Details of the Target

General Information of Target

Target ID LDTP06755
Target Name Leucine-rich repeat serine/threonine-protein kinase 1 (LRRK1)
Gene Name LRRK1
Gene ID 79705
Synonyms
KIAA1790; Leucine-rich repeat serine/threonine-protein kinase 1; EC 2.7.11.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGMSQRPPSMYWCVGPEESAVCPERAMETLNGAGDTGGKPSTRGGDPAARSRRTEGIRA
AYRRGDRGGARDLLEEACDQCASQLEKGQLLSIPAAYGDLEMVRYLLSKRLVELPTEPTD
DNPAVVAAYFGHTAVVQELLESLPGPCSPQRLLNWMLALACQRGHLGVVKLLVLTHGADP
ESYAVRKNEFPVIVRLPLYAAIKSGNEDIAIFLLRHGAYFCSYILLDSPDPSKHLLRKYF
IEASPLPSSYPGKTALRVKWSHLRLPWVDLDWLIDISCQITELDLSANCLATLPSVIPWG
LINLRKLNLSDNHLGELPGVQSSDEIICSRLLEIDISSNKLSHLPPGFLHLSKLQKLTAS
KNCLEKLFEEENATNWIGLRKLQELDISDNKLTELPALFLHSFKSLNSLNVSRNNLKVFP
DPWACPLKCCKASRNALECLPDKMAVFWKNHLKDVDFSENALKEVPLGLFQLDALMFLRL
QGNQLAALPPQEKWTCRQLKTLDLSRNQLGKNEDGLKTKRIAFFTTRGRQRSGTEAASVL
EFPAFLSESLEVLCLNDNHLDTVPPSVCLLKSLSELYLGNNPGLRELPPELGQLGNLWQL
DTEDLTISNVPAEIQKEGPKAMLSYLRAQLRKAEKCKLMKMIIVGPPRQGKSTLLEILQT
GRAPQVVHGEATIRTTKWELQRPAGSRAKVESVEFNVWDIGGPASMATVNQCFFTDKALY
VVVWNLALGEEAVANLQFWLLNIEAKAPNAVVLVVGTHLDLIEAKFRVERIATLRAYVLA
LCRSPSGSRATGFPDITFKHLHEISCKSLEGQEGLRQLIFHVTCSMKDVGSTIGCQRLAG
RLIPRSYLSLQEAVLAEQQRRSRDDDVQYLTDRQLEQLVEQTPDNDIKDYEDLQSAISFL
IETGTLLHFPDTSHGLRNLYFLDPIWLSECLQRIFNIKGSRSVAKNGVIRAEDLRMLLVG
TGFTQQTEEQYFQFLAKFEIALPVANDSYLLPHLLPSKPGLDTHGMRHPTANTIQRVFKM
SFVPVGFWQRFIARMLISLAEMDLQLFENKKNTKSRNRKVTIYSFTGNQRNRCSTFRVKR
NQTIYWQEGLLVTFDGGYLSVESSDVNWKKKKSGGMKIVCQSEVRDFSAMAFITDHVNSL
IDQWFPALTATESDGTPLMEQYVPCPVCETAWAQHTDPSEKSEDVQYFDMEDCVLTAIER
DFISCPRHPDLPVPLQELVPELFMTDFPARLFLENSKLEHSEDEGSVLGQGGSGTVIYRA
RYQGQPVAVKRFHIKKFKNFANVPADTMLRHLRATDAMKNFSEFRQEASMLHALQHPCIV
ALIGISIHPLCFALELAPLSSLNTVLSENARDSSFIPLGHMLTQKIAYQIASGLAYLHKK
NIIFCDLKSDNILVWSLDVKEHINIKLSDYGISRQSFHEGALGVEGTPGYQAPEIRPRIV
YDEKVDMFSYGMVLYELLSGQRPALGHHQLQIAKKLSKGIRPVLGQPEEVQFRRLQALMM
ECWDTKPEKRPLALSVVSQMKDPTFATFMYELCCGKQTAFFSSQGQEYTVVFWDGKEESR
NYTVVNTEKGLMEVQRMCCPGMKVSCQLQVQRSLWTATEDQKIYIYTLKGMCPLNTPQQA
LDTPAVVTCFLAVPVIKKNSYLVLAGLADGLVAVFPVVRGTPKDSCSYLCSHTANRSKFS
IADEDARQNPYPVKAMEVVNSGSEVWYSNGPGLLVIDCASLEICRRLEPYMAPSMVTSVV
CSSEGRGEEVVWCLDDKANSLVMYHSTTYQLCARYFCGVPSPLRDMFPVRPLDTEPPAAS
HTANPKVPEGDSIADVSIMYSEELGTQILIHQESLTDYCSMSSYSSSPPRQAARSPSSLP
SSPASSSSVPFSTDCEDSDMLHTPGAASDRSEHDLTPMDGETFSQHLQAVKILAVRDLIW
VPRRGGDVIVIGLEKDSGAQRGRVIAVLKARELTPHGVLVDAAVVAKDTVVCTFENENTE
WCLAVWRGWGAREFDIFYQSYEELGRLEACTRKRR
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, ROCO subfamily
Subcellular location
Cytoplasm
Function Plays a role in the negative regulation of bone mass, acting through the maturation of osteoclasts.
Uniprot ID
Q38SD2
Ensemble ID
ENST00000388948.8
HGNC ID
HGNC:18608

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.V1483I .
BT549 SNV: p.G1264A .
CCK81 SNV: p.L516M; p.S786F .
COLO792 SNV: p.R215W .
HCT15 SNV: p.Q1186Ter; p.G1660V .
HEC1 SNV: p.A82T .
HKGZCC SNV: p.L283I .
JURKAT SNV: p.Q1364Ter .
KYM1 SNV: p.M622T .
KYSE150 SNV: p.S805F .
MCAS SNV: p.C1165Y .
MCC13 SNV: p.P1788L .
MFE296 SNV: p.R1916G .
NALM6 SNV: p.R767C DBIA    Probe Info 
NCIH146 SNV: p.Q1544L .
NCIH2172 SNV: p.A34V .
NCIH661 SNV: p.M1880V .
OVK18 SNV: p.P564H .
REH SNV: p.G904S .
SHSY5Y SNV: p.A95T .
SKNSH SNV: p.A95T .
SNU1 SNV: p.R67H .
TC71 SNV: p.G98W .
TE4 SNV: p.R1462H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C425(2.38)  LDD3339  [1]
YN-1
 Probe Info  		N.A.  LDD0447  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A3-KAW C1120(1.18)  LDD2257  [1]
 LDCM0023  KB03 A3-KAW C1120(1.24)  LDD2674  [1]
 LDCM0024  KB05 NALM-6 C425(2.38)  LDD3339  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Death-associated protein kinase 1 (DAPK1) CAMK Ser/Thr protein kinase family P53355
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
Leucine-rich repeat serine/threonine-protein kinase 1 (LRRK1) TKL Ser/Thr protein kinase family Q38SD2
Tyrosine-protein kinase ABL1 (ABL1) Tyr protein kinase family P00519
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Integrin alpha-V (ITGAV) Integrin alpha chain family P06756
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
BAG family molecular chaperone regulator 5 (BAG5) . Q9UL15
CDK5 regulatory subunit-associated protein 2 (CDK5RAP2) . Q96SN8

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 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.