General Information of Target

Target ID LDTP10809
Target Name SRSF protein kinase 1 (SRPK1)
Gene Name SRPK1
Gene ID 6732
Synonyms
SRSF protein kinase 1; EC 2.7.11.1; SFRS protein kinase 1; Serine/arginine-rich protein-specific kinase 1; SR-protein-specific kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMKTEPRGPGGPLRSASPHRSAYEAGIQALKPPDAPGPDEAPKGAHHKKYGSNVHRIKSM
FLQMGTTAGPSGEAGGGAGLAEAPRASERGVRLSLPRASSLNENVDHSALLKLGTSVSER
VSRFDSKPAPSAQPAPPPHPPSRLQETRKLFERSAPAAAGGDKEAAARRLLRQERAGLQD
RKLDVVVRFNGSTEALDKLDADAVSPTVSQLSAVFEKADSRTGLHRGPGLPRAAGVPQVN
SKLVSKRSRVFQPPPPPPPAPSGDAPAEKERCPAGQQPPQHRVAPARPPPKPREVRKIKP
VEVEESGESEAESAPGEVIQAEVTVHAALENGSTVATAASPAPEEPKAQAAPEKEAAAVA
PPERGVGNGRAPDVAPEEVDESKKEDFSEADLVDVSAYSGLGEDSAGSALEEDDEDDEED
GEPPYEPESGCVEIPGLSEEEDPAPSRKIHFSTAPIQVFSTYSNEDYDRRNEDVDPMAAS
AEYELEKRVERLELFPVELEKDSEGLGISIIGMGAGADMGLEKLGIFVKTVTEGGAAHRD
GRIQVNDLLVEVDGTSLVGVTQSFAASVLRNTKGRVRFMIGRERPGEQSEVAQLIQQTLE
QERWQREMMEQRYAQYGEDDEETGEYATDEDEELSPTFPGGEMAIEVFELAENEDALSPV
DMEPEKLVHKFKELQIKHAVTEAEIQQLKRKLQSLEQEKGRWRVEKAQLEQSVEENKERM
EKLEGYWGEAQSLCQAVDEHLRETQAQYQALERKYSKAKRLIKDYQQKEIEFLKKETAQR
RVLEESELARKEEMDKLLDKISELEGNLQTLRNSNST
Target Type
Preclinical
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family
Subcellular location
Cytoplasm
Function
Serine/arginine-rich protein-specific kinase which specifically phosphorylates its substrates at serine residues located in regions rich in arginine/serine dipeptides, known as RS domains and is involved in the phosphorylation of SR splicing factors and the regulation of splicing. Plays a central role in the regulatory network for splicing, controlling the intranuclear distribution of splicing factors in interphase cells and the reorganization of nuclear speckles during mitosis. Can influence additional steps of mRNA maturation, as well as other cellular activities, such as chromatin reorganization in somatic and sperm cells and cell cycle progression. Isoform 2 phosphorylates SFRS2, ZRSR2, LBR and PRM1. Isoform 2 phosphorylates SRSF1 using a directional (C-terminal to N-terminal) and a dual-track mechanism incorporating both processive phosphorylation (in which the kinase stays attached to the substrate after each round of phosphorylation) and distributive phosphorylation steps (in which the kinase and substrate dissociate after each phosphorylation event). The RS domain of SRSF1 binds first to a docking groove in the large lobe of the kinase domain of SRPK1. This induces certain structural changes in SRPK1 and/or RRM2 domain of SRSF1, allowing RRM2 to bind the kinase and initiate phosphorylation. The cycles continue for several phosphorylation steps in a processive manner (steps 1-8) until the last few phosphorylation steps (approximately steps 9-12). During that time, a mechanical stress induces the unfolding of the beta-4 motif in RRM2, which then docks at the docking groove of SRPK1. This also signals RRM2 to begin to dissociate, which facilitates SRSF1 dissociation after phosphorylation is completed. Isoform 2 can mediate hepatitis B virus (HBV) core protein phosphorylation. It plays a negative role in the regulation of HBV replication through a mechanism not involving the phosphorylation of the core protein but by reducing the packaging efficiency of the pregenomic RNA (pgRNA) without affecting the formation of the viral core particles. Isoform 1 and isoform 2 can induce splicing of exon 10 in MAPT/TAU. The ratio of isoform 1/isoform 2 plays a decisive role in determining cell fate in K-562 leukaemic cell line: isoform 2 favors proliferation where as isoform 1 favors differentiation.
