Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTYRXD2T)

• DOT Name: Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1)
• Synonyms: EC 2.7.11.1; Myt1 kinase
• Gene Name: PKMYT1
• UniProt ID: PMYT1_HUMAN
• PDB ID: 3P1A; 5VCV; 5VCW; 5VCX; 5VCY; 5VCZ; 5VD0; 5VD1; 5VD3; 8D6C; 8D6D; 8D6E; 8D6F; 8WJY
• EC Number: 2.7.11.1
• Pfam ID: PF00069
• Sequence:
  MLERPPALAMPMPTEGTPPPLSGTPIPVPAYFRHAEPGFSLKRPRGLSRSLPPPPPAKGS
  IPISRLFPPRTPGWHQLQPRRVSFRGEASETLQSPGYDPSRPESFFQQSFQRLSRLGHGS
  YGEVFKVRSKEDGRLYAVKRSMSPFRGPKDRARKLAEVGSHEKVGQHPCCVRLEQAWEEG
  GILYLQTELCGPSLQQHCEAWGASLPEAQVWGYLRDTLLALAHLHSQGLVHLDVKPANIF
  LGPRGRCKLGDFGLLVELGTAGAGEVQEGDPRYMAPELLQGSYGTAADVFSLGLTILEVA
  CNMELPHGGEGWQQLRQGYLPPEFTAGLSSELRSVLVMMLEPDPKLRATAEALLALPVLR
  QPRAWGVLWCMAAEALSRGWALWQALLALLCWLWHGLAHPASWLQPLGPPATPPGSPPCS
  LLLDSSLSSNWDDDSLGPSLSPEAVLARTVGSTSTPRSRCTPRDALDLSDINSEPPRGSF
  PSFEPRNLLSLFEDTLDPT
• Function: Acts as a negative regulator of entry into mitosis (G2 to M transition) by phosphorylation of the CDK1 kinase specifically when CDK1 is complexed to cyclins. Mediates phosphorylation of CDK1 predominantly on 'Thr-14'. Also involved in Golgi fragmentation. May be involved in phosphorylation of CDK1 on 'Tyr-15' to a lesser degree, however tyrosine kinase activity is unclear and may be indirect.
• KEGG Pathway:
  Cell cycle (hsa04110)
  Oocyte meiosis (hsa04114)
  Progesterone-mediated oocyte maturation (hsa04914)
• Reactome Pathway:
  Cyclin A/B1/B2 associated events during G2/M transition (R-HSA-69273)
  G2/M DNA replication checkpoint (R-HSA-69478)
  Polo-like kinase mediated events (R-HSA-156711)

Molecular Interaction Atlas (MIA) of This DOT

2 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the methylation of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[1]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 increases the phosphorylation of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[18]

24 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[2]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[3]
Cupric Sulfate	DMP0NFQ	Approved	Cupric Sulfate affects the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[4]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[5]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[6]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[7]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[8]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[8]
Triclosan	DMZUR4N	Approved	Triclosan decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[9]
Cannabidiol	DM0659E	Approved	Cannabidiol decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[10]
Troglitazone	DM3VFPD	Approved	Troglitazone decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[11]
Dasatinib	DMJV2EK	Approved	Dasatinib decreases the activity of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[12]
Simvastatin	DM30SGU	Approved	Simvastatin decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[13]
GSK2110183	DMZHB37	Phase 2	GSK2110183 decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[14]
Saracatinib	DMBLHGP	Phase 2	Saracatinib decreases the activity of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[12]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[15]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[16]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[17]
THAPSIGARGIN	DMDMQIE	Preclinical	THAPSIGARGIN decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[19]
PD166285	DMAOHXY	Terminated	PD166285 decreases the activity of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[12]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[20]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[21]
geraniol	DMS3CBD	Investigative	geraniol decreases the expression of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[22]
PD-0173952	DMSCQ9U	Investigative	PD-0173952 decreases the activity of Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1).	[12]

References

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