Property Summary

NCBI Gene PubMed Count 63
Grant Count 164
R01 Count 96
Funding $42,674,183.06
PubMed Score 250.66
PubTator Score 99.00

Knowledge Summary

Patent

No data available

Expression

Synonym

Accession O96028 A2A2T2 A2A2T3 A2A2T4 A7MCZ1 D3DVQ2 O96031 Q4VBY8 Q672J1 Q6IS00 Q86V01 Q9BZB4 Q9UI92 Q9UPR2
Symbols WHS
TRX5
KMT3F
KMT3G
MMSET
WHSC1
REIIBP

Gene

MLP Assay (3)

AID Type Active / Inconclusive / Inactive Description
743445 screening 1662 / 0 / 308170 Development of Small Molecule Probes of the Histone Methyltransferase, NSD2 Measured in Biochemical System Using Plate Reader - 7053-01_Inhibitor_SinglePoint_HTS_Activity_Set2
743459 summary 0 / 0 / 0 Broad Institute Development of Small Molecule Probes of the Histone Methyltransferase, NSD2 Inhibitor Probe Project
1053173 confirmatory 390 / 3 / 1110 Development of Small Molecule Probes of the Histone Methyltransferase, NSD2 Measured in Biochemical System Using Plate Reader - 7053-01_Inhibitor_Dose_CherryPick_Activity

Gene RIF (42)

PMID Text
26912663 results identify a pivotal role for NSD2 binding to its catalytic product in regulating its cellular functions, and suggest a model for how this interaction may facilitate epigenetic spreading and propagation of H3K36me2.
26787850 NSD2 preferentially catalyzes the dimethylation of H3K36 along with a reduced preference for H3K36 monomethylation
26771714 In MMSET-depleted cells there are defects in DNA replication and a decreased association with chromatin.
26206755 It was observed that RE-IIBP induces MEIS1-mediated apoptosis, which was dependent on H2BK120 ubiquitination by RNF20.
25942451 Studies indicate that the NSD methyltransferases NSD1, NSD2/WHSC1/MMSET and NSD3/WHSC1L1 were overexpressed, amplified or somatically mutated in multiple types of cancer, suggesting their critical role in cancer.
25494638 The results describe the binding of NSD1, 2 and 3 catalytic domains (CD) on histone tails through recognition of histone-lysine and methylation properties.
25280969 Results show that WHSC1 is overexpressed in Squamous cell carcinoma of the head and neck (SCCHN) and that it promotes cell-cycle progression through activation of NEK7, indicating its potential role as an oncogenic force in SCCHN.
24923560 The role of the shorter isoform (REIIBP) in myeloma cells was characterized and identified a clear and novel interaction of REIIBP with members of the SMN complex.
24809779 Gastric cancer patients with high MMSET and BRCA1 attain a longer median survival compared with those with high BRCA1 and low MMSET.
24019522 all of the H3K36-specific methyltransferases, including ASH1L, HYPB, NSD1, and NSD2 were inhibited by ubH2A, whereas the other histone methyltransferases, including PRC2, G9a, and Pr-Set7 were not affected by ubH2A.
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AA Sequence

