Details of the Target

General Information of Target

Target ID LDTP09894
Target Name X-linked retinitis pigmentosa GTPase regulator (RPGR)
Gene Name RPGR
Gene ID 6103
Synonyms
RP3; XLRP3; X-linked retinitis pigmentosa GTPase regulator
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSKERPKRNIIQKKYDDSDGIPWSEERVVRKVLYLSLKEFKNSQKRQHAEGIAGSLKTVN
GLLGNDQSKGLGPASEQSENEKDDASQVSSTSNDVSSSDFEEGPSRKRPRLQAQRKFAQS
QPNSPSTTPVKIVEPLLPPPATQISDLSKRKPKTEDFLTFLCLRGSPALPNSMVYFGSSQ
DEEEVEEEDDETEDVKTATNNASSSCQSTPRKGKTHKHVHNGHVFNGSSRSTREKEPVQK
HKSKEATPAKEKHSDHRADSRREQASANHPAAAPSTGSSAKGLAATHHHPPLHRSAQDLR
KQVSKVNGVTRMSSLGAGVTSAKKMREVRPSPSKTVKYTATVTKGAVTYTKAKRELVKDT
KPNHHKPSSAVNHTISGKTESSNAKTRKQVLSLGGASKSTGPAVNGLKVSGRLNPKSCTK
EVGGRQLREGLQLREGLRNSKRRLEEAHQAEKPQSPPKKMKGAAGPAEGPGKKAPAERGL
LNGHVKKEVPERSLERNRPKRATAGKSTPGRQAHGKADSASCENRSTSQPESVHKPQDSG
KAEKGGGKAGWAAMDEIPVLRPSAKEFHDPLIYIESVRAQVEKFGMCRVIPPPDWRPECK
LNDEMRFVTQIQHIHKLGRRWGPNVQRLACIKKHLKSQGITMDELPLIGGCELDLACFFR
LINEMGGMQQVTDLKKWNKLADMLRIPRTAQDRLAKLQEAYCQYLLSYDSLSPEEHRRLE
KEVLMEKEILEKRKGPLEGHTENDHHKFHPLPRFEPKNGLIHGVAPRNGFRSKLKEVGQA
QLKTGRRRLFAQEKEVVKEEEEDKGVLNDFHKCIYKGRSVSLTTFYRTARNIMSMCFSKE
PAPAEIEQEYWRLVEEKDCHVAVHCGKVDTNTHGSGFPVGKSEPFSRHGWNLTVLPNNTG
SILRHLGAVPGVTIPWLNIGMVFSTSCWSRDQNHLPYIDYLHTGADCIWYCIPAEEENKL
EDVVHTLLQANGTPGLQMLESNVMISPEVLCKEGIKVHRTVQQSGQFVVCFPGSFVSKVC
CGYSVSETVHFATTQWTSMGFETAKEMKRRHIAKPFSMEKLLYQIAQAEAKKENGPTLST
ISALLDELRDTELRQRRQLFEAGLHSSARYGSHDGSSTVADGKKKPRKWLQLETSERRCQ
ICQHLCYLSMVVQENENVVFCLECALRHVEKQKSCRGLKLMYRYDEEQIISLVNQICGKV
SGKNGSIENCLSKPTPKRGPRKRATVDVPPSRLSASSSSKSASSSS
Target Type
Clinical trial
Target Bioclass
Enzyme
Subcellular location
Cytoplasm, cytoskeleton, flagellum axoneme; Cytoplasm, cytoskeleton, microtubule organizing center, centrosome
Function
Could be a guanine-nucleotide releasing factor. Plays a role in ciliogenesis. Probably regulates cilia formation by regulating actin stress filaments and cell contractility. Plays an important role in photoreceptor integrity. May play a critical role in spermatogenesis and in intraflagellar transport processes. May be involved in microtubule organization and regulation of transport in primary cilia.
