Details of the Target

General Information of Target

Target ID LDTP02468
Target Name Transcriptional activator GLI3 (GLI3)
Gene Name GLI3
Gene ID 2737
Synonyms
Transcriptional activator GLI3; GLI3 form of 190 kDa; GLI3-190; GLI3 full-length protein; GLI3FL) [Cleaved into: Transcriptional repressor GLI3R; GLI3 C-terminally truncated form; GLI3 form of 83 kDa; GLI3-83)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEAQSHSSTTTEKKKVENSIVKCSTRTDVSEKAVASSTTSNEDESPGQTYHRERRNAITM
QPQNVQGLSKVSEEPSTSSDERASLIKKEIHGSLPHVAEPSVPYRGTVFAMDPRNGYMEP
HYHPPHLFPAFHPPVPIDARHHEGRYHYDPSPIPPLHMTSALSSSPTYPDLPFIRISPHR
NPTAASESPFSPPHPYINPYMDYIRSLHSSPSLSMISATRGLSPTDAPHAGVSPAEYYHQ
MALLTGQRSPYADIIPSAATAGTGAIHMEYLHAMDSTRFSSPRLSARPSRKRTLSISPLS
DHSFDLQTMIRTSPNSLVTILNNSRSSSSASGSYGHLSASAISPALSFTYSSAPVSLHMH
QQILSRQQSLGSAFGHSPPLIHPAPTFPTQRPIPGIPTVLNPVQVSSGPSESSQNKPTSE
SAVSSTGDPMHNKRSKIKPDEDLPSPGARGQQEQPEGTTLVKEEGDKDESKQEPEVIYET
NCHWEGCAREFDTQEQLVHHINNDHIHGEKKEFVCRWLDCSREQKPFKAQYMLVVHMRRH
TGEKPHKCTFEGCTKAYSRLENLKTHLRSHTGEKPYVCEHEGCNKAFSNASDRAKHQNRT
HSNEKPYVCKIPGCTKRYTDPSSLRKHVKTVHGPEAHVTKKQRGDIHPRPPPPRDSGSHS
QSRSPGRPTQGALGEQQDLSNTTSKREECLQVKTVKAEKPMTSQPSPGGQSSCSSQQSPI
SNYSNSGLELPLTDGGSIGDLSAIDETPIMDSTISTATTALALQARRNPAGTKWMEHVKL
ERLKQVNGMFPRLNPILPPKAPAVSPLIGNGTQSNNTCSLGGPMTLLPGRSDLSGVDVTM
LNMLNRRDSSASTISSAYLSSRRSSGISPCFSSRRSSEASQAEGRPQNVSVADSYDPIST
DASRRSSEASQSDGLPSLLSLTPAQQYRLKAKYAAATGGPPPTPLPNMERMSLKTRLALL
GDALEPGVALPPVHAPRRCSDGGAHGYGRRHLQPHDAPGHGVRRASDPVRTGSEGLALPR
VPRFSSLSSCNPPAMATSAEKRSLVLQNYTRPEGGQSRNFHSSPCPPSITENVTLESLTM
DADANLNDEDFLPDDVVQYLNSQNQAGYEQHFPSALPDDSKVPHGPGDFDAPGLPDSHAG
QQFHALEQPCPEGSKTDLPIQWNEVSSGSADLSSSKLKCGPRPAVPQTRAFGFCNGMVVH
PQNPLRSGPAGGYQTLGENSNPYGGPEHLMLHNSPGSGTSGNAFHEQPCKAPQYGNCLNR
QPVAPGALDGACGAGIQASKLKSTPMQGSGGQLNFGLPVAPNESAGSMVNGMQNQDPVGQ
GYLAHQLLGDSMQHPGAGRPGQQMLGQISATSHINIYQGPESCLPGAHGMGSQPSSLAVV
RGYQPCASFGGSRRQAMPRDSLALQSGQLSDTSQTCRVNGIKMEMKGQPHPLCSNLQNYS
GQFYDQTVGFSQQDTKAGSFSISDASCLLQGTSAKNSELLSPGANQVTSTVDSLDSHDLE
GVQIDFDAIIDDGDHSSLMSGALSPSIIQNLSHSSSRLTTPRASLPFPALSMSTTNMAIG
DMSSLLTSLAEESKFLAVMQ
Target Bioclass
Transcription factor
Family
GLI C2H2-type zinc-finger protein family
Subcellular location
Nucleus
Function
Has a dual function as a transcriptional activator and a repressor of the sonic hedgehog (Shh) pathway, and plays a role in limb development. The full-length GLI3 form (GLI3FL) after phosphorylation and nuclear translocation, acts as an activator (GLI3A) while GLI3R, its C-terminally truncated form, acts as a repressor. A proper balance between the GLI3 activator and the repressor GLI3R, rather than the repressor gradient itself or the activator/repressor ratio gradient, specifies limb digit number and identity. In concert with TRPS1, plays a role in regulating the size of the zone of distal chondrocytes, in restricting the zone of PTHLH expression in distal cells and in activating chondrocyte proliferation. Binds to the minimal GLI-consensus sequence 5'-GGGTGGTC-3'.
