Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMJ249P)

• Drug Name: (-)-Cercosporamide Drug Info
• Synonyms: Cercosporamide; 131436-22-1; CHEBI:78696; ( )-Cercosporamide; AC1L2Z33; SCHEMBL12658718; CTK8E7014; MolPort-006-822-609; GEWLYFZWVLXQME-MRXNPFEDSA-N; ZINC5114136; ZINC100098020; AKOS024458192; CS-4664; HY-16982; RT-011975; J-006002; (9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxodibenzofuran-4-carboxamide; 4-Dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (S)-; (9aS)-8-Acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-4-dibenzofurancaboxamide

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 131379
  ChEBI ID: CHEBI:78696
  CAS Number: CAS 131436-22-1
  TTD Drug ID: DMJ249P

Molecule-Related Drug Atlas

Drug(s) Targeting Protein kinase C alpha (PRKCA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sodium phenylbutyrate	DMXLBCQ	Spinal muscular atrophy	8B61	Approved	[2]
Sotrastaurin acetate	DME53YS	Renal transplantation	NE84	Phase 2	[3]
PMID28460551-Compound-3	DMA1FRM	N. A.	N. A.	Patented	[4]
ISIS 3521	DMZFS69	N. A.	N. A.	Discontinued in Phase 2	[5]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[6]
RO-320432	DMFZ1YW	N. A.	N. A.	Terminated	[7]
LY-317644	DMM20PI	N. A.	N. A.	Terminated	[8]
Acteoside	DM0YHKB	Nephritis	GB40	Terminated	[9]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[10]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Protein kinase C beta (PRKCB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[12]
RUBOXISTAURIN HYDROCHLORIDE	DMQOCD8	Lymphoma	2A80-2A86	Phase 3	[13]
Sotrastaurin acetate	DME53YS	Renal transplantation	NE84	Phase 2	[3]
LY333531	DMGMC8H	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
MS-553	DM7ER9J	Chronic lymphocytic leukaemia	2A82.0	Phase 1	[15]
Linetastine	DMF8B62	Rhinitis	FA20	Discontinued in Phase 2	[16]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[6]
RO-320432	DMFZ1YW	N. A.	N. A.	Terminated	[7]
LY-317644	DMM20PI	N. A.	N. A.	Terminated	[8]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[10]

Drug(s) Targeting Protein kinase C gamma (PRKCG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[17]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[6]
RO-320432	DMFZ1YW	N. A.	N. A.	Terminated	[7]
LY-317644	DMM20PI	N. A.	N. A.	Terminated	[8]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[10]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[18]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	DMDO175	Discovery agent	N.A.	Investigative	[19]
3,4-diphenyl-1H-pyrrole-2,5-dione	DMPK6YT	Discovery agent	N.A.	Investigative	[19]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione	DMGC7RY	Discovery agent	N.A.	Investigative	[19]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione	DM3EV9N	Discovery agent	N.A.	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Protein kinase C alpha (PRKCA)	TTFJ8Q1	KPCA_HUMAN	Inhibitor	[1]
Protein kinase C beta (PRKCB)	TTYPXQF	KPCB_HUMAN	Inhibitor	[1]
Protein kinase C gamma (PRKCG)	TTRFOXJ	KPCG_HUMAN	Inhibitor	[1]

References

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• [2] Polo-like kinase inhibitor Ro5203280 has potent antitumor activity in nasopharyngeal carcinoma.Mol Cancer Ther. 2013 Aug;12(8):1393-401.
• [3] Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
• [4] Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jul;27(7):753-761.
• [5] Phase II study of PKC-alpha antisense oligonucleotide aprinocarsen in combination with gemcitabine and carboplatin in patients with advanced non-small cell lung cancer.Lung Cancer.2006 May;52(2):173-80.
• [6] Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins, Bioorg. Med. Chem. Lett. 5(18):2155-2160 (1995).
• [7] Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain, Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994).
• [8] Synthesis of bisindolylmaleimide macrocycles, Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995).
• [9] Phenylethanoid glycosides from Digitalis purpurea and Penstemon linarioides with PKCalpha-inhibitory activity. J Nat Prod. 1998 Nov;61(11):1410-2.
• [10] Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
• [11] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
• [12] The oral protein-kinase C beta inhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines. Leuk Lymphoma. 2008 Jul;49(7):1374-83.
• [13] Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-9.
• [14] Protein kinase C beta inhibition attenuates the progression of experimental diabetic nephropathy in the presence of continued hypertension. Diabetes. 2003 Feb;52(2):512-8.
• [15] ClinicalTrials.gov (NCT03492125) A Study Of The Selective PKC-beta Inhibitor MS- 553. U.S. National Institutes of Health.
• [16] Potential new medical therapies for diabetic retinopathy: protein kinase C inhibitors. Am J Ophthalmol. 2002 May;133(5):693-8.
• [17] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [18] Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.
• [19] Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.