General Information of Target

Target ID LDTP01425
Target Name Tubulin polymerization-promoting protein (TPPP)
Gene Name TPPP
Gene ID 11076
Synonyms
TPPP1; Tubulin polymerization-promoting protein; TPPP; EC 3.6.5.-; 25 kDa brain-specific protein; TPPP/p25; p24; p25-alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MADKAKPAKAANRTPPKSPGDPSKDRAAKRLSLESEGAGEGAAASPELSALEEAFRRFAV
HGDARATGREMHGKNWSKLCKDCQVIDGRNVTVTDVDIVFSKIKGKSCRTITFEQFQEAL
EELAKKRFKDKSSEEAVREVHRLIEGKAPIISGVTKAISSPTVSRLTDTTKFTGSHKERF
DPSGKGKGKAGRVDLVDESGYVSGYKHAGTYDQKVQGGK
Target Bioclass
Enzyme
Family
TPPP family
Subcellular location
Golgi outpost
Function
Regulator of microtubule dynamics that plays a key role in myelination by promoting elongation of the myelin sheath. Acts as a microtubule nucleation factor in oligodendrocytes: specifically localizes to the postsynaptic Golgi apparatus region, also named Golgi outpost, and promotes microtubule nucleation, an important step for elongation of the myelin sheath. Required for both uniform polarized growth of distal microtubules as well as directing the branching of proximal processes. Shows magnesium-dependent GTPase activity; the role of the GTPase activity is unclear. In addition to microtubule nucleation activity, also involved in microtubule bundling and stabilization of existing microtubules, thereby maintaining the integrity of the microtubule network. Regulates microtubule dynamics by promoting tubulin acetylation: acts by inhibiting the tubulin deacetylase activity of HDAC6. Also regulates cell migration: phosphorylation by ROCK1 inhibits interaction with HDAC6, resulting in decreased acetylation of tubulin and increased cell motility. Plays a role in cell proliferation by regulating the G1/S-phase transition. Involved in astral microtubule organization and mitotic spindle orientation during early stage of mitosis; this process is regulated by phosphorylation by LIMK2.
Uniprot ID
O94811
Ensemble ID
ENST00000360578.7
HGNC ID
HGNC:24164

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 
C83(0.80)  LDD3331  [1]
HHS-475
 Probe Info 
Y211(0.81)  LDD0264  [2]
HHS-465
 Probe Info 
Y211(10.00)  LDD2237  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0116  HHS-0101 DM93 Y211(0.81)  LDD0264  [2]
 LDCM0117  HHS-0201 DM93 Y211(0.80)  LDD0265  [2]
 LDCM0118  HHS-0301 DM93 Y211(0.91)  LDD0266  [2]
 LDCM0119  HHS-0401 DM93 Y211(0.83)  LDD0267  [2]
 LDCM0120  HHS-0701 DM93 Y211(0.66)  LDD0268  [2]
 LDCM0022  KB02 MKN-1 C83(1.17)  LDD2497  [1]
 LDCM0023  KB03 MKN-1 C83(1.24)  LDD2914  [1]
 LDCM0024  KB05 MKN-1 C83(0.80)  LDD3331  [1]

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 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
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.