General Information of Target

Target ID LDTP03828
Target Name Sterol regulatory element-binding protein 1 (SREBF1)
Gene Name SREBF1
Gene ID 6720
Synonyms
BHLHD1; SREBP1; Sterol regulatory element-binding protein 1; SREBP-1; Class D basic helix-loop-helix protein 1; bHLHd1; Sterol regulatory element-binding transcription factor 1) [Cleaved into: Processed sterol regulatory element-binding protein 1; Transcription factor SREBF1)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDEPPFSEAALEQALGEPCDLDAALLTDIEDMLQLINNQDSDFPGLFDPPYAGSGAGGTD
PASPDTSSPGSLSPPPATLSSSLEAFLSGPQAAPSPLSPPQPAPTPLKMYPSMPAFSPGP
GIKEESVPLSILQTPTPQPLPGALLPQSFPAPAPPQFSSTPVLGYPSPPGGFSTGSPPGN
TQQPLPGLPLASPPGVPPVSLHTQVQSVVPQQLLTVTAAPTAAPVTTTVTSQIQQVPVLL
QPHFIKADSLLLTAMKTDGATVKAAGLSPLVSGTTVQTGPLPTLVSGGTILATVPLVVDA
EKLPINRLAAGSKAPASAQSRGEKRTAHNAIEKRYRSSINDKIIELKDLVVGTEAKLNKS
AVLRKAIDYIRFLQHSNQKLKQENLSLRTAVHKSKSLKDLVSACGSGGNTDVLMEGVKTE
VEDTLTPPPSDAGSPFQSSPLSLGSRGSGSGGSGSDSEPDSPVFEDSKAKPEQRPSLHSR
GMLDRSRLALCTLVFLCLSCNPLASLLGARGLPSPSDTTSVYHSPGRNVLGTESRDGPGW
AQWLLPPVVWLLNGLLVLVSLVLLFVYGEPVTRPHSGPAVYFWRHRKQADLDLARGDFAQ
AAQQLWLALRALGRPLPTSHLDLACSLLWNLIRHLLQRLWVGRWLAGRAGGLQQDCALRV
DASASARDAALVYHKLHQLHTMGKHTGGHLTATNLALSALNLAECAGDAVSVATLAEIYV
AAALRVKTSLPRALHFLTRFFLSSARQACLAQSGSVPPAMQWLCHPVGHRFFVDGDWSVL
STPWESLYSLAGNPVDPLAQVTQLFREHLLERALNCVTQPNPSPGSADGDKEFSDALGYL
QLLNSCSDAAGAPAYSFSISSSMATTTGVDPVAKWWASLTAVVIHWLRRDEEAAERLCPL
VEHLPRVLQESERPLPRAALHSFKAARALLGCAKAESGPASLTICEKASGYLQDSLATTP
ASSSIDKAVQLFLCDLLLVVRTSLWRQQQPPAPAPAAQGTSSRPQASALELRGFQRDLSS
LRRLAQSFRPAMRRVFLHEATARLMAGASPTRTHQLLDRSLRRRAGPGGKGGAVAELEPR
PTRREHAEALLLASCYLPPGFLSAPGQRVGMLAEAARTLEKLGDRRLLHDCQQMLMRLGG
GTTVTSS
Target Type
Literature-reported
Target Bioclass
Transcription factor
Family
SREBP family
Subcellular location
Nucleus; Endoplasmic reticulum membrane
Function
[Sterol regulatory element-binding protein 1]: Precursor of the transcription factor form (Processed sterol regulatory element-binding protein 1), which is embedded in the endoplasmic reticulum membrane. Low sterol concentrations promote processing of this form, releasing the transcription factor form that translocates into the nucleus and activates transcription of genes involved in cholesterol biosynthesis and lipid homeostasis.; [Processed sterol regulatory element-binding protein 1]: Key transcription factor that regulates expression of genes involved in cholesterol biosynthesis and lipid homeostasis. Binds to the sterol regulatory element 1 (SRE-1) (5'-ATCACCCCAC-3'). Has dual sequence specificity binding to both an E-box motif (5'-ATCACGTGA-3') and to SRE-1 (5'-ATCACCCCAC-3'). Regulates the promoters of genes involved in cholesterol biosynthesis and the LDL receptor (LDLR) pathway of sterol regulation.; [Isoform SREBP-1A]: Isoform expressed only in select tissues, which has higher transcriptional activity compared to SREBP-1C. Able to stimulate both lipogenic and cholesterogenic gene expression. Has a role in the nutritional regulation of fatty acids and triglycerides in lipogenic organs such as the liver. Required for innate immune response in macrophages by regulating lipid metabolism.; [Isoform SREBP-1C]: Predominant isoform expressed in most tissues, which has weaker transcriptional activity compared to isoform SREBP-1A. Primarily controls expression of lipogenic gene. Strongly activates global lipid synthesis in rapidly growing cells.; [Isoform SREBP-1aDelta]: The absence of Golgi proteolytic processing requirement makes this isoform constitutively active in transactivation of lipogenic gene promoters.; [Isoform SREBP-1cDelta]: The absence of Golgi proteolytic processing requirement makes this isoform constitutively active in transactivation of lipogenic gene promoters.
TTD ID
T47236
Uniprot ID
P36956
DrugMap ID
TTER0UB
Ensemble ID
ENST00000261646.11
HGNC ID
HGNC:11289
ChEMBL ID
CHEMBL4630818

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
GB1 SNV: p.L658V .
LNCaP clone FGC SNV: p.A62V .
MFE319 SNV: p.I370T; p.L507P .
MOLT4 Deletion: p.A143PfsTer21
SNV: p.A541V
.
NUGC3 SNV: p.A669T .
RKO SNV: p.C404R .
SF295 SNV: p.T136P .
SNU5 SNV: p.Y522H .
TOV21G SNV: p.H478Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 10 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
10.42  LDD0402  [1]
STPyne
 Probe Info 
K365(10.00)  LDD0277  [2]
DBIA
 Probe Info 
C962(15.26)  LDD3311  [3]
NAIA_4
 Probe Info 
C945(0.00); C1095(0.00)  LDD2226  [4]
NAIA_5
 Probe Info 
N.A.  LDD2224  [4]
WYneN
 Probe Info 
N.A.  LDD0021  [5]
Compound 10
 Probe Info 
N.A.  LDD2216  [6]
Compound 11
 Probe Info 
N.A.  LDD2213  [6]
IPM
 Probe Info 
N.A.  LDD0005  [5]
TFBX
 Probe Info 
C656(0.00); C932(0.00); C898(0.00)  LDD0148  [7]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Alk-rapa
 Probe Info 
8.80  LDD0213  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C932(1.08)  LDD1507  [9]
 LDCM0215  AC10 HEK-293T C932(0.93)  LDD1508  [9]
 LDCM0226  AC11 HEK-293T C932(0.94)  LDD1509  [9]
 LDCM0237  AC12 HEK-293T C932(1.16)  LDD1510  [9]
 LDCM0259  AC14 HEK-293T C932(0.86)  LDD1512  [9]
 LDCM0270  AC15 HEK-293T C932(1.01); C816(1.34)  LDD1513  [9]
