Target Information

Target General Information

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Target ID

T88318 (Former ID: TTDC00181)

Target Name

Protein kinase C (PRKC)

Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 1 Target-related Diseases

Virus infection [ICD-11: 1A24-1D9Z]

BioChemical Class

Kinase

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Clinical Trial Drug(s)

[+] 9 Clinical Trial Drugs

Synthetic hypericin

Drug Info

Phase 3

Virus infection

[2]

AEB07

Drug Info

Phase 2

Transplant rejection

[4]

APH-0812

Drug Info

Phase 2

Human immunodeficiency virus-1 infection

[5], [6]

CYCLOPLATAM

Drug Info

Phase 2

Solid tumour/cancer

[7]

HO/03/03

Drug Info

Phase 2

Diabetic foot ulcer

[8]

LXS196

Drug Info

Phase 1/2

Solid tumour/cancer

[9]

AEB701

Drug Info

Phase 1

Melanoma

[10]

GCC-1290K

Drug Info

Phase 1

Parkinson disease

[11]

SAFINGOL

Drug Info

Phase 1

Psoriasis vulgaris

[12], [13]

Discontinued Drug(s)

[+] 2 Discontinued Drugs

Tecadenoson

Drug Info

Discontinued in Phase 3

Cardiac arrhythmias

[14], [15]

Ro-31-8830

Drug Info

Terminated

Inflammation

[18]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

Rottlerin

Drug Info

Preclinical

Parkinson disease

[16], [17]

Mode of Action

[+] 3 Modes of Action

Inhibitor

[+] 13 Inhibitor drugs

Synthetic hypericin

Drug Info

[1]

AEB07

Drug Info

[4]

APH-0812

Drug Info

[5], [6]

CYCLOPLATAM

Drug Info

[19]

LXS196

Drug Info

[21]

AEB701

Drug Info

[22]

SAFINGOL

Drug Info

[23]

Rottlerin

Drug Info

[17]

Calphostin C

Drug Info

[25]

Ro-31-8830

Drug Info

[26]

Bisindolylmaleimide-I

Drug Info

[27]

G6976

Drug Info

[28]

Staurosporine

Drug Info

[25]

Modulator

[+] 2 Modulator drugs

HO/03/03

Drug Info

[20]

GCC-1290K

Drug Info

[11]

Binder

[+] 1 Binder drugs

Tecadenoson

Drug Info

[24]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

Top

REF 1

Characterization 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 2

ClinicalTrials.gov (NCT02448381) Topical SGX301 (Synthetic Hypericin) for the Treatment of Cutaneous T-Cell Lymphoma (Mycosis Fungoides). U.S. National Institutes of Health.

REF 3

ClinicalTrials.gov (NCT03560245) A Randomized, Double-Blind, Placebo-Controlled, Phase 2 Study Assessing the Safety, Tolerability and Efficacy of Bryostatin in the Treatment of Moderately Severe to Severe Alzheimer's Disease Subjects Not Receiving Memantine Treatment. U.S.National Institutes of Health.

REF 4

What's next in the pipeline. Am J Transplant. 2008 Oct;8(10):1972-81.

REF 5

Targeting the protein kinase C family: are we there yet. Nat Rev Cancer. 2007 Jul;7(7):554-62.

REF 6

Bryostatin-1: a novel PKC inhibitor in clinical development. Cancer Invest. 2003;21(6):924-36.

REF 7

Results of phase II clinical trial of cycloplatam in refractory solid tumors. Vopr Onkol. 2001;47(6):752-6.

REF 8

ClinicalTrials.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 9

ClinicalTrials.gov (NCT03947385) Study of IDE196 in Patients With Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions. U.S. National Institutes of Health.

REF 10

Nearly 800 Medicines and Vaccines in Clinical Testing For Cancer Offer New Hope to Patients. Pharmaceutical Research and Manufacturers of America report. 2014.

REF 11

Inhibitory effect of glutamate release from rat cerebrocortical synaptosomes by dextromethorphan and its metabolite 3-hydroxymorphinan. Neurochem Int. 2009 Jul;54(8):526-34.

REF 12

ClinicalTrials.gov (NCT00084812) Safingol and Cisplatin in Treating Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.

REF 13

A 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 14

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. (Ligand id: 5592).

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010504)

REF 16

REF 17

Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42.

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001273)

REF 19

Effect 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 20

WO patent application no. 2014,0853,81, Pharmaceutical combinations.

REF 21

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 22

Changes 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 23

The 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 24

Protein kinase C as a molecular target for cancer prevention by selenocompounds. Nutr Cancer. 2001;40(1):55-63.

REF 25

Protein kinase C zeta isoform is critical for proliferation in human glioblastoma cell lines. J Neurooncol. 2000 Apr;47(2):109-15.

REF 26

Oral, anti-inflammatory activity of a potent, selective, protein kinase C inhibitor. Agents Actions. 1992 Sep;37(1-2):85-9.

REF 27

Protein kinase epsilon dampens the secretory response of model intestinal epithelia during ischemia. Surgery. 2001 Aug;130(2):310-8.

REF 28

The 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.

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