Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT9P6OW)

• DTT Name: G2/mitotic-specific cyclin B1 (CCNB1)
• Synonyms: G2/mitotic-specific cyclin-B1; Cyclin B1; CCNB
• Gene Name: CCNB1
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Eukaryotic nuclear pore complex
• UniProt ID: CCNB1_HUMAN
• TTD ID: T98459
• Sequence:
  MALRVTRNSKINAENKAKINMAGAKRVPTAPAATSKPGLRPRTALGDIGNKVSEQLQAKM
  PMKKEAKPSATGKVIDKKLPKPLEKVPMLVPVPVSEPVPEPEPEPEPEPVKEEKLSPEPI
  LVDTASPSPMETSGCAPAEEDLCQAFSDVILAVNDVDAEDGADPNLCSEYVKDIYAYLRQ
  LEEEQAVRPKYLLGREVTGNMRAILIDWLVQVQMKFRLLQETMYMTVSIIDRFMQNNCVP
  KKMLQLVGVTAMFIASKYEEMYPPEIGDFAFVTDNTYTKHQIRQMEMKILRALNFGLGRP
  LPLHFLRRASKIGEVDVEQHTLAKYLMELTMLDYDMVHFPPSQIAAGAFCLALKILDNGE
  WTPTLQHYLSYTEESLLPVMQHLAKNVVMVNQGLTKHMTVKNKYATSKHAKISTLPQLNS
  ALVQDLAKAVAKV
• Function: Essential for the control of the cell cycle at the G2/M (mitosis) transition.
• KEGG Pathway:
  FoxO signaling pathway (hsa04068)
  Cell cycle (hsa04110)
  Oocyte meiosis (hsa04114)
  p53 signaling pathway (hsa04115)
  Progesterone-mediated oocyte maturation (hsa04914)
• Reactome Pathway:
  Golgi Cisternae Pericentriolar Stack Reorganization (R-HSA-162658)
  Regulation of APC/C activators between G1/S and early anaphase (R-HSA-176408)
  Phosphorylation of the APC/C (R-HSA-176412)
  Phosphorylation of Emi1 (R-HSA-176417)
  Condensation of Prophase Chromosomes (R-HSA-2299718)
  MASTL Facilitates Mitotic Progression (R-HSA-2465910)
  Resolution of Sister Chromatid Cohesion (R-HSA-2500257)
  Condensation of Prometaphase Chromosomes (R-HSA-2514853)
  Regulation of PLK1 Activity at G2/M Transition (R-HSA-2565942)
  Activation of NIMA Kinases NEK9, NEK6, NEK7 (R-HSA-2980767)
  Recruitment of NuMA to mitotic centrosomes (R-HSA-380320)
  Depolymerisation of the Nuclear Lamina (R-HSA-4419969)
  Cyclin A/B1 associated events during G2/M transition (R-HSA-69273)
  G2/M DNA replication checkpoint (R-HSA-69478)
  Chk1/Chk2(Cds1) mediated inactivation of Cyclin B (R-HSA-75035)
  Polo-like kinase mediated events (R-HSA-156711)

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]

11 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3,4-bis(indol-3-yl)maleimide derivative	DMEQ1HC	Discovery agent	N.A.	Investigative	[2]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	DMDO175	Discovery agent	N.A.	Investigative	[3]
3,4-diphenyl-1H-pyrrole-2,5-dione	DMPK6YT	Discovery agent	N.A.	Investigative	[3]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione	DMGC7RY	Discovery agent	N.A.	Investigative	[3]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione	DM3EV9N	Discovery agent	N.A.	Investigative	[3]
4-(Quinolin-3-yl)-N-p-tolylpyrimidin-2-amine	DM4YFU5	Discovery agent	N.A.	Investigative	[4]
4-(Quinolin-4-yl)-N-p-tolylpyrimidin-2-amine	DMDW3SX	Discovery agent	N.A.	Investigative	[4]
AZAKENPAULLONE	DM61H07	Discovery agent	N.A.	Investigative	[5]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[2]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[2]
Thieno analogue of kenpaullone	DMIOTHG	Discovery agent	N.A.	Investigative	[5]

References

• [1] Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. Eur J Med Chem. 2010 Sep;45(9):4316-30.
• [2] Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.
• [3] Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
• [4] Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives. Eur J Med Chem. 2010 Jan;45(1):379-86.
• [5] 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.