Details of the Target

General Information of Target

Target ID LDTP07930
Target Name Serine/threonine-protein kinase MARK2 (MARK2)
Gene Name MARK2
Gene ID 2011
Synonyms
EMK1; Serine/threonine-protein kinase MARK2; EC 2.7.11.1; EC 2.7.11.26; ELKL motif kinase 1; EMK-1; MAP/microtubule affinity-regulating kinase 2; PAR1 homolog; PAR1 homolog b; Par-1b; Par1b
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSSARTPLPTLNERDTEQPTLGHLDSKPSSKSNMIRGRNSATSADEQPHIGNYRLLKTIG
KGNFAKVKLARHILTGKEVAVKIIDKTQLNSSSLQKLFREVRIMKVLNHPNIVKLFEVIE
TEKTLYLVMEYASGGEVFDYLVAHGRMKEKEARAKFRQIVSAVQYCHQKFIVHRDLKAEN
LLLDADMNIKIADFGFSNEFTFGNKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLGVIL
YTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKKFLILNPSKRGTLEQIMK
DRWMNVGHEDDELKPYVEPLPDYKDPRRTELMVSMGYTREEIQDSLVGQRYNEVMATYLL
LGYKSSELEGDTITLKPRPSADLTNSSAPSPSHKVQRSVSANPKQRRFSDQAAGPAIPTS
NSYSKKTQSNNAENKRPEEDRESGRKASSTAKVPASPLPGLERKKTTPTPSTNSVLSTST
NRSRNSPLLERASLGQASIQNGKDSLTMPGSRASTASASAAVSAARPRQHQKSMSASVHP
NKASGLPPTESNCEVPRPSTAPQRVPVASPSAHNISSSGGAPDRTNFPRGVSSRSTFHAG
QLRQVRDQQNLPYGVTPASPSGHSQGRRGASGSIFSKFTSKFVRRNLSFRFARRNLNEPE
SKDRVETLRPHVVGSGGNDKEKEEFREAKPRSLRFTWSMKTTSSMEPNEMMREIRKVLDA
NSCQSELHEKYMLLCMHGTPGHEDFVQWEMEVCKLPRLSLNGVRFKRISGTSMAFKNIAS
KIANELKL
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, SNF1 subfamily
Subcellular location
Cell membrane
Function
Serine/threonine-protein kinase. Involved in cell polarity and microtubule dynamics regulation. Phosphorylates CRTC2/TORC2, DCX, HDAC7, KIF13B, MAP2, MAP4 and RAB11FIP2. Phosphorylates the microtubule-associated protein MAPT/TAU. Plays a key role in cell polarity by phosphorylating the microtubule-associated proteins MAP2, MAP4 and MAPT/TAU at KXGS motifs, causing detachment from microtubules, and their disassembly. Regulates epithelial cell polarity by phosphorylating RAB11FIP2. Involved in the regulation of neuronal migration through its dual activities in regulating cellular polarity and microtubule dynamics, possibly by phosphorylating and regulating DCX. Regulates axogenesis by phosphorylating KIF13B, promoting interaction between KIF13B and 14-3-3 and inhibiting microtubule-dependent accumulation of KIF13B. Also required for neurite outgrowth and establishment of neuronal polarity. Regulates localization and activity of some histone deacetylases by mediating phosphorylation of HDAC7, promoting subsequent interaction between HDAC7 and 14-3-3 and export from the nucleus. Also acts as a positive regulator of the Wnt signaling pathway, probably by mediating phosphorylation of dishevelled proteins (DVL1, DVL2 and/or DVL3). Modulates the developmental decision to build a columnar versus a hepatic epithelial cell apparently by promoting a switch from a direct to a transcytotic mode of apical protein delivery. Essential for the asymmetric development of membrane domains of polarized epithelial cells.
