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Identification
NameMinocycline
Accession NumberDB01017  (APRD00547)
Typesmall molecule
Groupsapproved, investigational
Description

A tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
(4S,4AS,5ar,12as)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamideNot AvailableNot Available
7-Dimethylamino-6-demethyl-6-deoxytetracyclineNot AvailableNot Available
MinociclinaSpanishINN
MinociclinumNot AvailableNot Available
MinocyclinNot AvailableNot Available
MinocyclinumLatinINN
Salts
Name/CAS Structure Properties
Minocycline Hydrochloride
13614-98-7
Thumb
  • InChI Key: WTJXVDPDEQKTCV-VQAITOIOSA-N
  • Monoisotopic Mass: 493.161577972
  • Average Mass: 493.937
DBSALT000721
Brand names
NameCompany
AkneminNot Available
Apo-MinocyclineNot Available
ArestinNot Available
DynacinNot Available
KlinomycinNot Available
MinocinTriax Pharmaceuticals, LLC]
MinodermNot Available
MinomycinNot Available
MinopenNot Available
MinoxNot Available
MinozNot Available
SolodynNot Available
VectrinNot Available
XiminoNot Available
Brand mixturesNot Available
Categories
CAS number10118-90-8
WeightAverage: 457.4764
Monoisotopic: 457.184900233
Chemical FormulaC23H27N3O7
InChI KeyDYKFCLLONBREIL-KVUCHLLUSA-N
InChI
InChI=1S/C23H27N3O7/c1-25(2)12-5-6-13(27)15-10(12)7-9-8-11-17(26(3)4)19(29)16(22(24)32)21(31)23(11,33)20(30)14(9)18(15)28/h5-6,9,11,17,27,29-30,33H,7-8H2,1-4H3,(H2,24,32)/t9-,11-,17-,23-/m0/s1
IUPAC Name
(4S,4aS,5aR,12aS)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide
SMILES
[H][C@@]12CC3=C(C(O)=CC=C3N(C)C)C(=O)C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@]1([H])C2
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassBenzenoids
ClassAcenes and Derivatives
SubclassNaphthacenes
Direct parentNaphthacenes
Alternative parentsAnthracenecarboxylic Acids and Derivatives; Anthraquinones; Tetralins; Aminophenols; Tertiary Alcohols; Tertiary Amines; Primary Carboxylic Acid Amides; Polyols; Ketones; Carboxylic Acids; Enols; Polyamines; Enolates
Substituentsanthraquinone; tetralin; aminophenol; phenol derivative; benzene; tertiary alcohol; primary carboxylic acid amide; carboxamide group; tertiary amine; polyol; ketone; enolate; carboxylic acid derivative; polyamine; enol; carboxylic acid; amine; carbonyl group; alcohol; organonitrogen compound
Classification descriptionThis compound belongs to the naphthacenes. These are compounds containing a naphthacene moiety, which is a polyaromatic hydrocarbon made of four linearly fused benzene rings.
Pharmacology
IndicationFor the treatment of infections caused by susceptible strains of microorganisms, such as Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsial pox and tick fevers caused by Rickettsiae, upper respiratory tract infections caused by Streptococcus pneumoniae and for the treatment of asymptomatic carriers of Neisseria meningitidis.
PharmacodynamicsMinocycline, the most lipid soluble and most active tetracycline antibiotic, is, like doxycycline, a long-acting tetracycline. Minocycline's effects are related to the inhibition of protein synthesis. Although minocycline's broader spectrum of activity, compared to other members of the group, includes activity against Neisseria meningitidis, its use as a prophylaxis is no longer recomended because of side effects (dizziness and vertigo). Current research is examining the possible neuroprotective effects of minocycline against progression of Huntington's Disease, an inherited neurodegenerative disorder. The neuroprotective action of minocycline may include its inhibitory effect on 5-lipoxygenase, an inflammatory enzyme associated with brain aging.
Mechanism of actionMinocycline passes directly through the lipid bilayer or passively diffuses through porin channels in the bacterial membrane. Tetracyclines like minocycline bind to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex and interfering with protein synthesis.
AbsorptionRapidly absorbed from the gastrointestinal tract and absorption is not significantly impaired by ingestion of food or milk. Oral bioavailability is 100%.
Volume of distributionNot Available
Protein binding55% to 76%
Metabolism

Hepatic.

