HEK-293T C639(1.33)  LDD1533  [10]
 LDCM0296  AC35 HEK-293T C409(0.98)  LDD1535  [10]
 LDCM0297  AC36 HEK-293T C409(1.07)  LDD1536  [10]
 LDCM0298  AC37 HEK-293T C639(1.00); C409(0.99)  LDD1537  [10]
 LDCM0300  AC39 HEK-293T C639(1.07); C409(1.09)  LDD1539  [10]
 LDCM0301  AC4 HEK-293T C409(1.02)  LDD1540  [10]
 LDCM0302  AC40 HEK-293T C409(0.95)  LDD1541  [10]
 LDCM0303  AC41 HEK-293T C639(1.36)  LDD1542  [10]
 LDCM0305  AC43 HEK-293T C409(1.06)  LDD1544  [10]
 LDCM0306  AC44 HEK-293T C409(1.04)  LDD1545  [10]
 LDCM0307  AC45 HEK-293T C639(1.16); C409(1.04)  LDD1546  [10]
 LDCM0309  AC47 HEK-293T C639(1.20); C409(1.11)  LDD1548  [10]
 LDCM0310  AC48 HEK-293T C409(0.92)  LDD1549  [10]
 LDCM0311  AC49 HEK-293T C639(1.42)  LDD1550  [10]
 LDCM0312  AC5 HEK-293T C639(1.01); C409(1.03)  LDD1551  [10]
 LDCM0314  AC51 HEK-293T C409(0.98)  LDD1553  [10]
 LDCM0315  AC52 HEK-293T C409(1.06)  LDD1554  [10]
 LDCM0316  AC53 HEK-293T C639(1.15); C409(1.04)  LDD1555  [10]
 LDCM0318  AC55 HEK-293T C639(1.09); C409(1.13)  LDD1557  [10]
 LDCM0319  AC56 HEK-293T C409(1.01)  LDD1558  [10]
 LDCM0320  AC57 HEK-293T C639(1.22)  LDD1559  [10]
 LDCM0322  AC59 HEK-293T C409(1.01)  LDD1561  [10]
 LDCM0324  AC60 HEK-293T C409(1.02)  LDD1563  [10]
 LDCM0325  AC61 HEK-293T C639(1.08); C409(1.09)  LDD1564  [10]
 LDCM0327  AC63 HEK-293T C639(0.99); C409(1.03)  LDD1566  [10]
 LDCM0328  AC64 HEK-293T C409(1.00)  LDD1567  [10]
 LDCM0334  AC7 HEK-293T C639(1.05); C409(0.99)  LDD1568  [10]
 LDCM0345  AC8 HEK-293T C409(1.03)  LDD1569  [10]
 LDCM0248  AKOS034007472 HEK-293T C639(1.12); C409(1.03)  LDD1511  [10]
 LDCM0356  AKOS034007680 HEK-293T C639(1.47)  LDD1570  [10]
 LDCM0275  AKOS034007705 HEK-293T C409(1.09)  LDD1514  [10]
 LDCM0632  CL-Sc Hep-G2 C639(1.34)  LDD2227  [9]
 LDCM0369  CL100 HEK-293T C639(1.27)  LDD1573  [10]
 LDCM0371  CL102 HEK-293T C639(1.16)  LDD1575  [10]
 LDCM0373  CL104 HEK-293T C639(1.30)  LDD1577  [10]
 LDCM0375  CL106 HEK-293T C639(1.16)  LDD1579  [10]
 LDCM0377  CL108 HEK-293T C639(1.28)  LDD1581  [10]
 LDCM0379  CL11 HEK-293T C639(0.98); C409(0.97)  LDD1583  [10]
 LDCM0380  CL110 HEK-293T C639(1.20)  LDD1584  [10]
 LDCM0382  CL112 HEK-293T C639(1.46)  LDD1586  [10]
 LDCM0384  CL114 HEK-293T C639(1.33)  LDD1588  [10]
 LDCM0386  CL116 HEK-293T C639(1.31)  LDD1590  [10]
 LDCM0388  CL118 HEK-293T C639(1.30)  LDD1592  [10]
 LDCM0390  CL12 HEK-293T C409(1.10)  LDD1594  [10]
 LDCM0391  CL120 HEK-293T C639(1.22)  LDD1595  [10]
 LDCM0393  CL122 HEK-293T C639(1.23)  LDD1597  [10]
 LDCM0395  CL124 HEK-293T C639(1.31)  LDD1599  [10]
 LDCM0397  CL126 HEK-293T C639(0.97)  LDD1601  [10]
 LDCM0399  CL128 HEK-293T C639(1.26)  LDD1603  [10]
 LDCM0401  CL14 HEK-293T C639(1.15)  LDD1605  [10]
 LDCM0403  CL16 HEK-293T C639(1.23)  LDD1607  [10]
 LDCM0404  CL17 HEK-293T C639(1.13)  LDD1608  [10]
 LDCM0406  CL19 HEK-293T C409(1.08)  LDD1610  [10]
 LDCM0407  CL2 HEK-293T C639(1.10)  LDD1611  [10]
 LDCM0408  CL20 HEK-293T C409(1.06)  LDD1612  [10]
 LDCM0409  CL21 HEK-293T C639(1.17); C409(1.14)  LDD1613  [10]
 LDCM0411  CL23 HEK-293T C639(1.02); C409(1.03)  LDD1615  [10]
 LDCM0412  CL24 HEK-293T C409(1.06)  LDD1616  [10]
