Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T17485
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| Target Name |
Menin-MLL1 interaction (MEN1-KMT2A PPI)
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| Gene Name |
MEN1-KMT2A
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Acute myeloid leukaemia [ICD-11: 2A60] | |||||
| 2 | Malignant haematopoietic neoplasm [ICD-11: 2B33] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | KO-539 | Drug Info | Phase 1/2 | Acute myeloid leukaemia | [2] | |
| 2 | SNDX-5613 | Drug Info | Phase 1/2 | T lymphoblastic leukaemia | [3] | |
| 3 | JNJ-75276617 | Drug Info | Phase 1 | Haematological malignancy | [4] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Inhibitor | [+] 3 Inhibitor drugs | + | ||||
| 1 | KO-539 | Drug Info | [1] | |||
| 2 | SNDX-5613 | Drug Info | [5] | |||
| 3 | JNJ-75276617 | Drug Info | [6] | |||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Cholic acid | Ligand Info | |||||
| Structure Description | Crystal structure of human menin in complex with MLL1 and LEDGF | PDB:3U88 | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [7] |
| PDB Sequence |
GLKAAQKTLF
11 PLRSIDDVVR21 LFAAELGREE31 PDLVLLSLVL41 GFVEHFLAVN51 RVIPTNVPEL 61 TFQPSPAPDG73 GLTYFPVADL83 SIIAALYARF93 TAQIRGAVDL103 SLYPREGGVS 113 SRELVKKVSD123 VIWNSLSRSY133 FKDRAHIQSL143 FSFITGTKLD153 SSGVAFAVVG 163 ACQALGLRDV173 HLALSEDHAW183 VVFGPNGEQT193 AEVTWHGKGN203 EDRRGQTVNA 213 GVAERSWLYL223 KGSYMRCDRK233 MEVAFMVCAI243 NPSIDLHTDS253 LELLQLQQKL 263 LWLLYDLGHL273 ERYPMALGNL283 ADLEELEPTP293 GRPDPLTLYH303 KGIASAKTYY 313 RDEHIYPYMY323 LAGYHCRNRN333 VREALQAWAD343 TATVIQDYNY353 CREDEEIYKE 363 FFEVANDVIP373 NLLKEAASLL383 EASALQDPEC409 FAHLLRFYDG419 ICKWEEGSPT 429 PVLHVGWATF439 LVQSLGRFEG449 QVRQKVRIVS459 EGPVLTFQSE556 KMKGMKELLV 566 ATKINSSAIK576 LQLTAQS
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| Ligand Name: Glyoxalate, Glyoxylate | Ligand Info | |||||
| Structure Description | Crystal structure of human menin in complex with MLL1 and LEDGF | PDB:3U88 | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [7] |
| PDB Sequence |
GLKAAQKTLF
11 PLRSIDDVVR21 LFAAELGREE31 PDLVLLSLVL41 GFVEHFLAVN51 RVIPTNVPEL 61 TFQPSPAPDG73 GLTYFPVADL83 SIIAALYARF93 TAQIRGAVDL103 SLYPREGGVS 113 SRELVKKVSD123 VIWNSLSRSY133 FKDRAHIQSL143 FSFITGTKLD153 SSGVAFAVVG 163 ACQALGLRDV173 HLALSEDHAW183 VVFGPNGEQT193 AEVTWHGKGN203 EDRRGQTVNA 213 GVAERSWLYL223 KGSYMRCDRK233 MEVAFMVCAI243 NPSIDLHTDS253 LELLQLQQKL 263 LWLLYDLGHL273 ERYPMALGNL283 ADLEELEPTP293 GRPDPLTLYH303 KGIASAKTYY 313 RDEHIYPYMY323 LAGYHCRNRN333 VREALQAWAD343 TATVIQDYNY353 CREDEEIYKE 363 FFEVANDVIP373 NLLKEAASLL383 EASALQDPEC409 FAHLLRFYDG419 ICKWEEGSPT 429 PVLHVGWATF439 LVQSLGRFEG449 QVRQKVRIVS459 EGPVLTFQSE556 KMKGMKELLV 566 ATKINSSAIK576 LQLTAQS
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LYS135
3.106
ASP136
3.551
ASP153
3.796
SER154
3.380
HIS181
4.478
GLU195
3.251
THR197
2.715
TRP198
3.208
HIS199
3.803
GLY200
3.158
LYS201
4.532
GLU204
4.444
ASP205
3.806
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of Kura Oncology. | |||||
| REF 2 | ClinicalTrials.gov (NCT04067336) First in Human Study of KO-539 in Relapsed or Refractory Acute Myeloid Leukemia. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT04065399) A Study of SNDX-5613 in R/R Leukemias Including Those With an MLLr/KMT2A Gene Rearrangement or NPM1 Mutation (AUGMENT-101). U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT04811560) A First in Human Study of the Menin-KMT2A (MLL1) Inhibitor JNJ-75276617 in Participants With Acute Leukemia. U.S.National Institutes of Health. | |||||
| REF 5 | Clinical pipeline report, company report or official report of Syndax Pharmaceuticals. | |||||
| REF 6 | Targeting the undruggable: menin inhibitors ante portas. J Cancer Res Clin Oncol. 2023 Sep;149(11):9451-9459. | |||||
| REF 7 | The same pocket in menin binds both MLL and JUND but has opposite effects on transcription. Nature. 2012 Feb 12;482(7386):542-6. | |||||
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