TTD ID
T94201
Uniprot ID
Q96SB4
DrugMap ID
TTU3WV6
Ensemble ID
ENST00000373825.7
HGNC ID
HGNC:11305
ChEMBL ID
CHEMBL4375

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 27 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
15.00  LDD0402  [1]
STPyne
 Probe Info 
K25(6.67); K4(10.00); K486(0.97); K579(10.00)  LDD0277  [2]
Probe 1
 Probe Info 
Y117(14.40)  LDD3495  [3]
DBIA
 Probe Info 
C359(3.35)  LDD3312  [4]
BTD
 Probe Info 
C188(0.50)  LDD2089  [5]
DA-P3
 Probe Info 
5.05  LDD0182  [6]
AHL-Pu-1
 Probe Info 
C502(2.14); C455(2.02)  LDD0168  [7]
ATP probe
 Probe Info 
K506(0.00); K215(0.00); K191(0.00)  LDD0199  [8]
4-Iodoacetamidophenylacetylene
 Probe Info 
C455(0.00); C647(0.00); C188(0.00); C502(0.00)  LDD0038  [9]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [10]
IPIAA_L
 Probe Info 
N.A.  LDD0031  [11]
Lodoacetamide azide
 Probe Info 
C455(0.00); C647(0.00); C502(0.00); C188(0.00)  LDD0037  [9]
NAIA_4
 Probe Info 
C356(0.00); C455(0.00)  LDD2226  [12]
WYneO
 Probe Info 
N.A.  LDD0022  [13]
Compound 10
 Probe Info 
C502(0.00); C647(0.00)  LDD2216  [14]
ENE
 Probe Info 
N.A.  LDD0006  [13]
IPM
 Probe Info 
C356(0.00); C455(0.00); C647(0.00)  LDD0147  [15]
PF-06672131
 Probe Info 
N.A.  LDD0017  [16]
SF
 Probe Info 
N.A.  LDD0028  [17]
TFBX
 Probe Info 
C188(0.00); C455(0.00)  LDD0148  [15]
VSF
 Probe Info 
N.A.  LDD0007  [13]
Acrolein
 Probe Info 
C455(0.00); C647(0.00); C188(0.00)  LDD0217  [18]
Crotonaldehyde
 Probe Info 
C647(0.00); C455(0.00)  LDD0219  [18]
Methacrolein
 Probe Info 
C455(0.00); C647(0.00)  LDD0218  [18]
W1
 Probe Info 
N.A.  LDD0236  [19]
AOyne
 Probe Info 
15.00  LDD0443  [20]
NAIA_5
 Probe Info 
C455(0.00); C647(0.00)  LDD2223  [12]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C056
 Probe Info 
16.56  LDD1753  [21]
FFF probe14
 Probe Info 
20.00  LDD0477  [22]
FFF probe2
 Probe Info 
5.86  LDD0463  [22]
Probe 12
 Probe Info 
N.A.  LDD0420  [23]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C188(0.55)  LDD2095  [5]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C188(0.93)  LDD2130  [5]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C188(0.97); C455(1.21)  LDD2117  [5]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C188(1.59)  LDD2152  [5]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C188(0.81)  LDD2131  [5]
 LDCM0025  4SU-RNA HEK-293T C502(2.14); C455(2.02)  LDD0168  [7]
 LDCM0026  4SU-RNA+native RNA DM93 C455(5.75); C356(8.12)  LDD0171  [7]
 LDCM0214  AC1 HEK-293T C647(0.97); C455(1.04); C356(0.91)  LDD1507  [24]
 LDCM0215  AC10 HEK-293T C647(1.02); C455(0.94); C356(1.04)  LDD1508  [24]
 LDCM0226  AC11 HEK-293T C647(0.98); C455(0.95); C188(0.92); C356(0.97)  LDD1509  [24]
 LDCM0237  AC12 HEK-293T C455(0.92); C356(1.11)  LDD1510  [24]
 LDCM0259  AC14 HEK-293T C647(1.00); C455(0.99); C356(1.04)  LDD1512  [24]
 LDCM0270  AC15 HEK-293T C647(0.99); C455(1.06); C188(0.93)  LDD1513  [24]
 LDCM0276  AC17 HEK-293T C647(0.94); C455(0.98); C356(1.00)  LDD1515  [24]
 LDCM0277  AC18 HEK-293T C647(1.06); C455(0.99); C356(1.04)  LDD1516  [24]
 LDCM0278  AC19 HEK-293T C647(1.05); C455(1.02); C188(0.82); C356(1.13)  LDD1517  [24]
 LDCM0279  AC2 HEK-293T C647(1.01); C455(0.97); C356(1.11)  LDD1518  [24]
 LDCM0280  AC20 HEK-293T C455(0.98); C356(1.09)  LDD1519  [24]
 LDCM0281  AC21 HEK-293T C647(1.04); C455(1.05); C188(1.05); C356(0.95)  LDD1520  [24]
 LDCM0282  AC22 HEK-293T C647(0.93); C455(0.98); C356(1.10)  LDD1521  [24]
 LDCM0283  AC23 HEK-293T C647(0.93); C455(0.95); C188(1.08)  LDD1522  [24]
 LDCM0284  AC24 HEK-293T C647(1.00); C455(1.02); C356(0.89)  LDD1523  [24]