Uniprot ID
P10071
Ensemble ID
ENST00000395925.8
HGNC ID
HGNC:4319

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  		C870(0.92)  LDD0078  [1]
TFBX
 Probe Info  		N.A.  LDD0027  [2]
IPM
 Probe Info  		C1416(0.00); C1272(0.00); C1257(0.00); C870(0.00)  LDD2156  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0237  AC12 HEK-293T C1386(1.11)  LDD1510  [4]
 LDCM0259  AC14 HEK-293T C1257(0.91)  LDD1512  [4]
 LDCM0280  AC20 HEK-293T C1386(1.52)  LDD1519  [4]
 LDCM0282  AC22 HEK-293T C1257(0.65)  LDD1521  [4]
 LDCM0284  AC24 HEK-293T C1257(0.73)  LDD1523  [4]
 LDCM0288  AC28 HEK-293T C1386(1.50)  LDD1527  [4]
 LDCM0291  AC30 HEK-293T C1257(0.92)  LDD1530  [4]
 LDCM0293  AC32 HEK-293T C1257(1.30)  LDD1532  [4]
 LDCM0297  AC36 HEK-293T C1386(1.26)  LDD1536  [4]
 LDCM0299  AC38 HEK-293T C1257(0.64)  LDD1538  [4]
 LDCM0301  AC4 HEK-293T C1386(0.87)  LDD1540  [4]
 LDCM0302  AC40 HEK-293T C1257(0.95)  LDD1541  [4]
 LDCM0306  AC44 HEK-293T C1386(1.66)  LDD1545  [4]
 LDCM0308  AC46 HEK-293T C1257(1.28)  LDD1547  [4]
 LDCM0310  AC48 HEK-293T C1257(0.95)  LDD1549  [4]
 LDCM0315  AC52 HEK-293T C1386(1.12)  LDD1554  [4]
 LDCM0317  AC54 HEK-293T C1257(1.01)  LDD1556  [4]
 LDCM0319  AC56 HEK-293T C1257(1.29)  LDD1558  [4]
 LDCM0323  AC6 HEK-293T C1257(0.89)  LDD1562  [4]
 LDCM0324  AC60 HEK-293T C1386(1.17)  LDD1563  [4]
 LDCM0326  AC62 HEK-293T C1257(0.77)  LDD1565  [4]
 LDCM0328  AC64 HEK-293T C1257(1.26)  LDD1567  [4]
 LDCM0345  AC8 HEK-293T C1257(0.95)  LDD1569  [4]
 LDCM0275  AKOS034007705 HEK-293T C1257(0.92)  LDD1514  [4]
 LDCM0020  ARS-1620 HCC44 C870(0.92)  LDD0078  [1]
 LDCM0367  CL1 HEK-293T C689(0.96); C1467(0.83)  LDD1571  [4]
 LDCM0368  CL10 HEK-293T C1257(0.84)  LDD1572  [4]
 LDCM0369  CL100 HEK-293T C1467(0.72); C1386(1.03)  LDD1573  [4]
 LDCM0370  CL101 HEK-293T C689(1.11); C1467(0.80)  LDD1574  [4]
 LDCM0371  CL102 HEK-293T C1257(0.84); C1467(1.06)  LDD1575  [4]
 LDCM0373  CL104 HEK-293T C1467(1.11); C1386(1.24)  LDD1577  [4]
 LDCM0374  CL105 HEK-293T C689(0.97); C1467(0.91)  LDD1578  [4]
 LDCM0375  CL106 HEK-293T C1257(1.21); C1467(1.16)  LDD1579  [4]
 LDCM0377  CL108 HEK-293T C1467(1.36); C1386(1.02)  LDD1581  [4]
 LDCM0378  CL109 HEK-293T C689(1.02); C1467(0.89)  LDD1582  [4]
