Details of the Target

General Information of Target

Target ID LDTP01101
Target Name Microphthalmia-associated transcription factor (MITF)
Gene Name MITF
Gene ID 4286
Synonyms
BHLHE32; Microphthalmia-associated transcription factor; Class E basic helix-loop-helix protein 32; bHLHe32
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MQSESGIVPDFEVGEEFHEEPKTYYELKSQPLKSSSSAEHPGASKPPISSSSMTSRILLR
QQLMREQMQEQERREQQQKLQAAQFMQQRVPVSQTPAINVSVPTTLPSATQVPMEVLKVQ
THLENPTKYHIQQAQRQQVKQYLSTTLANKHANQVLSLPCPNQPGDHVMPPVPGSSAPNS
PMAMLTLNSNCEKEGFYKFEEQNRAESECPGMNTHSRASCMQMDDVIDDIISLESSYNEE
ILGLMDPALQMANTLPVSGNLIDLYGNQGLPPPGLTISNSCPANLPNIKRELTACIFPTE
SEARALAKERQKKDNHNLIERRRRFNINDRIKELGTLIPKSNDPDMRWNKGTILKASVDY
IRKLQREQQRAKELENRQKKLEHANRHLLLRIQELEMQARAHGLSLIPSTGLCSPDLVNR
IIKQEPVLENCSQDLLQHHADLTCTTTLDLTDGTITFNNNLGTGTEANQAYSVPTKMGSK
LEDILMDDTLSPVGVTDPLLSSVSPGASKTSSRRSSMSMEETEHTC
Target Bioclass
Transcription factor
Family
MiT/TFE family
Subcellular location
Nucleus
Function
Transcription factor that acts as a master regulator of melanocyte survival and differentiation as well as melanosome biogenesis. Binds to M-boxes (5'-TCATGTG-3') and symmetrical DNA sequences (E-boxes) (5'-CACGTG-3') found in the promoter of pigmentation genes, such as tyrosinase (TYR). Involved in the cellular response to amino acid availability by acting downstream of MTOR: in the presence of nutrients, MITF phosphorylation by MTOR promotes its inactivation. Upon starvation or lysosomal stress, inhibition of MTOR induces MITF dephosphorylation, resulting in transcription factor activity. Plays an important role in melanocyte development by regulating the expression of tyrosinase (TYR) and tyrosinase-related protein 1 (TYRP1). Plays a critical role in the differentiation of various cell types, such as neural crest-derived melanocytes, mast cells, osteoclasts and optic cup-derived retinal pigment epithelium.
Uniprot ID
O75030
Ensemble ID
ENST00000314557.10
HGNC ID
HGNC:7105
ChEMBL ID
CHEMBL1741165