 LDCM0285  AC25 HEK-293T C647(0.96); C455(1.00); C356(0.99)  LDD1524  [24]
 LDCM0286  AC26 HEK-293T C647(1.03); C455(0.99); C356(1.05)  LDD1525  [24]
 LDCM0287  AC27 HEK-293T C647(1.13); C455(0.94); C188(0.92); C356(1.01)  LDD1526  [24]
 LDCM0288  AC28 HEK-293T C455(0.95); C356(1.14)  LDD1527  [24]
 LDCM0289  AC29 HEK-293T C647(1.01); C455(1.05); C188(0.98); C356(0.97)  LDD1528  [24]
 LDCM0290  AC3 HEK-293T C647(1.21); C455(0.95); C188(0.93); C356(1.24)  LDD1529  [24]
 LDCM0291  AC30 HEK-293T C647(1.02); C455(0.98); C356(0.99)  LDD1530  [24]
 LDCM0292  AC31 HEK-293T C647(1.00); C455(0.94); C188(1.09)  LDD1531  [24]
 LDCM0293  AC32 HEK-293T C647(0.99); C455(1.03); C356(0.97)  LDD1532  [24]
 LDCM0294  AC33 HEK-293T C647(0.96); C455(0.95); C356(0.99)  LDD1533  [24]
 LDCM0295  AC34 HEK-293T C647(0.96); C455(0.94); C356(1.24)  LDD1534  [24]
 LDCM0296  AC35 HEK-293T C647(1.11); C455(0.86); C188(0.93); C356(1.32)  LDD1535  [24]
 LDCM0297  AC36 HEK-293T C455(0.87); C356(1.13)  LDD1536  [24]
 LDCM0298  AC37 HEK-293T C647(1.06); C455(0.88); C188(1.06); C356(1.11)  LDD1537  [24]
 LDCM0299  AC38 HEK-293T C647(1.04); C455(1.03); C356(0.99)  LDD1538  [24]
 LDCM0300  AC39 HEK-293T C647(1.03); C455(1.07); C188(1.05)  LDD1539  [24]
 LDCM0301  AC4 HEK-293T C455(0.96); C356(1.14)  LDD1540  [24]
 LDCM0302  AC40 HEK-293T C647(1.01); C455(0.93); C356(0.98)  LDD1541  [24]
 LDCM0303  AC41 HEK-293T C647(0.98); C455(1.00); C356(0.99)  LDD1542  [24]
 LDCM0304  AC42 HEK-293T C647(1.01); C455(0.97); C356(1.42)  LDD1543  [24]
 LDCM0305  AC43 HEK-293T C647(1.09); C455(0.93); C188(0.97); C356(1.01)  LDD1544  [24]
 LDCM0306  AC44 HEK-293T C455(0.94); C356(0.99)  LDD1545  [24]
 LDCM0307  AC45 HEK-293T C647(1.10); C455(0.96); C188(1.05); C356(0.96)  LDD1546  [24]
 LDCM0308  AC46 HEK-293T C647(1.01); C455(0.97); C356(0.92)  LDD1547  [24]
 LDCM0309  AC47 HEK-293T C647(1.01); C455(1.08); C188(1.13)  LDD1548  [24]
 LDCM0310  AC48 HEK-293T C647(0.99); C455(1.02); C356(1.07)  LDD1549  [24]
 LDCM0311  AC49 HEK-293T C647(0.95); C455(0.95); C356(0.85)  LDD1550  [24]
 LDCM0312  AC5 HEK-293T C647(0.99); C455(0.93); C188(1.11); C356(1.05)  LDD1551  [24]
 LDCM0313  AC50 HEK-293T C647(1.01); C455(0.94); C356(1.25)  LDD1552  [24]
 LDCM0314  AC51 HEK-293T C647(1.06); C455(0.93); C188(0.96); C356(1.11)  LDD1553  [24]
 LDCM0315  AC52 HEK-293T C455(0.99); C356(1.10)  LDD1554  [24]
 LDCM0316  AC53 HEK-293T C647(1.04); C455(0.87); C188(1.05); C356(1.27)  LDD1555  [24]
 LDCM0317  AC54 HEK-293T C647(1.02); C455(1.00); C356(0.91)  LDD1556  [24]
 LDCM0318  AC55 HEK-293T C647(0.93); C455(1.02); C188(1.04)  LDD1557  [24]
 LDCM0319  AC56 HEK-293T C647(1.03); C455(0.97); C356(0.98)  LDD1558  [24]
 LDCM0320  AC57 HEK-293T C647(1.01); C455(0.93); C356(1.00)  LDD1559  [24]
 LDCM0321  AC58 HEK-293T C647(1.08); C455(0.96); C356(1.15)  LDD1560  [24]
 LDCM0322  AC59 HEK-293T C647(1.07); C455(0.92); C188(0.98); C356(1.00)  LDD1561  [24]
 LDCM0323  AC6 HEK-293T C647(0.96); C455(0.99); C356(1.11)  LDD1562  [24]
 LDCM0324  AC60 HEK-293T C455(0.93); C356(1.12)  LDD1563  [24]
 LDCM0325  AC61 HEK-293T C647(0.98); C455(0.93); C188(1.03); C356(0.99)  LDD1564  [24]
 LDCM0326  AC62 HEK-293T C647(1.01); C455(1.01); C356(1.05)  LDD1565  [24]
 LDCM0327  AC63 HEK-293T C647(0.98); C455(1.05); C188(0.96)  LDD1566  [24]
 LDCM0328  AC64 HEK-293T C647(1.07); C455(0.95); C356(1.03)  LDD1567  [24]
 LDCM0334  AC7 HEK-293T C647(1.01); C455(1.03); C188(1.16)  LDD1568  [24]
 LDCM0345  AC8 HEK-293T C647(0.94); C455(0.98); C356(1.07)  LDD1569  [24]
 LDCM0545  Acetamide MDA-MB-231 C188(0.38)  LDD2138  [5]
 LDCM0520  AKOS000195272 MDA-MB-231 C188(0.23)  LDD2113  [5]