 LDCM0414  CL26 HEK-293T C639(1.09)  LDD1618  [10]
 LDCM0416  CL28 HEK-293T C639(1.19)  LDD1620  [10]
 LDCM0417  CL29 HEK-293T C639(1.14)  LDD1621  [10]
 LDCM0420  CL31 HEK-293T C409(1.13)  LDD1624  [10]
 LDCM0421  CL32 HEK-293T C409(1.12)  LDD1625  [10]
 LDCM0422  CL33 HEK-293T C639(1.04); C409(1.04)  LDD1626  [10]
 LDCM0424  CL35 HEK-293T C639(1.07); C409(1.07)  LDD1628  [10]
 LDCM0425  CL36 HEK-293T C409(0.98)  LDD1629  [10]
 LDCM0429  CL4 HEK-293T C639(1.02)  LDD1633  [10]
 LDCM0430  CL40 HEK-293T C639(1.24)  LDD1634  [10]
 LDCM0431  CL41 HEK-293T C639(1.17)  LDD1635  [10]
 LDCM0433  CL43 HEK-293T C409(1.01)  LDD1637  [10]
 LDCM0434  CL44 HEK-293T C409(1.06)  LDD1638  [10]
 LDCM0435  CL45 HEK-293T C639(1.14); C409(1.16)  LDD1639  [10]
 LDCM0437  CL47 HEK-293T C639(1.01); C409(1.06)  LDD1641  [10]
 LDCM0438  CL48 HEK-293T C409(0.96)  LDD1642  [10]
 LDCM0440  CL5 HEK-293T C639(1.06)  LDD1644  [10]
 LDCM0441  CL50 HEK-293T C639(1.28)  LDD1645  [10]
 LDCM0443  CL52 HEK-293T C639(1.24)  LDD1646  [10]
 LDCM0444  CL53 HEK-293T C639(1.23)  LDD1647  [10]
 LDCM0446  CL55 HEK-293T C409(0.99)  LDD1649  [10]
 LDCM0447  CL56 HEK-293T C409(1.10)  LDD1650  [10]
 LDCM0448  CL57 HEK-293T C639(1.23); C409(1.40)  LDD1651  [10]
 LDCM0450  CL59 HEK-293T C639(1.10); C409(1.14)  LDD1653  [10]
 LDCM0452  CL60 HEK-293T C409(1.04)  LDD1655  [10]
 LDCM0454  CL62 HEK-293T C639(1.26)  LDD1657  [10]
 LDCM0456  CL64 HEK-293T C639(1.26)  LDD1659  [10]
 LDCM0457  CL65 HEK-293T C639(1.31)  LDD1660  [10]
 LDCM0459  CL67 HEK-293T C409(1.07)  LDD1662  [10]
 LDCM0460  CL68 HEK-293T C409(1.05)  LDD1663  [10]
 LDCM0461  CL69 HEK-293T C639(1.24); C409(1.02)  LDD1664  [10]
 LDCM0462  CL7 HEK-293T C409(1.00)  LDD1665  [10]
 LDCM0464  CL71 HEK-293T C639(1.03); C409(1.13)  LDD1667  [10]
 LDCM0465  CL72 HEK-293T C409(0.98)  LDD1668  [10]
 LDCM0467  CL74 HEK-293T C639(1.23)  LDD1670  [10]
 LDCM0469  CL76 HEK-293T C639(1.27)  LDD1672  [10]
 LDCM0470  CL77 HEK-293T C639(1.17)  LDD1673  [10]
 LDCM0472  CL79 HEK-293T C409(1.00)  LDD1675  [10]
 LDCM0473  CL8 HEK-293T C409(0.96)  LDD1676  [10]
 LDCM0474  CL80 HEK-293T C409(1.01)  LDD1677  [10]
 LDCM0475  CL81 HEK-293T C639(1.23); C409(1.04)  LDD1678  [10]
 LDCM0477  CL83 HEK-293T C639(0.98); C409(1.06)  LDD1680  [10]
 LDCM0478  CL84 HEK-293T C409(0.94)  LDD1681  [10]
 LDCM0480  CL86 HEK-293T C639(1.01)  LDD1683  [10]
 LDCM0482  CL88 HEK-293T C639(1.21)  LDD1685  [10]
 LDCM0483  CL89 HEK-293T C639(1.06)  LDD1686  [10]
 LDCM0484  CL9 HEK-293T C639(1.11); C409(0.96)  LDD1687  [10]
 LDCM0486  CL91 HEK-293T C409(0.96)  LDD1689  [10]
 LDCM0487  CL92 HEK-293T C409(1.06)  LDD1690  [10]
 LDCM0488  CL93 HEK-293T C639(1.17); C409(1.06)  LDD1691  [10]
 LDCM0490  CL95 HEK-293T C639(1.02); C409(1.22)  LDD1693  [10]
 LDCM0491  CL96 HEK-293T C409(0.94)  LDD1694  [10]
 LDCM0493  CL98 HEK-293T C639(1.29)  LDD1696  [10]
 LDCM0427  Fragment51 HEK-293T C639(1.06)  LDD1631  [10]
 LDCM0022  KB02 HEK-293T C639(1.02)  LDD1492  [10]
 LDCM0023  KB03 HEK-293T C639(0.99)  LDD1497  [10]
 LDCM0024  KB05 SK-ES1 C657(3.65)  LDD3423  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nucleolar RNA helicase 2 (DDX21) DEAD box helicase family Q9NR30
