Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTYVI76)

• DTT Name: Fungal Protein kinase A (Fung ypkA)
• Synonyms: Protein kinase A
• Gene Name: Fung ypkA
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Kinase
• UniProt ID: Q56921_YEREN
• TTD ID: T87463
• Sequence:
  MKIMGTMSPSISLAKAHERISKHWQNPVGELNIEGKRYRIIDNQVVRLNPHSGFSLFREG
  VGKIFSGKMFSFSIARNLTDTLHAAQKTTSQELRSDIPNALSNLFGAKPQTELPLGWKGK
  PLSGAPDLEGMRVAETDKFAEGESHISIIETKDKQRLVAKIERSIAEGHLFAELEAYKHI
  YKTAGKHPNLANVHGMAVVPYGNRKEEALLMDEVDGWRCSDTLRSLADSWKQGKINSEAY
  WGTIKFIAHRLLDVTNHLAKAGIVHNDIKPGNVVFDRASGEPVVIDLGLHSRSGEQPKGF
  TESFKAPELGVGNLGASEKSDVFLVVSSLLHGIEGFEKDPEIKPNQGLRFITSEPAHVMD
  ENGYPIHRPGIAGVETAYTRFITDILGVSADSRPDSNEARLHEFLSDGTIDEESAKQILK
  DTLTGEMSPLPTDVRRITPKKLRELSDLLRTHLSSAATKQLDMGVVLSDLDTMLVALDKA
  EREGGVDKDQLKSFNSLILKTYSVIGAYIKGREGDTKSSSTEVSPYHRSNFMLSIVEPSL
  QRIQKHLDQTHSSDIGSLMRAHKHLETLLEVLVTLSQQGQPVTSETYSFLNRLAEAKVTL
  SQQLNTLQQQQESAKAQLSILINRSGSWADVARQSLLRFDSTRPVVKFGTEQYTAIHRQM
  MAAHAAITLQEVSEFTDDMRNFTADSIPLLIQLGRSSLMDEHLVEQREKLRELTTIAERL
  NRLEREWM
• Function: Exists as a heterotetramer consisting of two regulatory subunits that bind and inactivate two catalytic subunits.

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[1]

12 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[2]
BX-795	DMRIMLJ	Discovery agent	N.A.	Investigative	[3]
BX-912	DMZA45C	Discovery agent	N.A.	Investigative	[3]
chelerythrine	DMCP1G9	Discovery agent	N.A.	Investigative	[4]
N6 benzyl-cAMP	DMXSZ1A	Discovery agent	N.A.	Investigative	[5]
PMID19364658C33	DMSE1C3	Discovery agent	N.A.	Investigative	[6]
PMID20005102C1	DMMESBW	Discovery agent	N.A.	Investigative	[7]
PMID21742770C1	DME3JMH	Discovery agent	N.A.	Investigative	[8]
Ro-4396686	DM5DMCH	Discovery agent	N.A.	Investigative	[9]
Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPS)	DM1JWGH	Discovery agent	N.A.	Investigative	[10]
Rp-cAMPS	DMG0S9B	Discovery agent	N.A.	Investigative	[11]
[3H]cAMP	DMZRQU7	Discovery agent	N.A.	Investigative	[11]

References

• [1] Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address
• [2] 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
• [3] Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
• [4] A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
• [5] cAMP analog mapping of Epac1 and cAMP kinase. Discriminating analogs demonstrate that Epac and cAMP kinase act synergistically to promote PC-12 cel... J Biol Chem. 2003 Sep 12;278(37):35394-402.
• [6] Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51.
• [7] 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83.
• [8] A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
• [9] Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
• [10] Inhibition of protein kinase A activity interferes with long-term, but not short-term, memory of conditioned taste aversions. Behav Neurosci. 2002 Dec;116(6):1070-4.
• [11] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1694).