 LDCM0248  AKOS034007472 HEK-293T C647(1.14); C455(0.95); C188(1.11); C356(0.95)  LDD1511  [24]
 LDCM0356  AKOS034007680 HEK-293T C647(0.91); C455(1.03); C356(0.83)  LDD1570  [24]
 LDCM0275  AKOS034007705 HEK-293T C647(1.01); C455(0.96); C356(0.97)  LDD1514  [24]
 LDCM0156  Aniline NCI-H1299 11.71  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C188(0.56); C455(0.65)  LDD2091  [5]
 LDCM0108  Chloroacetamide HeLa C455(0.00); C647(0.00)  LDD0222  [18]
 LDCM0367  CL1 HEK-293T C647(1.06); C455(0.95); C188(0.92); C356(1.32)  LDD1571  [24]
 LDCM0368  CL10 HEK-293T C647(1.01); C455(0.84); C356(1.11)  LDD1572  [24]
 LDCM0369  CL100 HEK-293T C647(1.01); C455(0.91); C188(0.94); C356(0.92)  LDD1573  [24]
 LDCM0370  CL101 HEK-293T C647(0.98); C455(0.93); C188(0.94); C356(1.15)  LDD1574  [24]
 LDCM0371  CL102 HEK-293T C647(1.01); C455(0.87); C356(1.13)  LDD1575  [24]
 LDCM0372  CL103 HEK-293T C647(0.99); C455(0.88); C188(1.00); C356(1.09)  LDD1576  [24]
 LDCM0373  CL104 HEK-293T C647(1.00); C455(0.86); C188(0.92); C356(1.13)  LDD1577  [24]
 LDCM0374  CL105 HEK-293T C647(0.94); C455(1.00); C188(1.04); C356(1.11)  LDD1578  [24]
 LDCM0375  CL106 HEK-293T C647(1.10); C455(0.89); C356(1.24)  LDD1579  [24]
 LDCM0376  CL107 HEK-293T C647(1.10); C455(0.92); C188(1.03); C356(1.05)  LDD1580  [24]
 LDCM0377  CL108 HEK-293T C647(1.01); C455(1.01); C188(0.93); C356(1.11)  LDD1581  [24]
 LDCM0378  CL109 HEK-293T C647(0.91); C455(0.96); C188(1.02); C356(1.15)  LDD1582  [24]
 LDCM0379  CL11 HEK-293T C647(1.05); C455(1.11); C188(1.51)  LDD1583  [24]
 LDCM0380  CL110 HEK-293T C647(1.01); C455(0.82); C356(1.06)  LDD1584  [24]
 LDCM0381  CL111 HEK-293T C647(1.03); C455(0.85); C188(0.98); C356(0.92)  LDD1585  [24]
 LDCM0382  CL112 HEK-293T C647(1.10); C455(0.99); C188(0.88); C356(1.17)  LDD1586  [24]
 LDCM0383  CL113 HEK-293T C647(1.00); C455(0.95); C188(0.91); C356(1.04)  LDD1587  [24]
 LDCM0384  CL114 HEK-293T C647(1.03); C455(0.77); C356(1.07)  LDD1588  [24]
 LDCM0385  CL115 HEK-293T C647(1.05); C455(0.87); C188(0.95); C356(1.09)  LDD1589  [24]
 LDCM0386  CL116 HEK-293T C647(1.12); C455(0.85); C188(0.89); C356(1.29)  LDD1590  [24]
 LDCM0387  CL117 HEK-293T C647(1.07); C455(0.99); C188(0.99); C356(1.09)  LDD1591  [24]
 LDCM0388  CL118 HEK-293T C647(1.05); C455(0.92); C356(1.38)  LDD1592  [24]
 LDCM0389  CL119 HEK-293T C647(1.03); C455(0.87); C188(1.06); C356(1.00)  LDD1593  [24]
 LDCM0390  CL12 HEK-293T C647(0.97); C455(0.96); C356(1.08)  LDD1594  [24]
 LDCM0391  CL120 HEK-293T C647(1.05); C455(0.90); C188(0.91); C356(1.07)  LDD1595  [24]
 LDCM0392  CL121 HEK-293T C647(1.00); C455(0.92); C188(0.99); C356(1.13)  LDD1596  [24]
 LDCM0393  CL122 HEK-293T C647(1.04); C455(0.95); C356(1.20)  LDD1597  [24]
 LDCM0394  CL123 HEK-293T C647(0.95); C455(0.85); C188(1.06); C356(1.04)  LDD1598  [24]
 LDCM0395  CL124 HEK-293T C647(1.00); C455(0.83); C188(1.03); C356(1.07)  LDD1599  [24]
 LDCM0396  CL125 HEK-293T C647(0.93); C455(1.00); C188(1.09); C356(1.34)  LDD1600  [24]
 LDCM0397  CL126 HEK-293T C647(1.02); C455(0.88); C356(1.10)  LDD1601  [24]
 LDCM0398  CL127 HEK-293T C647(1.11); C455(0.86); C188(1.04); C356(1.15)  LDD1602  [24]
 LDCM0399  CL128 HEK-293T C647(0.92); C455(0.90); C188(0.94); C356(1.13)  LDD1603  [24]
 LDCM0400  CL13 HEK-293T C647(0.86); C455(1.03); C188(0.88); C356(1.21)  LDD1604  [24]
 LDCM0401  CL14 HEK-293T C647(0.97); C455(0.88); C356(1.24)  LDD1605  [24]
 LDCM0402  CL15 HEK-293T C647(0.92); C455(0.76); C188(0.99); C356(1.10)  LDD1606  [24]
 LDCM0403  CL16 HEK-293T C647(0.94); C455(0.80); C188(0.87); C356(1.31)  LDD1607  [24]