TTD ID
T54789
Uniprot ID
Q92834
DrugMap ID
TTHBDA9
Ensemble ID
ENST00000339363.7
HGNC ID
HGNC:10295

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
SISO SNV: p.F956L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C440(0.91)  LDD1507  [1]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [2]
IA-alkyne
 Probe Info  		C914(0.00); C343(0.00)  LDD0036  [2]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [2]
IPM
 Probe Info  		N.A.  LDD2156  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C440(0.91)  LDD1507  [1]
 LDCM0215  AC10 HEK-293T C914(0.90)  LDD1508  [1]
 LDCM0237  AC12 HEK-293T C440(1.14); C914(0.93)  LDD1510  [1]
 LDCM0259  AC14 HEK-293T C440(0.86)  LDD1512  [1]
 LDCM0270  AC15 HEK-293T C440(1.00)  LDD1513  [1]
 LDCM0276  AC17 HEK-293T C440(1.02)  LDD1515  [1]
 LDCM0277  AC18 HEK-293T C914(1.07)  LDD1516  [1]
 LDCM0279  AC2 HEK-293T C914(0.85)  LDD1518  [1]
 LDCM0280  AC20 HEK-293T C440(1.08); C914(0.87)  LDD1519  [1]
 LDCM0281  AC21 HEK-293T C440(0.97); C914(0.82)  LDD1520  [1]
 LDCM0282  AC22 HEK-293T C440(0.96)  LDD1521  [1]
 LDCM0283  AC23 HEK-293T C440(0.98)  LDD1522  [1]
 LDCM0284  AC24 HEK-293T C343(0.96); C440(1.22)  LDD1523  [1]
 LDCM0285  AC25 HEK-293T C440(1.10)  LDD1524  [1]
 LDCM0286  AC26 HEK-293T C914(0.96)  LDD1525  [1]
 LDCM0288  AC28 HEK-293T C440(1.03); C914(1.07)  LDD1527  [1]
 LDCM0289  AC29 HEK-293T C440(0.88); C914(0.87)  LDD1528  [1]
 LDCM0291  AC30 HEK-293T C440(1.04)  LDD1530  [1]
 LDCM0292  AC31 HEK-293T C440(1.00)  LDD1531  [1]
 LDCM0293  AC32 HEK-293T C343(0.70); C440(1.04)  LDD1532  [1]
 LDCM0294  AC33 HEK-293T C440(1.03)  LDD1533  [1]
 LDCM0295  AC34 HEK-293T C914(1.25)  LDD1534  [1]
 LDCM0297  AC36 HEK-293T C440(0.89); C914(1.08)  LDD1536  [1]
 LDCM0298  AC37 HEK-293T C440(1.14); C914(1.11)  LDD1537  [1]
 LDCM0299  AC38 HEK-293T C440(0.93)  LDD1538  [1]
 LDCM0300  AC39 HEK-293T C440(0.98)  LDD1539  [1]
 LDCM0301  AC4 HEK-293T C440(0.98); C914(1.19)  LDD1540  [1]
 LDCM0302  AC40 HEK-293T C343(0.86); C440(1.07)  LDD1541  [1]
 LDCM0303  AC41 HEK-293T C440(1.16)  LDD1542  [1]
 LDCM0304  AC42 HEK-293T C914(1.31)  LDD1543  [1]
 LDCM0306  AC44 HEK-293T C440(0.97); C914(1.19)  LDD1545  [1]
 LDCM0307  AC45 HEK-293T C440(0.94); C914(0.96)  LDD1546  [1]
 LDCM0308  AC46 HEK-293T C440(0.91)  LDD1547  [1]
 LDCM0309  AC47 HEK-293T C440(1.03)  LDD1548  [1]
 LDCM0310  AC48 HEK-293T C343(0.89); C440(1.02)  LDD1549  [1]
 LDCM0311  AC49 HEK-293T C440(0.95)  LDD1550  [1]
 LDCM0312  AC5 HEK-293T C440(0.89); C914(0.88)  LDD1551  [1]
 LDCM0313  AC50 HEK-293T C914(0.86)  LDD1552  [1]
