Target Information

Target General Infomation
Target ID
T88318
Former ID
TTDC00181
Target Name
Protein kinase C
Target Type
Clinical Trial
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Diabetic foot ulcer [ICD9: 707; ICD10: L88-L89]
HIV-1 infection [ICD9: 001-139, 042; ICD10: B20-B24]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Melanoma [ICD9: 172; ICD10: C43]
Psoriasis [ICD9: 696; ICD10: L40]
Parkinson's disease [ICD9: 332; ICD10: G20]
Transplant rejection [ICD9: 279.5, 996; ICD10: D89.8, T86]
Viral infections [ICD9: 054.0, 054.1, 054.2, 054.3, 075, 771.2, 052, 053; ICD10: B01, B02, A60, B00, B27, G05.1, P35.2]
BioChemical Class
Kinase
Target Validation
T88318
EC Number
EC 2.7.1.-
Drugs and Mode of Action
Drug(s) Synthetic hypericin Drug Info Phase 3 Viral infections [525201]
AEB07 Drug Info Phase 2 Transplant rejection [536867]
APH-0812 Drug Info Phase 2 HIV-1 infection [526936], [528914]
CYCLOPLATAM Drug Info Phase 2 Cancer [526263]
HO/03/03 Drug Info Phase 2 Diabetic foot ulcer [522706]
Staurosporine Drug Info Phase 2 Discovery agent [521620], [540398]
AEB701 Drug Info Phase 1 Melanoma [551507]
GCC-1290K Drug Info Phase 1 Parkinson's disease [530122]
SAFINGOL Drug Info Phase 1 Psoriasis [521599], [531343]
Rottlerin Drug Info Preclinical Parkinson's disease [536923], [539687]
Calphostin C Drug Info Terminated Discovery agent [468219], [545688]
Ro-31-8830 Drug Info Terminated Inflammatory disease [544834]
Inhibitor AEB07 Drug Info [536867]
AEB701 Drug Info [550085]
APH-0812 Drug Info [526936], [528914]
Calphostin C Drug Info [535047]
CYCLOPLATAM Drug Info [534310]
Go6850 Drug Info [535231]
Go6976 Drug Info [535669]
Ro-31-8830 Drug Info [526849]
Rottlerin Drug Info [536923]
SAFINGOL Drug Info [530494]
Staurosporine Drug Info [535047]
Synthetic hypericin Drug Info [527958]
Modulator GCC-1290K Drug Info [530122]
HO/03/03 Drug Info [550175]
Binder Selenocompounds Drug Info [535350]
References
Ref 468219(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. (Ligand id: 5156).
Ref 521599ClinicalTrials.gov (NCT00084812) Safingol and Cisplatin in Treating Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.
Ref 521620ClinicalTrials.gov (NCT00098956) 7-hydroxystaurosporine and Topotecan Hydrochloride in Treating Patients With Relapsed or Progressed Small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 522706ClinicalTrials.gov (NCT00926068) Safety and Efficacy of HO/03/03 10?? in the Treatment of Plantar Neuropathic Diabetic Foot Ulcers. U.S. National Institutes of Health.
Ref 525201ClinicalTrials.gov (NCT02448381) Topical SGX301 (Synthetic Hypericin) for the Treatment of Cutaneous T-Cell Lymphoma (Mycosis Fungoides). U.S. National Institutes of Health.
Ref 526263Results of phase II clinical trial of cycloplatam in refractory solid tumors. Vopr Onkol. 2001;47(6):752-6.
Ref 526936Bryostatin-1: a novel PKC inhibitor in clinical development. Cancer Invest. 2003;21(6):924-36.
Ref 528914Targeting the protein kinase C family: are we there yet. Nat Rev Cancer. 2007 Jul;7(7):554-62.
Ref 530122Inhibitory effect of glutamate release from rat cerebrocortical synaptosomes by dextromethorphan and its metabolite 3-hydroxymorphinan. Neurochem Int. 2009 Jul;54(8):526-34.
Ref 531343A phase I clinical trial of safingol in combination with cisplatin in advanced solid tumors. Clin Cancer Res. 2011 Apr 15;17(8):2484-92.
Ref 536867What's next in the pipeline. Am J Transplant. 2008 Oct;8(10):1972-81.
Ref 536923Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
Ref 539687(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. (Ligand id: 2611).
Ref 540398(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. (Ligand id: 346).
Ref 544834Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001273)
Ref 545688Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004175)
Ref 551507Nearly 800 Medicines and Vaccines in Clinical Testing For Cancer Offer New Hope to Patients. Pharmaceutical Research and Manufacturers of America report. 2014.
Ref 526849Oral, anti-inflammatory activity of a potent, selective, protein kinase C inhibitor. Agents Actions. 1992 Sep;37(1-2):85-9.
Ref 526936Bryostatin-1: a novel PKC inhibitor in clinical development. Cancer Invest. 2003;21(6):924-36.
Ref 527958Characterization of the interaction of hypericin with protein kinase C in U-87 MG human glioma cells. Photochem Photobiol. 2006 May-Jun;82(3):720-8.
Ref 528914Targeting the protein kinase C family: are we there yet. Nat Rev Cancer. 2007 Jul;7(7):554-62.
Ref 530122Inhibitory effect of glutamate release from rat cerebrocortical synaptosomes by dextromethorphan and its metabolite 3-hydroxymorphinan. Neurochem Int. 2009 Jul;54(8):526-34.
Ref 530494The role of protein kinase C in the synergistic interaction of safingol and irinotecan in colon cancer cells. Int J Oncol. 2009 Dec;35(6):1463-71.
Ref 534310Effect of anti-tumor agents cisplatin and cycloplatam on membrane protein kinase C activity in murine T-lymphocytes. Biokhimiia. 1996 Oct;61(10):1866-73.
Ref 535047Protein kinase C zeta isoform is critical for proliferation in human glioblastoma cell lines. J Neurooncol. 2000 Apr;47(2):109-15.
Ref 535231Protein kinase epsilon dampens the secretory response of model intestinal epithelia during ischemia. Surgery. 2001 Aug;130(2):310-8.
Ref 535350Protein kinase C as a molecular target for cancer prevention by selenocompounds. Nutr Cancer. 2001;40(1):55-63.
Ref 535669The protein kinase C inhibitor G?6976 is a potent inhibitor of DNA damage-induced S and G2 cell cycle checkpoints. Cancer Res. 2003 Jan 1;63(1):31-5.
Ref 536867What's next in the pipeline. Am J Transplant. 2008 Oct;8(10):1972-81.
Ref 536923Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.
Ref 550085Changes in Serum Cytokine Profile after AEB071 (Sotrastaurin) or Tacrolimus versus Their Combinations in Rat Heterotopic Cardiac Allografts. J Korean Soc Transplant. 2012 Dec;26(4):248-253.
Ref 550175WO patent application no. 2014,0853,81, Pharmaceutical combinations.

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