 LDCM0404  CL17 HEK-293T C647(0.87); C455(0.83); C356(0.81)  LDD1608  [24]
 LDCM0405  CL18 HEK-293T C647(0.91); C455(0.96); C356(1.20)  LDD1609  [24]
 LDCM0406  CL19 HEK-293T C647(1.00); C455(0.99); C188(0.98); C356(1.16)  LDD1610  [24]
 LDCM0407  CL2 HEK-293T C647(1.01); C455(0.89); C356(1.17)  LDD1611  [24]
 LDCM0408  CL20 HEK-293T C455(0.95); C356(1.20)  LDD1612  [24]
 LDCM0409  CL21 HEK-293T C647(0.89); C455(0.82); C188(1.30); C356(0.87)  LDD1613  [24]
 LDCM0410  CL22 HEK-293T C647(0.93); C455(1.00); C356(1.01)  LDD1614  [24]
 LDCM0411  CL23 HEK-293T C647(0.98); C455(0.98); C188(1.19)  LDD1615  [24]
 LDCM0412  CL24 HEK-293T C647(1.00); C455(0.99); C356(1.23)  LDD1616  [24]
 LDCM0413  CL25 HEK-293T C647(0.95); C455(0.87); C188(1.05); C356(1.38)  LDD1617  [24]
 LDCM0414  CL26 HEK-293T C647(1.02); C455(0.88); C356(1.21)  LDD1618  [24]
 LDCM0415  CL27 HEK-293T C647(0.97); C455(0.88); C188(1.04); C356(0.95)  LDD1619  [24]
 LDCM0416  CL28 HEK-293T C647(0.92); C455(1.01); C188(0.89); C356(1.06)  LDD1620  [24]
 LDCM0417  CL29 HEK-293T C647(0.94); C455(1.03); C356(0.92)  LDD1621  [24]
 LDCM0418  CL3 HEK-293T C647(1.04); C455(0.86); C188(1.03); C356(1.19)  LDD1622  [24]
 LDCM0419  CL30 HEK-293T C647(0.99); C455(0.97); C356(1.36)  LDD1623  [24]
 LDCM0420  CL31 HEK-293T C647(1.07); C455(0.95); C188(1.03); C356(1.10)  LDD1624  [24]
 LDCM0421  CL32 HEK-293T C455(0.90); C356(1.07)  LDD1625  [24]
 LDCM0422  CL33 HEK-293T C647(1.10); C455(0.81); C188(1.39); C356(0.80)  LDD1626  [24]
 LDCM0423  CL34 HEK-293T C647(1.00); C455(0.96); C356(0.70)  LDD1627  [24]
 LDCM0424  CL35 HEK-293T C647(1.03); C455(1.05); C188(1.17)  LDD1628  [24]
 LDCM0425  CL36 HEK-293T C647(1.07); C455(0.99); C356(0.95)  LDD1629  [24]
 LDCM0426  CL37 HEK-293T C647(0.94); C455(0.96); C188(1.11); C356(1.16)  LDD1630  [24]
 LDCM0428  CL39 HEK-293T C647(0.96); C455(0.84); C188(1.00); C356(0.99)  LDD1632  [24]
 LDCM0429  CL4 HEK-293T C647(0.86); C455(0.82); C188(0.86); C356(1.07)  LDD1633  [24]
 LDCM0430  CL40 HEK-293T C647(0.96); C455(0.99); C188(0.87); C356(1.15)  LDD1634  [24]
 LDCM0431  CL41 HEK-293T C647(0.93); C455(0.99); C356(0.99)  LDD1635  [24]
 LDCM0432  CL42 HEK-293T C647(1.10); C455(0.98); C356(1.20)  LDD1636  [24]
 LDCM0433  CL43 HEK-293T C647(1.12); C455(0.91); C188(1.11); C356(0.99)  LDD1637  [24]
 LDCM0434  CL44 HEK-293T C455(0.90); C356(1.11)  LDD1638  [24]
 LDCM0435  CL45 HEK-293T C647(1.02); C455(0.91); C188(1.29); C356(1.15)  LDD1639  [24]
 LDCM0436  CL46 HEK-293T C647(1.15); C455(0.98); C356(0.86)  LDD1640  [24]
 LDCM0437  CL47 HEK-293T C647(1.00); C455(1.06); C188(1.18)  LDD1641  [24]
 LDCM0438  CL48 HEK-293T C647(1.09); C455(0.98); C356(1.04)  LDD1642  [24]
 LDCM0439  CL49 HEK-293T C647(0.97); C455(0.94); C188(1.04); C356(1.29)  LDD1643  [24]
 LDCM0440  CL5 HEK-293T C647(0.88); C455(0.88); C356(0.82)  LDD1644  [24]
 LDCM0441  CL50 HEK-293T C647(1.02); C455(0.89); C356(1.15)  LDD1645  [24]
 LDCM0443  CL52 HEK-293T C647(1.09); C455(0.89); C188(0.90); C356(1.14)  LDD1646  [24]
 LDCM0444  CL53 HEK-293T C647(0.97); C455(0.87); C356(0.76)  LDD1647  [24]
 LDCM0445  CL54 HEK-293T C647(0.99); C455(0.83); C356(1.08)  LDD1648  [24]
 LDCM0446  CL55 HEK-293T C647(1.17); C455(0.86); C188(1.08); C356(1.01)  LDD1649  [24]
 LDCM0447  CL56 HEK-293T C455(0.89); C356(1.11)  LDD1650  [24]
 LDCM0448  CL57 HEK-293T C647(1.00); C455(0.80); C188(1.39); C356(1.06)  LDD1651  [24]
 LDCM0449  CL58 HEK-293T C647(1.02); C455(0.95); C356(0.93)  LDD1652  [24]
 LDCM0450  CL59 HEK-293T C647(1.06); C455(0.99); C188(1.32)  LDD1653  [24]
 LDCM0451  CL6 HEK-293T C647(0.95); C455(0.89); C356(1.20)  LDD1654  [24]