MEFSIKQSPLSVQSVVKCIKMKQAPEILGSANGKTPSCEVNRECSVFLSKAQLSSSLQEGVMQKFNGHDA      1 - 70
LPFIPADKLKDLTSRVFNGEPGAHDAKLRFESQEMKGIGTPPNTTPIKNGSPEIKLKITKTYMNGKPLFE     71 - 140
SSICGDSAADVSQSEENGQKPENKARRNRKRSIKYDSLLEQGLVEAALVSKISSPSDKKIPAKKESCPNT    141 - 210
GRDKDHLLKYNVGDLVWSKVSGYPWWPCMVSADPLLHSYTKLKGQKKSARQYHVQFFGDAPERAWIFEKS    211 - 280
LVAFEGEGQFEKLCQESAKQAPTKAEKIKLLKPISGKLRAQWEMGIVQAEEAASMSVEERKAKFTFLYVG    281 - 350
DQLHLNPQVAKEAGIAAESLGEMAESSGVSEEAAENPKSVREECIPMKRRRRAKLCSSAETLESHPDIGK    351 - 420
STPQKTAEADPRRGVGSPPGRKKTTVSMPRSRKGDAASQFLVFCQKHRDEVVAEHPDASGEEIEELLRSQ    421 - 490
WSLLSEKQRARYNTKFALVAPVQAEEDSGNVNGKKRNHTKRIQDPTEDAEAEDTPRKRLRTDKHSLRKRD    491 - 560
TITDKTARTSSYKAMEAASSLKSQAATKNLSDACKPLKKRNRASTAASSALGFSKSSSPSASLTENEVSD    561 - 630
SPGDEPSESPYESADETQTEVSVSSKKSERGVTAKKEYVCQLCEKPGSLLLCEGPCCGAFHLACLGLSRR    631 - 700
PEGRFTCSECASGIHSCFVCKESKTDVKRCVVTQCGKFYHEACVKKYPLTVFESRGFRCPLHSCVSCHAS    701 - 770
NPSNPRPSKGKMMRCVRCPVAYHSGDACLAAGCSVIASNSIICTAHFTARKGKRHHAHVNVSWCFVCSKG    771 - 840
GSLLCCESCPAAFHPDCLNIEMPDGSWFCNDCRAGKKLHFQDIIWVKLGNYRWWPAEVCHPKNVPPNIQK    841 - 910
MKHEIGEFPVFFFGSKDYYWTHQARVFPYMEGDRGSRYQGVRGIGRVFKNALQEAEARFREIKLQREARE    911 - 980
TQESERKPPPYKHIKVNKPYGKVQIYTADISEIPKCNCKPTDENPCGFDSECLNRMLMFECHPQVCPAGE    981 - 1050
FCQNQCFTKRQYPETKIIKTDGKGWGLVAKRDIRKGEFVNEYVGELIDEEECMARIKHAHENDITHFYML   1051 - 1120
TIDKDRIIDAGPKGNYSRFMNHSCQPNCETLKWTVNGDTRVGLFAVCDIPAGTELTFNYNLDCLGNEKTV   1121 - 1190
CRCGASNCSGFLGDRPKTSTTLSSEEKGKKTKKKTRRRRAKGEGKRQSEDECFRCGDGGQLVLCDRKFCT   1191 - 1260
KAYHLSCLGLGKRPFGKWECPWHHCDVCGKPSTSFCHLCPNSFCKEHQDGTAFSCTPDGRSYCCEHDLGA   1261 - 1330
ASVRSTKTEKPPPEPGKPKGKRRRRRGWRRVTEGK                                      1331 - 1365
//

Text Mined References (70)

PMID Year Title
26912663 2016 A PWWP Domain of Histone-Lysine N-Methyltransferase NSD2 Binds to Dimethylated Lys-36 of Histone H3 and Regulates NSD2 Function at Chromatin.
26787850 2016 Transition state for the NSD2-catalyzed methylation of histone H3 lysine 36.
26771714 2016 MMSET is dynamically regulated during cell-cycle progression and promotes normal DNA replication.
26206755 2015 RE-IIBP Methylates H3K79 and Induces MEIS1-mediated Apoptosis via H2BK120 Ubiquitination by RNF20.
25942451 2015 The NSD family of protein methyltransferases in human cancer.
25494638 2014 In vitro histone lysine methylation by NSD1, NSD2/MMSET/WHSC1 and NSD3/WHSC1L.
25280969 2015 WHSC1 promotes oncogenesis through regulation of NIMA-related kinase-7 in squamous cell carcinoma of the head and neck.
24923560 2014 A novel functional role for MMSET in RNA processing based on the link between the REIIBP isoform and its interaction with the SMN complex.
24809779 2014 Differential effect of MMSET mRNA levels on survival to first-line FOLFOX and second-line docetaxel in gastric cancer.
24129315 2014 Immunoaffinity enrichment and mass spectrometry analysis of protein methylation.
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