| Id: | acc0919 |
| Group: | 2sens |
| Protein: | SAMHD1 |
| Gene Symbol: | SAMHD1 |
| Protein Id: | Q9Y3Z3 |
| Protein Name: | SAMH1_HUMAN |
| PTM: | phosphorylation |
| Site: | Thr592 |
| Site Sequence: | DGDVIAPLITPQKKEWNDSTS |
| Disease Category: | Cancer |
| Disease: | Leukemia |
| Disease Subtype: | CML |
| Disease Cellline: | CD4+ T |
| Disease Info: | |
| Drug: | dasatinib |
| Drug Info: | "Dasatinib is a tyrosine kinase inhibitor that targets BCR-ABL and SRC family kinases, used in the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), particularly in patients resistant or intolerant to prior therapy including imatinib." |
| Effect: | modulate |
| Effect Info: | "Tyrosine kinase inhibitors (TKIs), such as dasatinib, inhibit the phosphorylation of SAMHD1, rendering the CD4+ T cells of patients with chronic myeloid leukemia (CML) resistant to in vitro HIV - 1 infection." |
| Note: | no tumor effct |
| Score: | 3.0 |
| Pubmed(PMID): | 32828803 |
| Sentence Index: | 32828803_2-3 |
| Sentence: | "Our group previously described that CD4+ T cells from patients with CML on treatment with TKIs such as dasatinib were resistant to HIV-1 infection ex vivo. The main mechanism for this antiviral activity was primarily based on the inhibition of SAMHD1 phosphorylation, which preserves the activity against HIV-1 of this innate immune factor." |
Sequence & Structure:
MQRADSEQPSKRPRCDDSPRTPSNTPSAEADWSPGLELHPDYKTWGPEQVCSFLRRGGFEEPVLLKNIRENEITGALLPCLDESRFENLGVSSLGERKKLLSYIQRLVQIHVDTMKVINDPIHGHIELHPLLVRIIDTPQFQRLRYIKQLGGGYYVFPGASHNRFEHSLGVGYLAGCLVHALGEKQPELQISERDVLCVQIAGLCHDLGHGPFSHMFDGRFIPLARPEVKWTHEQGSVMMFEHLINSNGIKPVMEQYGLIPEEDICFIKEQIVGPLESPVEDSLWPYKGRPENKSFLYEIVSNKRNGIDVDKWDYFARDCHHLGIQNNFDYKRFIKFARVCEVDNELRICARDKEVGNLYDMFHTRNSLHRRAYQHKVGNIIDTMITDAFLKADDYIEITGAGGKKYRISTAIDDMEAYTKLTDNIFLEILYSTDPKLKDAREILKQIEYRNLFKYVGETQPTGQIKIKREDYESLPKEVASAKPKVLLDVKLKAEDFIVDVINMDYGMQEKNPIDHVSFYCKTAPNRAIRITKNQVSQLLPEKFAEQLIRVYCKKVDRKSLYAARQYFVQWCADRNFTKPQDGDVIAPLITPQKKEWNDSTSVQNPTRLREASKSRVQLFKDDPM
Select PDB:
No data.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTAC| SAMHD1-Thr592 | |
|---|---|
| Cancer | Intensity |
| BRCA | -0.956 |
| COAD | -0.082 |
| HGSC | 1.039 |
| ccRCC | |
| GBM | |
| HNSC | |
| LUAD | |
| LUSC | |
| non_ccRCC | |
| PDAC | |
| UCEC | |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptM| Protein | Gene | PTM | Position | Modified sequence | Cell | Drug | pEC50 | Regulation | Experiment |
|---|---|---|---|---|---|---|---|---|---|
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.2846 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.2694 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | -1.3208 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | -1.4395 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.6006 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | 1.6516 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.3174 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | -0.484 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.46 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | -0.4851 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQK | SU-DHL-4 | Rituximab | -1.4421 | - | |
| Q9Y3Z3 | SAMHD1 | P | Thr592 | NFTKPQDGDVIAPLIT(ph)PQKK | SU-DHL-4 | Rituximab | -1.1432 | - |
pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.
Function score:
source: funscoRNo data.