 LDCM0315  AC52 HEK-293T C440(1.01); C914(1.10)  LDD1554  [1]
 LDCM0316  AC53 HEK-293T C440(0.92); C914(0.91)  LDD1555  [1]
 LDCM0317  AC54 HEK-293T C440(0.91)  LDD1556  [1]
 LDCM0318  AC55 HEK-293T C440(1.06)  LDD1557  [1]
 LDCM0319  AC56 HEK-293T C343(1.01); C440(1.18)  LDD1558  [1]
 LDCM0320  AC57 HEK-293T C440(0.94)  LDD1559  [1]
 LDCM0321  AC58 HEK-293T C914(0.97)  LDD1560  [1]
 LDCM0323  AC6 HEK-293T C440(0.84)  LDD1562  [1]
 LDCM0324  AC60 HEK-293T C440(1.16); C914(1.07)  LDD1563  [1]
 LDCM0325  AC61 HEK-293T C440(0.97); C914(0.89)  LDD1564  [1]
 LDCM0326  AC62 HEK-293T C440(0.84)  LDD1565  [1]
 LDCM0327  AC63 HEK-293T C440(0.98)  LDD1566  [1]
 LDCM0328  AC64 HEK-293T C343(0.91); C440(1.18)  LDD1567  [1]
 LDCM0334  AC7 HEK-293T C440(1.00)  LDD1568  [1]
 LDCM0345  AC8 HEK-293T C343(1.19); C440(1.05)  LDD1569  [1]
 LDCM0248  AKOS034007472 HEK-293T C440(0.91); C914(1.02)  LDD1511  [1]
 LDCM0356  AKOS034007680 HEK-293T C440(1.14)  LDD1570  [1]
 LDCM0275  AKOS034007705 HEK-293T C343(0.91); C440(1.20)  LDD1514  [1]
 LDCM0367  CL1 HEK-293T C440(0.97)  LDD1571  [1]
 LDCM0368  CL10 HEK-293T C440(0.28)  LDD1572  [1]
 LDCM0369  CL100 HEK-293T C384(1.56); C80(1.22); C914(1.31)  LDD1573  [1]
 LDCM0370  CL101 HEK-293T C440(1.08)  LDD1574  [1]
 LDCM0372  CL103 HEK-293T C440(1.02); C384(0.94)  LDD1576  [1]
 LDCM0373  CL104 HEK-293T C384(1.10); C80(1.02); C914(1.00)  LDD1577  [1]
 LDCM0374  CL105 HEK-293T C440(0.86)  LDD1578  [1]
 LDCM0376  CL107 HEK-293T C440(0.90); C384(1.65)  LDD1580  [1]
 LDCM0377  CL108 HEK-293T C384(2.20); C80(0.90); C914(1.12)  LDD1581  [1]
 LDCM0378  CL109 HEK-293T C440(1.26)  LDD1582  [1]
 LDCM0379  CL11 HEK-293T C440(1.00)  LDD1583  [1]
 LDCM0381  CL111 HEK-293T C440(1.05); C384(1.06)  LDD1585  [1]
 LDCM0382  CL112 HEK-293T C384(1.45); C80(1.07); C914(1.12)  LDD1586  [1]
 LDCM0383  CL113 HEK-293T C440(0.96)  LDD1587  [1]
 LDCM0385  CL115 HEK-293T C440(0.97); C384(1.06)  LDD1589  [1]
 LDCM0386  CL116 HEK-293T C384(1.42); C80(1.04); C914(1.35)  LDD1590  [1]
 LDCM0387  CL117 HEK-293T C440(1.14)  LDD1591  [1]
 LDCM0389  CL119 HEK-293T C440(1.11); C384(0.81)  LDD1593  [1]
 LDCM0390  CL12 HEK-293T C343(1.08); C440(0.99)  LDD1594  [1]
 LDCM0391  CL120 HEK-293T C384(1.01); C80(1.02); C914(1.16)  LDD1595  [1]
 LDCM0392  CL121 HEK-293T C440(0.90)  LDD1596  [1]
 LDCM0394  CL123 HEK-293T C440(0.98); C384(1.26)  LDD1598  [1]
 LDCM0395  CL124 HEK-293T C384(1.36); C80(0.93); C914(0.96)  LDD1599  [1]
 LDCM0396  CL125 HEK-293T C440(1.32)  LDD1600  [1]
 LDCM0398  CL127 HEK-293T C440(1.10); C384(0.79)  LDD1602  [1]