 LDCM0452  CL60 HEK-293T C647(1.08); C455(0.81); C356(1.01)  LDD1655  [24]
 LDCM0453  CL61 HEK-293T C647(0.91); C455(0.96); C188(1.02); C356(1.16)  LDD1656  [24]
 LDCM0454  CL62 HEK-293T C647(0.98); C455(0.92); C356(1.08)  LDD1657  [24]
 LDCM0455  CL63 HEK-293T C647(1.01); C455(0.86); C188(0.94); C356(0.99)  LDD1658  [24]
 LDCM0456  CL64 HEK-293T C647(0.99); C455(0.79); C188(0.90); C356(1.12)  LDD1659  [24]
 LDCM0457  CL65 HEK-293T C647(0.93); C455(0.98); C356(0.94)  LDD1660  [24]
 LDCM0458  CL66 HEK-293T C647(1.02); C455(0.90); C356(1.34)  LDD1661  [24]
 LDCM0459  CL67 HEK-293T C647(1.04); C455(0.90); C188(1.01); C356(1.12)  LDD1662  [24]
 LDCM0460  CL68 HEK-293T C455(0.92); C356(1.02)  LDD1663  [24]
 LDCM0461  CL69 HEK-293T C647(1.08); C455(0.84); C188(1.36); C356(1.01)  LDD1664  [24]
 LDCM0462  CL7 HEK-293T C647(0.98); C455(1.01); C188(1.15); C356(1.15)  LDD1665  [24]
 LDCM0463  CL70 HEK-293T C647(1.03); C455(0.98); C356(0.86)  LDD1666  [24]
 LDCM0464  CL71 HEK-293T C647(0.99); C455(1.03); C188(1.13)  LDD1667  [24]
 LDCM0465  CL72 HEK-293T C647(1.03); C455(1.01); C356(1.06)  LDD1668  [24]
 LDCM0466  CL73 HEK-293T C647(0.93); C455(0.92); C188(1.22); C356(1.16)  LDD1669  [24]
 LDCM0467  CL74 HEK-293T C647(1.05); C455(0.87); C356(1.05)  LDD1670  [24]
 LDCM0469  CL76 HEK-293T C647(0.97); C455(0.90); C188(0.90); C356(1.19)  LDD1672  [24]
 LDCM0470  CL77 HEK-293T C647(0.97); C455(0.86); C356(0.98)  LDD1673  [24]
 LDCM0471  CL78 HEK-293T C647(1.04); C455(0.95); C356(1.02)  LDD1674  [24]
 LDCM0472  CL79 HEK-293T C647(1.18); C455(0.94); C188(1.01); C356(1.04)  LDD1675  [24]
 LDCM0473  CL8 HEK-293T C455(0.71); C356(1.16)  LDD1676  [24]
 LDCM0474  CL80 HEK-293T C455(0.88); C356(1.03)  LDD1677  [24]
 LDCM0475  CL81 HEK-293T C647(0.93); C455(0.93); C188(1.15); C356(0.80)  LDD1678  [24]
 LDCM0476  CL82 HEK-293T C647(1.12); C455(0.96); C356(0.87)  LDD1679  [24]
 LDCM0477  CL83 HEK-293T C647(1.01); C455(1.02); C188(1.30)  LDD1680  [24]
 LDCM0478  CL84 HEK-293T C647(1.11); C455(1.02); C356(0.99)  LDD1681  [24]
 LDCM0479  CL85 HEK-293T C647(0.78); C455(0.93); C188(0.98); C356(1.09)  LDD1682  [24]
 LDCM0480  CL86 HEK-293T C647(0.97); C455(0.88); C356(1.07)  LDD1683  [24]
 LDCM0481  CL87 HEK-293T C647(0.98); C455(0.88); C188(1.02); C356(1.16)  LDD1684  [24]
 LDCM0482  CL88 HEK-293T C647(1.03); C455(0.88); C188(0.94); C356(1.17)  LDD1685  [24]
 LDCM0483  CL89 HEK-293T C647(0.99); C455(0.97); C356(0.96)  LDD1686  [24]
 LDCM0484  CL9 HEK-293T C647(0.91); C455(0.86); C188(1.28); C356(0.96)  LDD1687  [24]
 LDCM0485  CL90 HEK-293T C647(1.08); C455(0.82); C356(1.01)  LDD1688  [24]
 LDCM0486  CL91 HEK-293T C647(1.14); C455(0.85); C188(1.03); C356(1.22)  LDD1689  [24]
 LDCM0487  CL92 HEK-293T C455(0.76); C356(1.16)  LDD1690  [24]
 LDCM0488  CL93 HEK-293T C647(0.99); C455(0.82); C188(1.24); C356(0.92)  LDD1691  [24]
 LDCM0489  CL94 HEK-293T C647(1.08); C455(0.96); C356(0.99)  LDD1692  [24]
 LDCM0490  CL95 HEK-293T C647(1.09); C455(0.91); C188(1.23)  LDD1693  [24]
 LDCM0491  CL96 HEK-293T C647(1.05); C455(0.88); C356(1.07)  LDD1694  [24]
 LDCM0492  CL97 HEK-293T C647(0.99); C455(0.96); C188(1.03); C356(1.26)  LDD1695  [24]
 LDCM0493  CL98 HEK-293T C647(1.00); C455(0.86); C356(1.06)  LDD1696  [24]
 LDCM0494  CL99 HEK-293T C647(0.97); C455(0.88); C188(0.97); C356(0.87)  LDD1697  [24]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [23]
 LDCM0634  CY-0357 Hep-G2 C455(0.47)  LDD2228  [12]
 LDCM0495  E2913 HEK-293T C647(0.98); C455(0.83); C188(1.00); C356(1.09)  LDD1698  [24]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C188(6.85); C502(0.87)  LDD1702  [5]