 LDCM0276  AC17 HEK-293T C932(1.05)  LDD1515  [9]
 LDCM0277  AC18 HEK-293T C932(1.02)  LDD1516  [9]
 LDCM0278  AC19 HEK-293T C932(1.00)  LDD1517  [9]
 LDCM0279  AC2 HEK-293T C932(0.93)  LDD1518  [9]
 LDCM0280  AC20 HEK-293T C932(1.06)  LDD1519  [9]
 LDCM0282  AC22 HEK-293T C932(0.97)  LDD1521  [9]
 LDCM0283  AC23 HEK-293T C932(1.00); C816(1.21)  LDD1522  [9]
 LDCM0284  AC24 HEK-293T C932(0.92)  LDD1523  [9]
 LDCM0285  AC25 HEK-293T C932(1.09)  LDD1524  [9]
 LDCM0286  AC26 HEK-293T C932(0.93)  LDD1525  [9]
 LDCM0287  AC27 HEK-293T C932(0.87)  LDD1526  [9]
 LDCM0288  AC28 HEK-293T C932(0.91)  LDD1527  [9]
 LDCM0290  AC3 HEK-293T C932(1.07)  LDD1529  [9]
 LDCM0291  AC30 HEK-293T C932(0.89)  LDD1530  [9]
 LDCM0292  AC31 HEK-293T C932(1.02); C816(1.17)  LDD1531  [9]
 LDCM0293  AC32 HEK-293T C932(0.96)  LDD1532  [9]
 LDCM0294  AC33 HEK-293T C932(1.23)  LDD1533  [9]
 LDCM0295  AC34 HEK-293T C932(1.02)  LDD1534  [9]
 LDCM0296  AC35 HEK-293T C932(0.96)  LDD1535  [9]
 LDCM0297  AC36 HEK-293T C932(1.03)  LDD1536  [9]
 LDCM0299  AC38 HEK-293T C932(0.98)  LDD1538  [9]
 LDCM0300  AC39 HEK-293T C932(1.04); C816(1.20)  LDD1539  [9]
 LDCM0301  AC4 HEK-293T C932(1.02)  LDD1540  [9]
 LDCM0302  AC40 HEK-293T C932(0.88)  LDD1541  [9]
 LDCM0303  AC41 HEK-293T C932(1.17)  LDD1542  [9]
 LDCM0304  AC42 HEK-293T C932(0.98)  LDD1543  [9]
 LDCM0305  AC43 HEK-293T C932(0.98)  LDD1544  [9]
 LDCM0306  AC44 HEK-293T C932(1.05)  LDD1545  [9]
 LDCM0308  AC46 HEK-293T C932(0.87)  LDD1547  [9]
 LDCM0309  AC47 HEK-293T C932(1.05); C816(1.01)  LDD1548  [9]
 LDCM0310  AC48 HEK-293T C932(0.75)  LDD1549  [9]
 LDCM0311  AC49 HEK-293T C932(1.06)  LDD1550  [9]
 LDCM0313  AC50 HEK-293T C932(0.92)  LDD1552  [9]
 LDCM0314  AC51 HEK-293T C932(0.88)  LDD1553  [9]
 LDCM0315  AC52 HEK-293T C932(1.09)  LDD1554  [9]
 LDCM0317  AC54 HEK-293T C932(0.80)  LDD1556  [9]
 LDCM0318  AC55 HEK-293T C932(1.00); C816(1.26)  LDD1557  [9]
 LDCM0319  AC56 HEK-293T C932(0.80)  LDD1558  [9]
 LDCM0320  AC57 HEK-293T C932(1.08)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C932(0.84)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C932(1.25)  LDD1561  [9]
 LDCM0323  AC6 HEK-293T C932(0.91)  LDD1562  [9]
 LDCM0324  AC60 HEK-293T C932(1.13)  LDD1563  [9]
 LDCM0326  AC62 HEK-293T C932(0.86)  LDD1565  [9]
 LDCM0327  AC63 HEK-293T C932(1.02); C816(1.18)  LDD1566  [9]
 LDCM0328  AC64 HEK-293T C932(0.77)  LDD1567  [9]
 LDCM0334  AC7 HEK-293T C932(1.00); C816(1.47)  LDD1568  [9]
 LDCM0345  AC8 HEK-293T C932(0.96)  LDD1569  [9]
 LDCM0356  AKOS034007680 HEK-293T C932(1.10)  LDD1570  [9]