TTD ID
T01396
Uniprot ID
Q7KZI7
DrugMap ID
TTAJ45Y
Ensemble ID
ENST00000350490.11
HGNC ID
HGNC:3332
ChEMBL ID
CHEMBL3831

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.R259P DBIA    Probe Info 
HDMYZ SNV: p.K464R DBIA    Probe Info 
HT115 SNV: p.R407H DBIA    Probe Info 
KYSE150 Substitution: p.P588F DBIA    Probe Info 
KYSE30 Substitution: p.A217S DBIA    Probe Info 
LNCaP clone FGC SNV: p.L21S DBIA    Probe Info 
MELHO Substitution: p.R445Q DBIA    Probe Info 
MEWO SNV: p.R153G DBIA    Probe Info 
OVK18 Insertion: p.Y226IfsTer2 DBIA    Probe Info 
RKO SNV: p.A70T DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		14.52  LDD0402  [1]
TH211
 Probe Info  		Y53(9.07)  LDD0257  [2]
STPyne
 Probe Info  		K641(5.77); K776(9.20)  LDD0277  [3]
BTD
 Probe Info  		C723(0.83)  LDD2089  [4]
DBIA
 Probe Info  		C553(13.77)  LDD0204  [5]
IPM
 Probe Info  		C723(1.77)  LDD1702  [4]
ATP probe
 Probe Info  		K96(0.00); K394(0.00)  LDD0199  [6]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [7]
Lodoacetamide azide
 Probe Info  		C166(0.00); C723(0.00); C277(0.00)  LDD0037  [7]
ATP probe
 Probe Info  		K177(0.00); K82(0.00)  LDD0035  [8]
WYneN
 Probe Info  		N.A.  LDD0021  [9]
KY-26
 Probe Info  		N.A.  LDD0301  [10]
SF
 Probe Info  		N.A.  LDD0028  [11]
AOyne
 Probe Info  		6.30  LDD0443  [12]
NAIA_5
 Probe Info  		C723(0.00); C277(0.00)  LDD2223  [13]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C338
 Probe Info  		17.03  LDD2001  [14]
Staurosporine capture compound
 Probe Info  		N.A.  LDD0083  [15]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C723(0.65)  LDD2130  [4]
 LDCM0214  AC1 HEK-293T C553(1.19)  LDD1507  [16]
 LDCM0215  AC10 HEK-293T C553(0.89)  LDD1508  [16]
 LDCM0226  AC11 HEK-293T C553(1.01)  LDD1509  [16]
 LDCM0237  AC12 HEK-293T C553(1.17)  LDD1510  [16]
 LDCM0259  AC14 HEK-293T C553(0.86)  LDD1512  [16]
 LDCM0270  AC15 HEK-293T C553(0.91)  LDD1513  [16]
 LDCM0276  AC17 HEK-293T C553(1.04)  LDD1515  [16]
 LDCM0277  AC18 HEK-293T C553(0.99)  LDD1516  [16]
 LDCM0278  AC19 HEK-293T C553(1.16)  LDD1517  [16]
 LDCM0279  AC2 HEK-293T C553(0.94)  LDD1518  [16]
 LDCM0280  AC20 HEK-293T C553(1.08)  LDD1519  [16]
 LDCM0281  AC21 HEK-293T C553(1.03)  LDD1520  [16]
 LDCM0282  AC22 HEK-293T C553(0.83)  LDD1521  [16]
 LDCM0283  AC23 HEK-293T C553(0.89)  LDD1522  [16]
 LDCM0285  AC25 HEK-293T C553(1.09)  LDD1524  [16]
 LDCM0286  AC26 HEK-293T C553(0.97)  LDD1525  [16]
 LDCM0287  AC27 HEK-293T C553(1.16)  LDD1526  [16]
 LDCM0288  AC28 HEK-293T C553(1.03)  LDD1527  [16]
 LDCM0289  AC29 HEK-293T C553(1.01)  LDD1528  [16]
 LDCM0290  AC3 HEK-293T C553(0.99)  LDD1529  [16]
 LDCM0291  AC30 HEK-293T C553(1.06)  LDD1530  [16]
 LDCM0292  AC31 HEK-293T C553(0.93)  LDD1531  [16]
 LDCM0294  AC33 HEK-293T C553(1.22)  LDD1533  [16]
 LDCM0295  AC34 HEK-293T C553(0.87)  LDD1534  [16]
 LDCM0296  AC35 HEK-293T C553(1.00)  LDD1535  [16]
 LDCM0297  AC36 HEK-293T C553(0.84)  LDD1536  [16]
 LDCM0298  AC37 HEK-293T C553(1.05)  LDD1537  [16]
 LDCM0299  AC38 HEK-293T C553(0.83)  LDD1538  [16]