 LDCM0625  F8 Ramos C455(1.30)  LDD2187  [25]
 LDCM0572  Fragment10 Ramos C455(0.91)  LDD2189  [25]
 LDCM0573  Fragment11 Ramos C455(0.85)  LDD2190  [25]
 LDCM0574  Fragment12 Ramos C455(0.91)  LDD2191  [25]
 LDCM0575  Fragment13 Ramos C455(0.95)  LDD2192  [25]
 LDCM0576  Fragment14 Ramos C455(0.83)  LDD2193  [25]
 LDCM0579  Fragment20 Ramos C455(0.59)  LDD2194  [25]
 LDCM0580  Fragment21 Ramos C455(0.96)  LDD2195  [25]
 LDCM0582  Fragment23 Ramos C455(0.95)  LDD2196  [25]
 LDCM0578  Fragment27 Ramos C455(0.88)  LDD2197  [25]
 LDCM0586  Fragment28 Ramos C455(0.82)  LDD2198  [25]
 LDCM0588  Fragment30 Ramos C455(1.00)  LDD2199  [25]
 LDCM0589  Fragment31 Ramos C455(0.81)  LDD2200  [25]
 LDCM0590  Fragment32 Ramos C455(0.91)  LDD2201  [25]
 LDCM0468  Fragment33 HEK-293T C647(0.99); C455(0.89); C188(1.09); C356(1.00)  LDD1671  [24]
 LDCM0596  Fragment38 Ramos C455(1.04)  LDD2203  [25]
 LDCM0566  Fragment4 Ramos C455(1.18)  LDD2184  [25]
 LDCM0427  Fragment51 HEK-293T C647(1.08); C455(0.94); C356(1.22)  LDD1631  [24]
 LDCM0610  Fragment52 Ramos C455(1.36)  LDD2204  [25]
 LDCM0614  Fragment56 Ramos C455(1.32)  LDD2205  [25]
 LDCM0569  Fragment7 Ramos C455(1.33)  LDD2186  [25]
 LDCM0571  Fragment9 Ramos C455(0.91)  LDD2188  [25]
 LDCM0107  IAA HeLa N.A.  LDD0221  [18]
 LDCM0022  KB02 HEK-293T C647(0.90); C455(0.99); C63(0.79); C188(0.86)  LDD1492  [24]
 LDCM0023  KB03 HEK-293T C647(0.98); C455(1.00); C63(0.98); C188(0.89)  LDD1497  [24]
 LDCM0024  KB05 HMCB C359(3.35)  LDD3312  [4]
 LDCM0030  Luteolin HEK-293T 5.05  LDD0182  [6]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C188(0.70)  LDD2102  [5]
 LDCM0109  NEM HeLa H211(0.00); C647(0.00)  LDD0223  [18]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C188(0.50)  LDD2089  [5]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C188(0.21)  LDD2101  [5]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C455(0.85)  LDD2106  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C188(0.96)  LDD2107  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C188(0.79)  LDD2109  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C188(0.69)  LDD2111  [5]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C188(0.29)  LDD2115  [5]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C455(0.98)  LDD2118  [5]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C188(1.07)  LDD2119  [5]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C455(1.01)  LDD2122  [5]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C188(0.95)  LDD2123  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C188(1.07); C455(1.25)  LDD2125  [5]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C455(0.97)  LDD2126  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C188(1.06); C455(1.28)  LDD2127  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C188(0.80)  LDD2129  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C188(0.25)  LDD2134  [5]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C188(0.83)  LDD2135  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C502(1.06)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C188(1.12)  LDD2137  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C188(0.52)  LDD2140  [5]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C188(1.33)  LDD2143  [5]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C188(1.03)  LDD2144  [5]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C188(0.65)  LDD2146  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C188(0.30); C647(0.73)  LDD2148  [5]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C188(0.44); C455(0.58)  LDD2150  [5]