 LDCM0380  CL110 HEK-293T C1257(1.12); C1467(1.00)  LDD1584  [4]
 LDCM0382  CL112 HEK-293T C1467(0.90); C1386(0.92)  LDD1586  [4]
 LDCM0383  CL113 HEK-293T C689(1.03); C1467(0.81)  LDD1587  [4]
 LDCM0384  CL114 HEK-293T C1257(1.01); C1467(0.87)  LDD1588  [4]
 LDCM0386  CL116 HEK-293T C1467(0.91); C1386(0.98)  LDD1590  [4]
 LDCM0387  CL117 HEK-293T C689(0.98); C1467(0.90)  LDD1591  [4]
 LDCM0388  CL118 HEK-293T C1257(1.02); C1467(0.92)  LDD1592  [4]
 LDCM0390  CL12 HEK-293T C1257(0.88)  LDD1594  [4]
 LDCM0391  CL120 HEK-293T C1467(0.94); C1386(0.92)  LDD1595  [4]
 LDCM0392  CL121 HEK-293T C689(0.97); C1467(0.89)  LDD1596  [4]
 LDCM0393  CL122 HEK-293T C1257(1.01); C1467(0.91)  LDD1597  [4]
 LDCM0395  CL124 HEK-293T C1467(0.82); C1386(0.82)  LDD1599  [4]
 LDCM0396  CL125 HEK-293T C689(0.91); C1467(1.05)  LDD1600  [4]
 LDCM0397  CL126 HEK-293T C1257(0.73); C1467(1.19)  LDD1601  [4]
 LDCM0399  CL128 HEK-293T C1467(0.87); C1386(0.98)  LDD1603  [4]
 LDCM0400  CL13 HEK-293T C689(1.07); C1467(1.30)  LDD1604  [4]
 LDCM0401  CL14 HEK-293T C1257(0.75); C1467(1.11)  LDD1605  [4]
 LDCM0403  CL16 HEK-293T C1467(1.11); C1386(1.06)  LDD1607  [4]
 LDCM0407  CL2 HEK-293T C1257(0.84); C1467(1.12)  LDD1611  [4]
 LDCM0408  CL20 HEK-293T C1386(1.32)  LDD1612  [4]
 LDCM0410  CL22 HEK-293T C1257(0.94)  LDD1614  [4]
 LDCM0412  CL24 HEK-293T C1257(0.86)  LDD1616  [4]
 LDCM0413  CL25 HEK-293T C689(0.82); C1467(0.83)  LDD1617  [4]
 LDCM0414  CL26 HEK-293T C1257(0.72); C1467(0.92)  LDD1618  [4]
 LDCM0416  CL28 HEK-293T C1467(1.13); C1386(0.95)  LDD1620  [4]
 LDCM0421  CL32 HEK-293T C1386(2.09)  LDD1625  [4]
 LDCM0423  CL34 HEK-293T C1257(0.85)  LDD1627  [4]
 LDCM0425  CL36 HEK-293T C1257(1.04)  LDD1629  [4]
 LDCM0426  CL37 HEK-293T C689(0.98); C1467(0.89)  LDD1630  [4]
 LDCM0429  CL4 HEK-293T C1467(1.12); C1386(1.32)  LDD1633  [4]
 LDCM0430  CL40 HEK-293T C1467(0.84); C1386(0.93)  LDD1634  [4]
 LDCM0434  CL44 HEK-293T C1386(1.72)  LDD1638  [4]
 LDCM0436  CL46 HEK-293T C1257(1.12)  LDD1640  [4]
 LDCM0438  CL48 HEK-293T C1257(0.96)  LDD1642  [4]
 LDCM0439  CL49 HEK-293T C689(1.01); C1467(0.90)  LDD1643  [4]
 LDCM0441  CL50 HEK-293T C1257(0.82); C1467(0.97)  LDD1645  [4]