 LDCM0300  AC39 HEK-293T C553(0.91)  LDD1539  [16]
 LDCM0301  AC4 HEK-293T C553(0.95)  LDD1540  [16]
 LDCM0303  AC41 HEK-293T C553(1.13)  LDD1542  [16]
 LDCM0304  AC42 HEK-293T C553(1.03)  LDD1543  [16]
 LDCM0305  AC43 HEK-293T C553(1.11)  LDD1544  [16]
 LDCM0306  AC44 HEK-293T C553(1.01)  LDD1545  [16]
 LDCM0307  AC45 HEK-293T C553(1.09)  LDD1546  [16]
 LDCM0308  AC46 HEK-293T C553(1.04)  LDD1547  [16]
 LDCM0309  AC47 HEK-293T C553(0.87)  LDD1548  [16]
 LDCM0311  AC49 HEK-293T C553(1.12)  LDD1550  [16]
 LDCM0312  AC5 HEK-293T C553(1.04)  LDD1551  [16]
 LDCM0313  AC50 HEK-293T C553(1.05)  LDD1552  [16]
 LDCM0314  AC51 HEK-293T C553(1.10)  LDD1553  [16]
 LDCM0315  AC52 HEK-293T C553(1.18)  LDD1554  [16]
 LDCM0316  AC53 HEK-293T C553(1.06)  LDD1555  [16]
 LDCM0317  AC54 HEK-293T C553(0.95)  LDD1556  [16]
 LDCM0318  AC55 HEK-293T C553(0.86)  LDD1557  [16]
 LDCM0320  AC57 HEK-293T C553(1.22)  LDD1559  [16]
 LDCM0321  AC58 HEK-293T C553(0.88)  LDD1560  [16]
 LDCM0322  AC59 HEK-293T C553(1.04)  LDD1561  [16]
 LDCM0323  AC6 HEK-293T C553(0.83)  LDD1562  [16]
 LDCM0324  AC60 HEK-293T C553(1.02)  LDD1563  [16]
 LDCM0325  AC61 HEK-293T C553(1.09)  LDD1564  [16]
 LDCM0326  AC62 HEK-293T C553(0.88)  LDD1565  [16]
 LDCM0327  AC63 HEK-293T C553(1.08)  LDD1566  [16]
 LDCM0334  AC7 HEK-293T C553(1.01)  LDD1568  [16]
 LDCM0248  AKOS034007472 HEK-293T C553(1.01)  LDD1511  [16]
 LDCM0356  AKOS034007680 HEK-293T C553(1.09)  LDD1570  [16]
 LDCM0156  Aniline NCI-H1299 14.10  LDD0403  [1]
 LDCM0102  BDHI 8 Jurkat C553(13.77)  LDD0204  [5]
 LDCM0632  CL-Sc Hep-G2 C166(3.40)  LDD2227  [13]
 LDCM0367  CL1 HEK-293T C553(1.04); C723(1.11)  LDD1571  [16]
 LDCM0368  CL10 HEK-293T C553(1.01)  LDD1572  [16]
 LDCM0369  CL100 HEK-293T C553(1.08); C723(1.02)  LDD1573  [16]
 LDCM0370  CL101 HEK-293T C553(1.17); C723(1.03)  LDD1574  [16]
 LDCM0372  CL103 HEK-293T C553(1.02)  LDD1576  [16]
 LDCM0373  CL104 HEK-293T C553(1.09); C723(0.99)  LDD1577  [16]
 LDCM0374  CL105 HEK-293T C553(0.96); C723(1.03)  LDD1578  [16]
 LDCM0376  CL107 HEK-293T C553(0.94)  LDD1580  [16]
 LDCM0377  CL108 HEK-293T C553(0.91); C723(0.95)  LDD1581  [16]
 LDCM0378  CL109 HEK-293T C553(0.99); C723(0.95)  LDD1582  [16]
 LDCM0379  CL11 HEK-293T C553(0.93)  LDD1583  [16]
 LDCM0381  CL111 HEK-293T C553(0.98)  LDD1585  [16]
 LDCM0382  CL112 HEK-293T C553(1.05); C723(0.98)  LDD1586  [16]
 LDCM0383  CL113 HEK-293T C553(0.91); C723(0.90)  LDD1587  [16]
 LDCM0385  CL115 HEK-293T C553(0.99)  LDD1589  [16]
 LDCM0386  CL116 HEK-293T C553(1.12); C723(1.06)  LDD1590  [16]
 LDCM0387  CL117 HEK-293T C553(1.00); C723(1.00)  LDD1591  [16]
 LDCM0389  CL119 HEK-293T C553(1.07)  LDD1593  [16]
 LDCM0391  CL120 HEK-293T C553(1.05); C723(1.02)  LDD1595  [16]
 LDCM0392  CL121 HEK-293T C553(0.90); C723(0.97)  LDD1596  [16]
 LDCM0394  CL123 HEK-293T C553(0.82)  LDD1598  [16]
 LDCM0395  CL124 HEK-293T C553(1.13); C723(1.00)  LDD1599  [16]
 LDCM0396  CL125 HEK-293T C553(0.86); C723(0.81)  LDD1600  [16]
 LDCM0398  CL127 HEK-293T C553(1.06)  LDD1602  [16]