 LDCM0275  AKOS034007705 HEK-293T C932(0.85)  LDD1514  [9]
 LDCM0367  CL1 HEK-293T C932(1.10); C404(1.10)  LDD1571  [9]
 LDCM0368  CL10 HEK-293T C932(1.66)  LDD1572  [9]
 LDCM0369  CL100 HEK-293T C932(0.87)  LDD1573  [9]
 LDCM0370  CL101 HEK-293T C932(1.06); C404(1.13)  LDD1574  [9]
 LDCM0371  CL102 HEK-293T C932(1.24)  LDD1575  [9]
 LDCM0372  CL103 HEK-293T C932(1.06)  LDD1576  [9]
 LDCM0373  CL104 HEK-293T C932(0.90)  LDD1577  [9]
 LDCM0374  CL105 HEK-293T C932(1.06); C404(1.07)  LDD1578  [9]
 LDCM0375  CL106 HEK-293T C932(1.40)  LDD1579  [9]
 LDCM0376  CL107 HEK-293T C932(1.14)  LDD1580  [9]
 LDCM0377  CL108 HEK-293T C932(1.14)  LDD1581  [9]
 LDCM0378  CL109 HEK-293T C932(0.97); C404(1.09)  LDD1582  [9]
 LDCM0379  CL11 HEK-293T C932(1.14); C816(1.02)  LDD1583  [9]
 LDCM0380  CL110 HEK-293T C932(1.32)  LDD1584  [9]
 LDCM0381  CL111 HEK-293T C932(0.96)  LDD1585  [9]
 LDCM0382  CL112 HEK-293T C932(0.93)  LDD1586  [9]
 LDCM0383  CL113 HEK-293T C932(1.04); C404(1.23)  LDD1587  [9]
 LDCM0384  CL114 HEK-293T C932(1.44)  LDD1588  [9]
 LDCM0385  CL115 HEK-293T C932(1.10)  LDD1589  [9]
 LDCM0386  CL116 HEK-293T C932(0.94)  LDD1590  [9]
 LDCM0387  CL117 HEK-293T C932(1.12); C404(1.14)  LDD1591  [9]
 LDCM0388  CL118 HEK-293T C932(1.36)  LDD1592  [9]
 LDCM0389  CL119 HEK-293T C932(1.03)  LDD1593  [9]
 LDCM0390  CL12 HEK-293T C932(0.94)  LDD1594  [9]
 LDCM0391  CL120 HEK-293T C932(0.95)  LDD1595  [9]
 LDCM0392  CL121 HEK-293T C932(1.06); C404(1.15)  LDD1596  [9]
 LDCM0393  CL122 HEK-293T C932(1.01)  LDD1597  [9]
 LDCM0394  CL123 HEK-293T C932(1.20)  LDD1598  [9]
 LDCM0395  CL124 HEK-293T C932(0.78)  LDD1599  [9]
 LDCM0396  CL125 HEK-293T C932(1.14); C404(1.20)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C932(1.21)  LDD1601  [9]
 LDCM0398  CL127 HEK-293T C932(0.98)  LDD1602  [9]
 LDCM0399  CL128 HEK-293T C932(0.93)  LDD1603  [9]
 LDCM0400  CL13 HEK-293T C932(1.15); C404(1.13)  LDD1604  [9]
 LDCM0401  CL14 HEK-293T C932(1.07)  LDD1605  [9]
 LDCM0402  CL15 HEK-293T C932(1.30)  LDD1606  [9]
 LDCM0403  CL16 HEK-293T C932(1.02)  LDD1607  [9]
 LDCM0404  CL17 HEK-293T C932(1.33)  LDD1608  [9]
 LDCM0405  CL18 HEK-293T C932(1.17)  LDD1609  [9]
 LDCM0406  CL19 HEK-293T C932(1.00)  LDD1610  [9]
 LDCM0407  CL2 HEK-293T C932(1.28)  LDD1611  [9]
 LDCM0408  CL20 HEK-293T C932(1.32)  LDD1612  [9]
 LDCM0410  CL22 HEK-293T C932(1.14)  LDD1614  [9]
 LDCM0411  CL23 HEK-293T C932(1.07); C816(0.87)  LDD1615  [9]
 LDCM0412  CL24 HEK-293T C932(0.98)  LDD1616  [9]
 LDCM0413  CL25 HEK-293T C932(1.26); C404(1.13)  LDD1617  [9]
 LDCM0414  CL26 HEK-293T C932(1.54)  LDD1618  [9]