 LDCM0399  CL128 HEK-293T C384(1.04); C80(0.97); C914(0.88)  LDD1603  [1]
 LDCM0400  CL13 HEK-293T C440(0.98)  LDD1604  [1]
 LDCM0402  CL15 HEK-293T C440(0.94); C384(0.77)  LDD1606  [1]
 LDCM0403  CL16 HEK-293T C384(1.02); C80(1.11); C914(1.19)  LDD1607  [1]
 LDCM0404  CL17 HEK-293T C440(1.11)  LDD1608  [1]
 LDCM0405  CL18 HEK-293T C914(1.05)  LDD1609  [1]
 LDCM0408  CL20 HEK-293T C440(1.29); C914(1.34)  LDD1612  [1]
 LDCM0409  CL21 HEK-293T C440(0.95); C914(0.95)  LDD1613  [1]
 LDCM0410  CL22 HEK-293T C440(0.81)  LDD1614  [1]
 LDCM0411  CL23 HEK-293T C440(0.96)  LDD1615  [1]
 LDCM0412  CL24 HEK-293T C343(0.97); C440(1.04)  LDD1616  [1]
 LDCM0413  CL25 HEK-293T C440(1.03)  LDD1617  [1]
 LDCM0415  CL27 HEK-293T C440(1.10); C384(1.05)  LDD1619  [1]
 LDCM0416  CL28 HEK-293T C384(1.44); C80(0.99); C914(1.10)  LDD1620  [1]
 LDCM0417  CL29 HEK-293T C440(0.99)  LDD1621  [1]
 LDCM0418  CL3 HEK-293T C440(1.03); C384(0.83)  LDD1622  [1]
 LDCM0419  CL30 HEK-293T C914(0.91)  LDD1623  [1]
 LDCM0421  CL32 HEK-293T C440(1.12); C914(1.05)  LDD1625  [1]
 LDCM0422  CL33 HEK-293T C440(0.71); C914(0.80)  LDD1626  [1]
 LDCM0423  CL34 HEK-293T C440(0.90)  LDD1627  [1]
 LDCM0424  CL35 HEK-293T C440(0.96)  LDD1628  [1]
 LDCM0425  CL36 HEK-293T C343(1.16); C440(0.89)  LDD1629  [1]
 LDCM0426  CL37 HEK-293T C440(1.22)  LDD1630  [1]
 LDCM0428  CL39 HEK-293T C440(1.05); C384(1.26)  LDD1632  [1]
 LDCM0429  CL4 HEK-293T C384(1.27); C80(1.04); C914(1.11)  LDD1633  [1]
 LDCM0430  CL40 HEK-293T C384(1.49); C80(1.06); C914(1.20)  LDD1634  [1]
 LDCM0431  CL41 HEK-293T C440(1.00)  LDD1635  [1]
 LDCM0432  CL42 HEK-293T C914(1.24)  LDD1636  [1]
 LDCM0434  CL44 HEK-293T C440(0.93); C914(1.22)  LDD1638  [1]
 LDCM0435  CL45 HEK-293T C440(0.94); C914(1.09)  LDD1639  [1]
 LDCM0436  CL46 HEK-293T C440(0.94)  LDD1640  [1]
 LDCM0437  CL47 HEK-293T C440(1.03)  LDD1641  [1]
 LDCM0438  CL48 HEK-293T C343(1.00); C440(0.96)  LDD1642  [1]
 LDCM0439  CL49 HEK-293T C440(1.18)  LDD1643  [1]
 LDCM0440  CL5 HEK-293T C440(1.02)  LDD1644  [1]
 LDCM0443  CL52 HEK-293T C384(1.16); C80(1.08); C914(1.02)  LDD1646  [1]
 LDCM0444  CL53 HEK-293T C440(1.10)  LDD1647  [1]
 LDCM0445  CL54 HEK-293T C914(1.25)  LDD1648  [1]
 LDCM0447  CL56 HEK-293T C440(1.04); C914(1.33)  LDD1650  [1]
 LDCM0448  CL57 HEK-293T C440(0.86); C914(1.16)  LDD1651  [1]
 LDCM0449  CL58 HEK-293T C440(0.85)  LDD1652  [1]
 LDCM0450  CL59 HEK-293T C440(1.08)  LDD1653  [1]
 LDCM0451  CL6 HEK-293T C914(1.11)  LDD1654  [1]
 LDCM0452  CL60 HEK-293T C343(1.23); C440(1.11)  LDD1655  [1]
 LDCM0453  CL61 HEK-293T C440(0.98)  LDD1656  [1]