 LDCM0399  CL128 HEK-293T C553(1.32); C723(1.00)  LDD1603  [16]
 LDCM0400  CL13 HEK-293T C553(1.24); C723(0.97)  LDD1604  [16]
 LDCM0402  CL15 HEK-293T C553(1.05)  LDD1606  [16]
 LDCM0403  CL16 HEK-293T C553(1.04); C723(1.15)  LDD1607  [16]
 LDCM0404  CL17 HEK-293T C553(0.97)  LDD1608  [16]
 LDCM0405  CL18 HEK-293T C553(1.02)  LDD1609  [16]
 LDCM0406  CL19 HEK-293T C553(1.15)  LDD1610  [16]
 LDCM0408  CL20 HEK-293T C553(1.27)  LDD1612  [16]
 LDCM0409  CL21 HEK-293T C553(0.88)  LDD1613  [16]
 LDCM0410  CL22 HEK-293T C553(1.04)  LDD1614  [16]
 LDCM0411  CL23 HEK-293T C553(0.98)  LDD1615  [16]
 LDCM0413  CL25 HEK-293T C553(0.89); C723(0.92)  LDD1617  [16]
 LDCM0415  CL27 HEK-293T C553(1.07)  LDD1619  [16]
 LDCM0416  CL28 HEK-293T C553(1.04); C723(0.99)  LDD1620  [16]
 LDCM0417  CL29 HEK-293T C553(1.04)  LDD1621  [16]
 LDCM0418  CL3 HEK-293T C553(0.84)  LDD1622  [16]
 LDCM0419  CL30 HEK-293T C553(0.87)  LDD1623  [16]
 LDCM0420  CL31 HEK-293T C553(0.89)  LDD1624  [16]
 LDCM0421  CL32 HEK-293T C553(1.19)  LDD1625  [16]
 LDCM0422  CL33 HEK-293T C553(0.82)  LDD1626  [16]
 LDCM0423  CL34 HEK-293T C553(1.03)  LDD1627  [16]
 LDCM0424  CL35 HEK-293T C553(0.78)  LDD1628  [16]
 LDCM0426  CL37 HEK-293T C553(0.97); C723(1.24)  LDD1630  [16]
 LDCM0428  CL39 HEK-293T C553(0.93)  LDD1632  [16]
 LDCM0429  CL4 HEK-293T C553(1.16); C723(1.06)  LDD1633  [16]
 LDCM0430  CL40 HEK-293T C553(0.99); C723(0.96)  LDD1634  [16]
 LDCM0431  CL41 HEK-293T C553(1.08)  LDD1635  [16]
 LDCM0432  CL42 HEK-293T C553(1.05)  LDD1636  [16]
 LDCM0433  CL43 HEK-293T C553(1.11)  LDD1637  [16]
 LDCM0434  CL44 HEK-293T C553(1.01)  LDD1638  [16]
 LDCM0435  CL45 HEK-293T C553(0.87)  LDD1639  [16]
 LDCM0436  CL46 HEK-293T C553(1.02)  LDD1640  [16]
 LDCM0437  CL47 HEK-293T C553(0.81)  LDD1641  [16]
 LDCM0439  CL49 HEK-293T C553(1.04); C723(0.93)  LDD1643  [16]
 LDCM0440  CL5 HEK-293T C553(1.17)  LDD1644  [16]
 LDCM0443  CL52 HEK-293T C553(0.92); C723(1.10)  LDD1646  [16]
 LDCM0444  CL53 HEK-293T C553(1.10)  LDD1647  [16]
 LDCM0445  CL54 HEK-293T C553(0.96)  LDD1648  [16]
 LDCM0446  CL55 HEK-293T C553(1.06)  LDD1649  [16]
 LDCM0447  CL56 HEK-293T C553(1.17)  LDD1650  [16]
 LDCM0448  CL57 HEK-293T C553(0.90)  LDD1651  [16]
 LDCM0449  CL58 HEK-293T C553(0.88)  LDD1652  [16]
 LDCM0450  CL59 HEK-293T C553(0.78)  LDD1653  [16]
 LDCM0451  CL6 HEK-293T C553(1.04)  LDD1654  [16]
 LDCM0453  CL61 HEK-293T C553(0.86); C723(1.10)  LDD1656  [16]
 LDCM0455  CL63 HEK-293T C553(0.99)  LDD1658  [16]
 LDCM0456  CL64 HEK-293T C553(1.16); C723(1.08)  LDD1659  [16]
 LDCM0457  CL65 HEK-293T C553(1.04)  LDD1660  [16]
 LDCM0458  CL66 HEK-293T C553(0.88)  LDD1661  [16]
 LDCM0459  CL67 HEK-293T C553(1.07)  LDD1662  [16]
 LDCM0460  CL68 HEK-293T C553(1.15)  LDD1663  [16]
 LDCM0461  CL69 HEK-293T C553(0.97)  LDD1664  [16]
 LDCM0462  CL7 HEK-293T C553(1.12)  LDD1665  [16]
 LDCM0463  CL70 HEK-293T C553(1.04)  LDD1666  [16]
 LDCM0464  CL71 HEK-293T C553(0.90)  LDD1667  [16]
 LDCM0466  CL73 HEK-293T C553(0.94); C723(1.14)  LDD1669  [16]