 LDCM0415  CL27 HEK-293T C932(1.06)  LDD1619  [9]
 LDCM0416  CL28 HEK-293T C932(0.87)  LDD1620  [9]
 LDCM0417  CL29 HEK-293T C932(1.07)  LDD1621  [9]
 LDCM0418  CL3 HEK-293T C932(1.12)  LDD1622  [9]
 LDCM0419  CL30 HEK-293T C932(1.02)  LDD1623  [9]
 LDCM0420  CL31 HEK-293T C932(0.95)  LDD1624  [9]
 LDCM0421  CL32 HEK-293T C932(1.15)  LDD1625  [9]
 LDCM0423  CL34 HEK-293T C932(1.11)  LDD1627  [9]
 LDCM0424  CL35 HEK-293T C932(1.15); C816(0.83)  LDD1628  [9]
 LDCM0425  CL36 HEK-293T C932(1.00)  LDD1629  [9]
 LDCM0426  CL37 HEK-293T C932(0.97); C404(1.14)  LDD1630  [9]
 LDCM0428  CL39 HEK-293T C932(1.13)  LDD1632  [9]
 LDCM0429  CL4 HEK-293T C932(0.92)  LDD1633  [9]
 LDCM0430  CL40 HEK-293T C932(1.00)  LDD1634  [9]
 LDCM0431  CL41 HEK-293T C932(1.17)  LDD1635  [9]
 LDCM0432  CL42 HEK-293T C932(1.12)  LDD1636  [9]
 LDCM0433  CL43 HEK-293T C932(0.83)  LDD1637  [9]
 LDCM0434  CL44 HEK-293T C932(1.12)  LDD1638  [9]
 LDCM0436  CL46 HEK-293T C932(1.11)  LDD1640  [9]
 LDCM0437  CL47 HEK-293T C932(1.20); C816(1.05)  LDD1641  [9]
 LDCM0438  CL48 HEK-293T C932(1.02)  LDD1642  [9]
 LDCM0439  CL49 HEK-293T C932(1.12); C404(1.11)  LDD1643  [9]
 LDCM0440  CL5 HEK-293T C932(1.11)  LDD1644  [9]
 LDCM0441  CL50 HEK-293T C932(1.22)  LDD1645  [9]
 LDCM0443  CL52 HEK-293T C932(0.98)  LDD1646  [9]
 LDCM0444  CL53 HEK-293T C932(1.39)  LDD1647  [9]
 LDCM0445  CL54 HEK-293T C932(1.20)  LDD1648  [9]
 LDCM0446  CL55 HEK-293T C932(1.01)  LDD1649  [9]
 LDCM0447  CL56 HEK-293T C932(1.18)  LDD1650  [9]
 LDCM0449  CL58 HEK-293T C932(1.03)  LDD1652  [9]
 LDCM0450  CL59 HEK-293T C932(1.14); C816(1.23)  LDD1653  [9]
 LDCM0451  CL6 HEK-293T C932(1.25)  LDD1654  [9]
 LDCM0452  CL60 HEK-293T C932(1.24)  LDD1655  [9]
 LDCM0453  CL61 HEK-293T C932(1.01); C404(0.99)  LDD1656  [9]
 LDCM0454  CL62 HEK-293T C932(1.32)  LDD1657  [9]
 LDCM0455  CL63 HEK-293T C932(0.94)  LDD1658  [9]
 LDCM0456  CL64 HEK-293T C932(1.02)  LDD1659  [9]
 LDCM0457  CL65 HEK-293T C932(1.05)  LDD1660  [9]
 LDCM0458  CL66 HEK-293T C932(0.85)  LDD1661  [9]
 LDCM0459  CL67 HEK-293T C932(1.10)  LDD1662  [9]
 LDCM0460  CL68 HEK-293T C932(1.28)  LDD1663  [9]
 LDCM0462  CL7 HEK-293T C932(1.22)  LDD1665  [9]
 LDCM0463  CL70 HEK-293T C932(1.00)  LDD1666  [9]
 LDCM0464  CL71 HEK-293T C932(1.18); C816(0.79)  LDD1667  [9]
 LDCM0465  CL72 HEK-293T C932(1.14)  LDD1668  [9]
 LDCM0466  CL73 HEK-293T C932(1.19); C404(1.18)  LDD1669  [9]
 LDCM0467  CL74 HEK-293T C932(1.21)  LDD1670  [9]
 LDCM0469  CL76 HEK-293T C932(0.87)  LDD1672  [9]
 LDCM0470  CL77 HEK-293T C932(1.21)  LDD1673  [9]