 LDCM0455  CL63 HEK-293T C440(1.05); C384(0.88)  LDD1658  [1]
 LDCM0456  CL64 HEK-293T C384(1.28); C80(1.00); C914(0.98)  LDD1659  [1]
 LDCM0457  CL65 HEK-293T C440(1.55)  LDD1660  [1]
 LDCM0458  CL66 HEK-293T C914(1.25)  LDD1661  [1]
 LDCM0460  CL68 HEK-293T C440(0.98); C914(1.15)  LDD1663  [1]
 LDCM0461  CL69 HEK-293T C440(0.93); C914(0.76)  LDD1664  [1]
 LDCM0463  CL70 HEK-293T C440(0.87)  LDD1666  [1]
 LDCM0464  CL71 HEK-293T C440(1.07)  LDD1667  [1]
 LDCM0465  CL72 HEK-293T C343(1.01); C440(1.04)  LDD1668  [1]
 LDCM0466  CL73 HEK-293T C440(1.07)  LDD1669  [1]
 LDCM0469  CL76 HEK-293T C384(1.07); C80(0.97); C914(0.65)  LDD1672  [1]
 LDCM0470  CL77 HEK-293T C440(0.81)  LDD1673  [1]
 LDCM0471  CL78 HEK-293T C914(0.71)  LDD1674  [1]
 LDCM0473  CL8 HEK-293T C440(0.90); C914(0.94)  LDD1676  [1]
 LDCM0474  CL80 HEK-293T C440(1.02); C914(1.14)  LDD1677  [1]
 LDCM0475  CL81 HEK-293T C440(0.99); C914(0.83)  LDD1678  [1]
 LDCM0476  CL82 HEK-293T C440(0.81)  LDD1679  [1]
 LDCM0477  CL83 HEK-293T C440(0.92)  LDD1680  [1]
 LDCM0478  CL84 HEK-293T C343(1.16); C440(0.92)  LDD1681  [1]
 LDCM0479  CL85 HEK-293T C440(1.22)  LDD1682  [1]
 LDCM0481  CL87 HEK-293T C440(0.96); C384(1.32)  LDD1684  [1]
 LDCM0482  CL88 HEK-293T C384(1.51); C80(0.95); C914(0.77)  LDD1685  [1]
 LDCM0483  CL89 HEK-293T C440(0.98)  LDD1686  [1]
 LDCM0484  CL9 HEK-293T C440(0.94); C914(1.03)  LDD1687  [1]
 LDCM0485  CL90 HEK-293T C914(0.80)  LDD1688  [1]
 LDCM0487  CL92 HEK-293T C440(0.95); C914(1.27)  LDD1690  [1]
 LDCM0488  CL93 HEK-293T C440(0.82); C914(1.01)  LDD1691  [1]
 LDCM0489  CL94 HEK-293T C440(1.00)  LDD1692  [1]
 LDCM0490  CL95 HEK-293T C440(0.96)  LDD1693  [1]
 LDCM0491  CL96 HEK-293T C343(0.89); C440(1.12)  LDD1694  [1]
 LDCM0492  CL97 HEK-293T C440(1.14)  LDD1695  [1]
 LDCM0494  CL99 HEK-293T C440(1.02); C384(1.18)  LDD1697  [1]
 LDCM0495  E2913 HEK-293T C440(1.01); C384(0.66)  LDD1698  [1]
 LDCM0468  Fragment33 HEK-293T C440(0.90); C384(0.83)  LDD1671  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta (PDE6D) PDE6D/unc-119 family O43924
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
X-linked retinitis pigmentosa GTPase regulator-interacting protein 1 (RPGRIP1) RPGRIP1 family Q96KN7

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Biib-088 Gene therapy DKH94Z
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aav-rpgr Gene therapy DZ8FV2
Agtc-501 Gene therapy DO76YM

References

1 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
2 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
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