 LDCM0469  CL76 HEK-293T C553(1.06); C723(1.06)  LDD1672  [16]
 LDCM0470  CL77 HEK-293T C553(1.08)  LDD1673  [16]
 LDCM0471  CL78 HEK-293T C553(0.96)  LDD1674  [16]
 LDCM0472  CL79 HEK-293T C553(1.05)  LDD1675  [16]
 LDCM0473  CL8 HEK-293T C553(0.69)  LDD1676  [16]
 LDCM0474  CL80 HEK-293T C553(1.70)  LDD1677  [16]
 LDCM0475  CL81 HEK-293T C553(0.88)  LDD1678  [16]
 LDCM0476  CL82 HEK-293T C553(0.92)  LDD1679  [16]
 LDCM0477  CL83 HEK-293T C553(0.91)  LDD1680  [16]
 LDCM0479  CL85 HEK-293T C553(0.94); C723(0.95)  LDD1682  [16]
 LDCM0481  CL87 HEK-293T C553(1.06)  LDD1684  [16]
 LDCM0482  CL88 HEK-293T C553(1.27); C723(0.99)  LDD1685  [16]
 LDCM0483  CL89 HEK-293T C553(1.31)  LDD1686  [16]
 LDCM0484  CL9 HEK-293T C553(1.00)  LDD1687  [16]
 LDCM0485  CL90 HEK-293T C553(1.01)  LDD1688  [16]
 LDCM0486  CL91 HEK-293T C553(1.08)  LDD1689  [16]
 LDCM0487  CL92 HEK-293T C553(1.20)  LDD1690  [16]
 LDCM0488  CL93 HEK-293T C553(0.91)  LDD1691  [16]
 LDCM0489  CL94 HEK-293T C553(0.97)  LDD1692  [16]
 LDCM0490  CL95 HEK-293T C553(0.88)  LDD1693  [16]
 LDCM0492  CL97 HEK-293T C553(0.93); C723(0.91)  LDD1695  [16]
 LDCM0494  CL99 HEK-293T C553(1.08)  LDD1697  [16]
 LDCM0495  E2913 HEK-293T C553(1.00)  LDD1698  [16]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C723(1.77)  LDD1702  [4]
 LDCM0468  Fragment33 HEK-293T C553(1.07)  LDD1671  [16]
 LDCM0022  KB02 HEK-293T C553(1.33)  LDD1492  [16]
 LDCM0023  KB03 Jurkat C277(83.81); C210(5.76)  LDD0209  [5]
 LDCM0024  KB05 G361 C82(3.31); C38(2.21)  LDD3311  [17]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C723(0.64)  LDD2121  [4]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C723(0.83)  LDD2089  [4]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [15]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein gamma (YWHAG) 14-3-3 family P61981
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein beta/alpha (YWHAB) 14-3-3 family P31946
14-3-3 protein eta (YWHAH) 14-3-3 family Q04917
Partitioning defective 6 homolog gamma (PARD6G) PAR6 family Q9BYG4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010

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 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 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
4 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
5 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
6 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.
7 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
8 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
9 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
10 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
11 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
12 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.
13 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
14 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
15 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
16 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
17 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