 LDCM0443  CL52 HEK-293T C1467(1.16); C1386(1.10)  LDD1646  [4]
 LDCM0447  CL56 HEK-293T C1386(1.13)  LDD1650  [4]
 LDCM0449  CL58 HEK-293T C1257(1.09)  LDD1652  [4]
 LDCM0452  CL60 HEK-293T C1257(1.02)  LDD1655  [4]
 LDCM0453  CL61 HEK-293T C689(0.84); C1467(0.87)  LDD1656  [4]
 LDCM0454  CL62 HEK-293T C1257(0.84); C1467(1.07)  LDD1657  [4]
 LDCM0456  CL64 HEK-293T C1467(0.90); C1386(0.98)  LDD1659  [4]
 LDCM0460  CL68 HEK-293T C1386(1.56)  LDD1663  [4]
 LDCM0463  CL70 HEK-293T C1257(0.93)  LDD1666  [4]
 LDCM0465  CL72 HEK-293T C1257(0.91)  LDD1668  [4]
 LDCM0466  CL73 HEK-293T C689(0.85); C1467(0.89)  LDD1669  [4]
 LDCM0467  CL74 HEK-293T C1257(0.86); C1467(0.90)  LDD1670  [4]
 LDCM0469  CL76 HEK-293T C1467(0.77); C1386(0.96)  LDD1672  [4]
 LDCM0473  CL8 HEK-293T C1386(1.20)  LDD1676  [4]
 LDCM0474  CL80 HEK-293T C1386(1.36)  LDD1677  [4]
 LDCM0476  CL82 HEK-293T C1257(0.69)  LDD1679  [4]
 LDCM0478  CL84 HEK-293T C1257(1.17)  LDD1681  [4]
 LDCM0479  CL85 HEK-293T C689(0.81); C1467(0.93)  LDD1682  [4]
 LDCM0480  CL86 HEK-293T C1257(1.10); C1467(0.90)  LDD1683  [4]
 LDCM0482  CL88 HEK-293T C1467(1.05); C1386(0.99)  LDD1685  [4]
 LDCM0487  CL92 HEK-293T C1386(1.75)  LDD1690  [4]
 LDCM0489  CL94 HEK-293T C1257(0.70)  LDD1692  [4]
 LDCM0491  CL96 HEK-293T C1257(0.90)  LDD1694  [4]
 LDCM0492  CL97 HEK-293T C689(0.87); C1467(0.86)  LDD1695  [4]
 LDCM0493  CL98 HEK-293T C1257(0.88); C1467(0.74)  LDD1696  [4]
 LDCM0427  Fragment51 HEK-293T C1257(0.93); C1467(1.04)  LDD1631  [4]
 LDCM0022  KB02 A-375 C1467(1.38)  LDD2255  [5]
 LDCM0023  KB03 A101D C1467(2.24)  LDD2667  [5]
 LDCM0024  KB05 ONS-76 C1467(1.78)  LDD3376  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein EMX1 (EMX1) EMX homeobox family Q04741
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Suppressor of fused homolog (SUFU) SUFU family Q9UMX1
WD repeat-containing protein 11 (WDR11) . Q9BZH6

References

1 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.
2 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
3 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
4 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
5 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