 LDCM0471  CL78 HEK-293T C932(0.95)  LDD1674  [9]
 LDCM0472  CL79 HEK-293T C932(1.08)  LDD1675  [9]
 LDCM0473  CL8 HEK-293T C932(1.54)  LDD1676  [9]
 LDCM0474  CL80 HEK-293T C932(1.14)  LDD1677  [9]
 LDCM0476  CL82 HEK-293T C932(1.09)  LDD1679  [9]
 LDCM0477  CL83 HEK-293T C932(1.17); C816(1.51)  LDD1680  [9]
 LDCM0478  CL84 HEK-293T C932(1.23)  LDD1681  [9]
 LDCM0479  CL85 HEK-293T C932(1.12); C404(1.13)  LDD1682  [9]
 LDCM0480  CL86 HEK-293T C932(1.38)  LDD1683  [9]
 LDCM0481  CL87 HEK-293T C932(1.15)  LDD1684  [9]
 LDCM0482  CL88 HEK-293T C932(0.84)  LDD1685  [9]
 LDCM0483  CL89 HEK-293T C932(1.17)  LDD1686  [9]
 LDCM0485  CL90 HEK-293T C932(1.36)  LDD1688  [9]
 LDCM0486  CL91 HEK-293T C932(1.12)  LDD1689  [9]
 LDCM0487  CL92 HEK-293T C932(1.24)  LDD1690  [9]
 LDCM0489  CL94 HEK-293T C932(1.01)  LDD1692  [9]
 LDCM0490  CL95 HEK-293T C932(1.48); C816(1.15)  LDD1693  [9]
 LDCM0491  CL96 HEK-293T C932(0.92)  LDD1694  [9]
 LDCM0492  CL97 HEK-293T C932(0.93); C404(1.06)  LDD1695  [9]
 LDCM0493  CL98 HEK-293T C932(1.09)  LDD1696  [9]
 LDCM0494  CL99 HEK-293T C932(1.01)  LDD1697  [9]
 LDCM0495  E2913 HEK-293T C932(1.00)  LDD1698  [9]
 LDCM0468  Fragment33 HEK-293T C932(1.16)  LDD1671  [9]
 LDCM0427  Fragment51 HEK-293T C932(1.15)  LDD1631  [9]
 LDCM0022  KB02 A2058 C686(3.44); C928(3.88)  LDD2253  [3]
 LDCM0023  KB03 MDA-MB-231 C656(1.00)  LDD1701  [10]
 LDCM0024  KB05 G361 C962(15.26)  LDD3311  [3]
 LDCM0090  Rapamycin JHH-7 8.80  LDD0213  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) Sirtuin family Q96EB6
CREB-binding protein (CREBBP) . Q92793
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ataxin-1 (ATXN1) ATXN1 family P54253
Mediator of RNA polymerase II transcription subunit 15 (MED15) Mediator complex subunit 15 family Q96RN5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Doconexent Small molecular drug DB03756
Fish Oil . DB13961
Omega-3 Fatty Acids . DB11133
Omega-3-acid Ethyl Esters . DB09539

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 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
4 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
5 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
6 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
7 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
8 Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth. Cell Chem Biol. 2022 Mar 17;29(3):373-385.e6. doi: 10.1016/j.chembiol.2021.10.006. Epub 2021 Oct 26.
9 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
10 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