Drug General Information |
Drug ID |
D0B9EH
|
Former ID |
DCL000019
|
Drug Name |
Dermolastin
|
Drug Type |
Small molecular drug
|
Indication |
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10:L00-L99]
|
Discontinued in Phase 2 |
[1]
|
Company |
Arriva Pharma
|
Structure |
|
Download
2D MOL
3D MOL
|
Formula |
C27H31NOS2
|
Canonical SMILES |
CCN(CC=CC#CC(C)(C)C)CC1=CC(=CC=C1)OCC2=CC(=CS2)C3=CSC=C<br />3
|
InChI |
1S/C27H31NOS2/c1-5-28(14-8-6-7-13-27(2,3)4)18-22-10-9-11-25(16-22)29-19-26-17-24(21-31-26)23-12-15-30-20-23/h6,8-12,15-17,20-21H,5,14,18-19H2,1-4H3/b8-6+
|
InChIKey |
KIRGLCXNEVICOG-SOFGYWHQSA-N
|
PubChem Compound ID |
|
PubChem Substance ID |
11969045, 12014524, 14808557, 29217603, 43035751, 53466659, 57369379, 103197210, 103941282, 114567706, 134338732, 134340267, 135167254, 135650692, 163621011, 163686342, 172919320, 185974820, 234856456, 234856459, 252480125
|
Target and Pathway |
Target(s) |
Leukocyte elastase |
Target Info |
Inhibitor |
[2],
[3],
[4],
[5]
|
Cathepsin G |
Target Info |
Inhibitor |
[2],
[3],
[4],
[5]
|
Tissue kallikrein |
Target Info |
Inhibitor |
[2],
[3],
[4],
[5]
|
Trypsin |
Target Info |
Inhibitor |
[2],
[3],
[4],
[5]
|
Coagulation factor IIa |
Target Info |
Inhibitor |
[2],
[3],
[4],
[5]
|
KEGG Pathway
|
Transcriptional misregulation in cancer
|
Systemic lupus erythematosushsa04080:Neuroactive ligand-receptor interaction
|
Lysosome
|
Renin-angiotensin system
|
Amoebiasis
|
Systemic lupus erythematosushsa04961:Endocrine and other factor-regulated calcium reabsorptionhsa04080:Neuroactive ligand-receptor interaction
|
Pancreatic secretion
|
Protein digestion and absorption
|
Influenza Ahsa04080:Neuroactive ligand-receptor interaction
|
Complement and coagulation cascades
|
Regulation of actin cytoskeleton
|
NetPath Pathway
|
IL2 Signaling PathwayNetPath_11:TCR Signaling Pathway
|
PANTHER Pathway
|
Blood coagulation
|
Pathway Interaction Database
|
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
|
C-MYB transcription factor networkupa_upar_pathway:Urokinase-type plasminogen activator (uPA) and uPAR-mediated signalingar_pathway:Coregulation of Androgen receptor activity
|
Regulation of Androgen receptor activitythrombin_pathway:Thrombin/protease-activated receptor (PAR) pathway
|
Angiopoietin receptor Tie2-mediated signaling
|
FOXA2 and FOXA3 transcription factor networks
|
PAR4-mediated thrombin signaling events
|
Syndecan-4-mediated signaling events
|
PAR1-mediated thrombin signaling events
|
PathWhiz Pathway
|
Vitamin K Metabolism
|
Coagulation
|
Reactome
|
Collagen degradation
|
Degradation of the extracellular matrix
|
Activation of Matrix MetalloproteinasesR-HSA-1474228:Degradation of the extracellular matrix
|
Activation of Matrix Metalloproteinases
|
Metabolism of Angiotensinogen to Angiotensins
|
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)R-HSA-1592389:Activation of Matrix Metalloproteinases
|
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
|
Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3R-HSA-1592389:Activation of Matrix Metalloproteinases
|
Cobalamin (Cbl, vitamin B12) transport and metabolismR-HSA-140837:Intrinsic Pathway of Fibrin Clot Formation
|
Common Pathway of Fibrin Clot Formation
|
Gamma-carboxylation of protein precursors
|
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus
|
Removal of aminoterminal propeptides from gamma-carboxylated proteins
|
Cell surface interactions at the vascular wall
|
Peptide ligand-binding receptors
|
G alpha (q) signalling events
|
Thrombin signalling through proteinase activated receptors (PARs)
|
WikiPathways
|
Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
|
Human Complement System
|
Degradation of collagenWP554:ACE Inhibitor Pathway
|
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)WP2263:Prostate CancerWP2769:Activation of Matrix MetalloproteinasesWP558:Complement and Coagulation Cascades
|
Regulation of Actin Cytoskeleton
|
IL1 and megakaryotyces in obesity
|
Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
|
PTM: gamma carboxylation, hypusine formation and arylsulfatase activation
|
Blood Clotting Cascade
|
Gastrin-CREB signalling pathway via PKC and MAPK
|
Thrombin signalling through proteinase activated receptors (PARs)
|
Platelet Aggregation (Plug Formation)
|
GPCR ligand binding
|
GPCR downstream signaling
|
Formation of Fibrin Clot (Clotting Cascade)
|
Cell surface interactions at the vascular wall
|
Folate Metabolism
|
Vitamin B12 Metabolism
|
Selenium Micronutrient Network
|
References |
REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071) |
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REF 2 | rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82. |
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REF 3 | Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20. |
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REF 4 | Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34. |
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REF 5 | Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009. |