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
FADU SNV: p.R370H .
HCC44 SNV: p.E66Ter .
MM1S SNV: p.Q311H .
MOLT4 SNV: p.E26K .
SW1783 SNV: p.R377Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C46(0.98)  LDD3314  [1]
AHL-Pu-1
 Probe Info  		C295(2.52)  LDD0170  [2]
Acrolein
 Probe Info  		N.A.  LDD0222  [3]
NAIA_4
 Probe Info  		C209(0.00); C295(0.00); C413(0.00)  LDD2226  [4]
NAIA_5
 Probe Info  		N.A.  LDD2224  [4]
IPM
 Probe Info  		N.A.  LDD0147  [5]
TFBX
 Probe Info  		N.A.  LDD0148  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C295(2.52)  LDD0170  [2]
 LDCM0026  4SU-RNA+native RNA DM93 C413(2.32); C295(3.83); C160(2.33)  LDD0171  [2]
 LDCM0270  AC15 HEK-293T C413(1.01)  LDD1513  [6]
 LDCM0283  AC23 HEK-293T C413(1.01)  LDD1522  [6]
 LDCM0292  AC31 HEK-293T C413(0.92)  LDD1531  [6]
 LDCM0300  AC39 HEK-293T C413(0.94)  LDD1539  [6]
 LDCM0309  AC47 HEK-293T C413(1.11)  LDD1548  [6]
 LDCM0318  AC55 HEK-293T C413(1.05)  LDD1557  [6]
 LDCM0327  AC63 HEK-293T C413(1.00)  LDD1566  [6]
 LDCM0334  AC7 HEK-293T C413(0.98)  LDD1568  [6]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [3]
 LDCM0632  CL-Sc Hep-G2 C413(1.22)  LDD2227  [4]
 LDCM0369  CL100 HEK-293T C413(1.07)  LDD1573  [6]
 LDCM0371  CL102 HEK-293T C413(0.87)  LDD1575  [6]
 LDCM0373  CL104 HEK-293T C413(0.98)  LDD1577  [6]
 LDCM0375  CL106 HEK-293T C413(0.96)  LDD1579  [6]
 LDCM0377  CL108 HEK-293T C413(1.33)  LDD1581  [6]
 LDCM0379  CL11 HEK-293T C413(0.99)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C413(0.84)  LDD1584  [6]
 LDCM0382  CL112 HEK-293T C413(1.08)  LDD1586  [6]
 LDCM0384  CL114 HEK-293T C413(0.85)  LDD1588  [6]
 LDCM0386  CL116 HEK-293T C413(0.91)  LDD1590  [6]
 LDCM0388  CL118 HEK-293T C413(0.96)  LDD1592  [6]
 LDCM0391  CL120 HEK-293T C413(1.04)  LDD1595  [6]
 LDCM0393  CL122 HEK-293T C413(0.96)  LDD1597  [6]
 LDCM0395  CL124 HEK-293T C413(1.05)  LDD1599  [6]
 LDCM0397  CL126 HEK-293T C413(0.79)  LDD1601  [6]
 LDCM0399  CL128 HEK-293T C413(1.05)  LDD1603  [6]
 LDCM0401  CL14 HEK-293T C413(0.83)  LDD1605  [6]
 LDCM0403  CL16 HEK-293T C413(0.94)  LDD1607  [6]
 LDCM0407  CL2 HEK-293T C413(0.85)  LDD1611  [6]
 LDCM0411  CL23 HEK-293T C413(1.05)  LDD1615  [6]
 LDCM0414  CL26 HEK-293T C413(0.83)  LDD1618  [6]
 LDCM0416  CL28 HEK-293T C413(1.13)  LDD1620  [6]
 LDCM0424  CL35 HEK-293T C413(0.99)  LDD1628  [6]
 LDCM0429  CL4 HEK-293T C413(1.01)  LDD1633  [6]
 LDCM0430  CL40 HEK-293T C413(1.03)  LDD1634  [6]
 LDCM0437  CL47 HEK-293T C413(0.97)  LDD1641  [6]
 LDCM0441  CL50 HEK-293T C413(0.78)  LDD1645  [6]
 LDCM0443  CL52 HEK-293T C413(1.05)  LDD1646  [6]
 LDCM0450  CL59 HEK-293T C413(1.03)  LDD1653  [6]
 LDCM0454  CL62 HEK-293T C413(0.92)  LDD1657  [6]
 LDCM0456  CL64 HEK-293T C413(0.89)  LDD1659  [6]
 LDCM0464  CL71 HEK-293T C413(1.03)  LDD1667  [6]
 LDCM0467  CL74 HEK-293T C413(0.77)  LDD1670  [6]
 LDCM0469  CL76 HEK-293T C413(1.01)  LDD1672  [6]
 LDCM0477  CL83 HEK-293T C413(1.00)  LDD1680  [6]
 LDCM0480  CL86 HEK-293T C413(0.99)  LDD1683  [6]
 LDCM0482  CL88 HEK-293T C413(1.09)  LDD1685  [6]
 LDCM0490  CL95 HEK-293T C413(0.99)  LDD1693  [6]
 LDCM0493  CL98 HEK-293T C413(0.69)  LDD1696  [6]
 LDCM0427  Fragment51 HEK-293T C413(0.80)  LDD1631  [6]
 LDCM0022  KB02 HEK-293T C413(0.96)  LDD1492  [6]
 LDCM0023  KB03 HEK-293T C413(0.99)  LDD1497  [6]
 LDCM0024  KB05 IGR37 C46(0.98)  LDD3314  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Clathrin heavy chain 1 (CLTC) Clathrin heavy chain family Q00610

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 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
3 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.
4 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
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 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