Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTSFWA7)

• DTT Name: Plasmodium CDK Pfmrk (Malaria Pfmrk)
• Synonyms: Pfmrk; MO15-related protein kinase Pfmrk
• Gene Name: Malaria Pfmrk
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Kinase
• UniProt ID: P90584_PLAFA
• TTD ID: T04820
• EC Number: EC 2.7.1.37
• Sequence:
  MENNSTERYIFKPNFLGEGSYGKVYKAYDTILKKEVAIKKMKLNEISNYIDDCGINFVLL
  REIKIMKEIKHKNIMSALDLYCEKDYINLVMEIMDYDLSKIINRKIFLTDSQKKCILLQI
  LNGLNVLHKYYFMHRDLSPANIFINKKGEVKLADFGLCTKYGYDMYSDKLFRDKYKKNLN
  LTSKVVTLWYRAPELLLGSNKYNSSIDMWSFGCIFAELLLQKALFPGENEIDQLGKIFFL
  LGTPNENNWPEALCLPLYTEFTKATKKDFKTYFKIDDDDCIDLLTSFLKLNAHERISAED
  AMKHRYFFNDPLPCDISQLPFNDL
• Function: Association of Pfmrk with human cyclin H (the cyclin partner for hCDK7) or Pfcyc-1 (a cyclin homologue in P. falciparum) stimulates kinase activity in vitro.

Molecular Interaction Atlas (MIA) of This DTT

1 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
KENPAULLONE	DMAGVXW	Discovery agent	N.A.	Patented	[1]

20 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(E)-1-(4-Nitro-phenyl)-3-pyridin-2-yl-propenone	DMEP903	Discovery agent	N.A.	Investigative	[1]
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide	DMU5J8Y	Discovery agent	N.A.	Investigative	[2]
2,5-dichloro-N-phenylthiophene-3-sulfonamide	DM9PK1R	Discovery agent	N.A.	Investigative	[2]
2-chloro-N-(o-tolylcarbamoyl)benzamide	DMLDQ6I	Discovery agent	N.A.	Investigative	[2]
3-[3-(2-Hydroxy-ethoxy)-phenyl]-1H-quinolin-2-one	DMLX9SI	Discovery agent	N.A.	Investigative	[1]
5-chloro-4-nitrothiophene-2-sulfonamide	DMRS82Q	Discovery agent	N.A.	Investigative	[2]
5-Nitro-1H-indole-2,3-dione	DMTS06Z	Discovery agent	N.A.	Investigative	[1]
APIGENIN	DMI3491	Discovery agent	N.A.	Investigative	[1]
N'-(2-fluorobenzoyl)-2-naphthohydrazide	DM7BKUQ	Discovery agent	N.A.	Investigative	[2]
N-(2-aminoethyl)isoquinoline-5-sulfonamide	DMG2MSX	Discovery agent	N.A.	Investigative	[3]
Oxindole derivative	DM1AU8V	Malaria	1F40-1F45	Investigative	[4]
Thiophene sulfonamide	DMAKW2S	Malaria	1F40-1F45	Investigative	[5]
WR-080539	DMUCGK8	Discovery agent	N.A.	Investigative	[6]
WR-089120	DMT9WPJ	Discovery agent	N.A.	Investigative	[6]
WR-190706	DM3TI6L	Discovery agent	N.A.	Investigative	[6]
WR-203581	DM9M1UO	Discovery agent	N.A.	Investigative	[6]
WR-289009	DM5W9GR	Discovery agent	N.A.	Investigative	[6]
WR-289010	DMS2QUL	Discovery agent	N.A.	Investigative	[6]
WR-289012	DMG2LVM	Discovery agent	N.A.	Investigative	[6]
WR-289016	DMT08ZH	Discovery agent	N.A.	Investigative	[6]

References

• [1] A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different class... J Med Chem. 2004 Oct 21;47(22):5418-26.
• [2] Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases, Bioorg. Med. Chem. Lett. 20(13):3863-3867 (2010).
• [3] Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4961-6.
• [4] Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10.
• [5] Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97.
• [6] Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5.