Probable ATP-dependent RNA helicase DDX6 (DDX6) DEAD box helicase family P26196
Heat shock cognate 71 kDa protein (HSPA8) Heat shock protein 70 family P11142
Calpain-10 (CAPN10) Peptidase C2 family Q9HC96
Serine protease HTRA1 (HTRA1) Peptidase S1C family Q92743
RAC-alpha serine/threonine-protein kinase (AKT1) AGC Ser/Thr protein kinase family P31749
Glycogen synthase kinase-3 beta (GSK3B) CMGC Ser/Thr protein kinase family P49841
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tubulin alpha-1A chain (TUBA1A) Tubulin family Q71U36
E3 ubiquitin-protein ligase CHIP (STUB1) . Q9UNE7
Peptidyl-prolyl cis-trans isomerase FKBP5 (FKBP5) . Q13451
Transporter and channel
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Annexin A2 (ANXA2) Annexin family P07355
Annexin A6 (ANXA6) Annexin family P08133
Apolipoprotein E (APOE) Apolipoprotein A1/A4/E family P02649
Amyloid-beta precursor protein (APP) APP family P05067
Excitatory amino acid transporter 2 (SLC1A2) Dicarboxylate/amino acid:cation symporter (DAACS) family P43004
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Major prion protein (PRNP) Prion family P04156
Alpha-synuclein (SNCA) Synuclein family P37840
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger homeobox protein 2 (ZFHX2) . Q9C0A1
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein sigma (SFN) 14-3-3 family P31947
Dynactin subunit 1 (DCTN1) Dynactin 150 kDa subunit family Q14203
Large ribosomal subunit protein eL28 (RPL28) Eukaryotic ribosomal protein eL28 family P46779
Microtubule-associated protein RP/EB family member 3 (MAPRE3) MAPRE family Q9UPY8
RNA-binding protein Musashi homolog 1 (MSI1) Musashi family O43347
RNA-binding protein Musashi homolog 2 (MSI2) Musashi family Q96DH6
Microtubule-associated protein tau (MAPT) . P10636
Placental protein 13-like (LGALS14) . Q8TCE9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Astemizole Small molecular drug DB00637
Docetaxel Small molecular drug DB01248
Lansoprazole Small molecular drug DB00448
Paclitaxel Small molecular drug DB01229
Flortaucipir F-18 . DB14914
Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Trx0237 Small molecular drug D5FSV8
Davunetide . D0V1FF
Lmt-x . D05XDZ
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pbt-2 Small molecular drug D00GXL
Tau-binding Pet Tracer Small molecular drug D02IJA
Biib092 . D0I8FS
Rg6100 . D01EJG
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly3303560 . D02DZK
Pti-80 . D0P8YJ
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Al-408 . D0D2GZ
Blv-0703 . D0T9PL
Ni-105 . D03LGX

References

1 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
2 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
3 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
4 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
5 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
6 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
7 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
8 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
9 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
10 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