 LDCM0032  Oleacein HEK-293T 4.75  LDD0184  [6]
 LDCM0131  RA190 MM1.R C356(1.41); C455(1.22)  LDD0304  [26]

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
ATP-dependent RNA helicase DHX8 (DHX8) DEAD box helicase family Q14562
Ubiquitin carboxyl-terminal hydrolase 39 (USP39) Peptidase C19 family Q53GS9
SRSF protein kinase 3 (SRPK3) CMGC Ser/Thr protein kinase family Q9UPE1
Cyclin-dependent kinase 7 (CDK7) CMGC Ser/Thr protein kinase family P50613
Focal adhesion kinase 1 (PTK2) Tyr protein kinase family Q05397
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
RNA-binding protein 8A (RBM8A) RBM8A family Q9Y5S9
RNA-binding protein with serine-rich domain 1 (RNPS1) Splicing factor SR family Q15287
Other
Click To Hide/Show 15 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
KRR1 small subunit processome component homolog (KRR1) KRR1 family Q13601
Putative RNA-binding protein Luc7-like 1 (LUC7L) Luc7 family Q9NQ29
Putative RNA-binding protein Luc7-like 2 (LUC7L2) Luc7 family Q9Y383
Pre-mRNA-splicing factor 38A (PRPF38A) PRP38 family Q8NAV1
RNA-binding protein 39 (RBM39) Splicing factor SR family Q14498
Serine/arginine-rich splicing factor 1 (SRSF1) Splicing factor SR family Q07955
Serine/arginine-rich splicing factor 7 (SRSF7) Splicing factor SR family Q16629
Serine/arginine-rich splicing factor 8 (SRSF8) Splicing factor SR family Q9BRL6
Splicing factor U2AF 35 kDa subunit (U2AF1) Splicing factor SR family Q01081
Splicing regulatory glutamine/lysine-rich protein 1 (SREK1) Splicing factor SR family Q8WXA9
Microprocessor complex subunit DGCR8 (DGCR8) . Q8WYQ5
Scaffold attachment factor B1 (SAFB) . Q15424
U1 small nuclear ribonucleoprotein 70 kDa (SNRNP70) . P08621
U2 small nuclear ribonucleoprotein auxiliary factor 35 kDa subunit-related protein 2 (ZRSR2) . Q15696
YTH domain-containing protein 1 (YTHDC1) . Q96MU7

The Drug(s) Related To This Target

Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sphinx31 Small molecular drug D86ILE
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid15925511c13 Small molecular drug D0J1JB
Patented
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sphinx Small molecular drug D0LA9D
Sphinx Scaffold, 3 Small molecular drug D0NY4A
Zinc959121 Small molecular drug D03OBN

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 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
5 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
6 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
7 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
8 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
9 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
10 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
11 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
12 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
13 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
14 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
15 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
16 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
17 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
18 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.
19 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
20 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
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Mass spectrometry data entry: PXD041587
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Mass spectrometry data entry: PXD044402
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Mass spectrometry data entry: PXD027578
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