Route of eliminationNot Available
Half life11-22 hours
ClearanceNot Available
ToxicityMinocycline has been observed to cause a dark discoloration of the thyroid in experimental animals (rats, minipigs, dogs and monkeys). In the rat, chronic treatment with minocycline has resulted in goiter accompanied by elevated radioactive iodine uptake and evidence of thyroid tumor production. Minocycline has also been found to produce thyroid hyperplasia in rats and dogs. LD50=2380 mg/kg (rat, oral), LD50=3600 mg/kg (mouse, oral)
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
PathwayCategorySMPDB ID
Minocycline Action PathwayDrug actionSMP00292
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.7469
Blood Brain Barrier - 0.9783
Caco-2 permeable + 0.5711
P-glycoprotein substrate Substrate 0.7366
P-glycoprotein inhibitor I Non-inhibitor 0.7968
P-glycoprotein inhibitor II Non-inhibitor 0.7036
Renal organic cation transporter Non-inhibitor 0.9536
CYP450 2C9 substrate Non-substrate 0.8145
CYP450 2D6 substrate Non-substrate 0.9036
CYP450 3A4 substrate Substrate 0.6805
CYP450 1A2 substrate Non-inhibitor 0.9088
CYP450 2C9 substrate Non-inhibitor 0.9071
CYP450 2D6 substrate Non-inhibitor 0.9232
CYP450 2C19 substrate Non-inhibitor 0.9081
CYP450 3A4 substrate Non-inhibitor 0.9058
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7561
Ames test Non AMES toxic 0.8909
Carcinogenicity Non-carcinogens 0.9091
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.4354 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9954
hERG inhibition (predictor II) Non-inhibitor 0.6783
Pharmacoeconomics
Manufacturers
  • Medicis pharmaceutical corp
  • Triax pharmaceuticals llc
  • Aurobindo pharma ltd
  • Impax laboratories inc
  • Ranbaxy laboratories ltd
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Lederle laboratories div american cyanamid co
  • Orapharma inc
  • Barr laboratories inc
  • Matrix laboratories ltd
  • Sandoz inc
  • Dr reddys laboratories ltd
  • Medicis Pharmaceutical Corporation
Packagers
Dosage forms
FormRouteStrength
CapsuleOral
Prices
Unit descriptionCostUnit
Minocin PAC 100 mg Kit Box695.5USDbox
Minocin kit 100 mg combo668.17USDkit
Minocin kit 50 mg combo334.78USDkit
Minocin 100 mg vial59.64USDvial
Arestin 1 mg microsphere30.0USDeach
Solodyn 135 mg 24 Hour tablet24.89USDtablet
Solodyn 45 mg 24 Hour tablet24.89USDtablet
Solodyn 65 mg 24 Hour tablet24.89USDtablet
Solodyn 90 mg 24 Hour tablet24.89USDtablet
Solodyn er 115 mg tablet23.93USDtablet
Solodyn er 135 mg tablet23.93USDtablet
Solodyn er 45 mg tablet23.93USDtablet
Solodyn er 65 mg tablet23.93USDtablet
Solodyn er 90 mg tablet23.93USDtablet
Minocycline hcl powder21.0USDg
Minocycline HCl 135 mg 24 Hour tablet19.21USDtablet
Minocycline HCl 45 mg 24 Hour tablet19.21USDtablet
Dynacin 100 mg tablet13.37USDtablet
Dynacin 75 mg tablet13.12USDtablet
Minocin 100 mg capsule12.05USDcapsule
Minocin 100 mg pelletized cap11.11USDpellet
Dynacin 50 mg tablet8.76USDtablet
Dynacin 75 mg capsule7.15USDcapsule
Minocycline hcl 100 mg tablet6.15USDtablet
Minocin 50 mg pelletized cap5.56USDpellet
Minocin 50 mg capsule5.24USDcapsule
Minocycline hcl 75 mg tablet5.14USDtablet
Dynacin 50 mg capsule3.85USDcapsule
Minocycline HCl 100 mg capsule3.53USDcapsule
Minocycline hcl 50 mg tablet3.5USDtablet
Minocycline HCl 75 mg capsule2.06USDcapsule
Minocycline 75 mg capsule1.98USDcapsule
Minocycline HCl 50 mg capsule1.77USDcapsule
Minocin 100 mg Capsule1.34USDcapsule
Apo-Minocycline 100 mg Capsule1.08USDcapsule
Minocycline 100 mg Capsule1.08USDcapsule
Mylan-Minocycline 100 mg Capsule1.08USDcapsule
Novo-Minocycline 100 mg Capsule1.08USDcapsule
Pms-Minocycline 100 mg Capsule1.08USDcapsule
Ratio-Minocycline 100 mg Capsule1.08USDcapsule
Sandoz Minocycline 100 mg Capsule1.08USDcapsule
Minocin 50 mg Capsule0.69USDcapsule
Apo-Minocycline 50 mg Capsule0.56USDcapsule
Minocycline 50 mg Capsule0.56USDcapsule
Mylan-Minocycline 50 mg Capsule0.56USDcapsule
Novo-Minocycline 50 mg Capsule0.56USDcapsule
Pms-Minocycline 50 mg Capsule0.56USDcapsule
Ratio-Minocycline 50 mg Capsule0.56USDcapsule
Sandoz Minocycline 50 mg Capsule0.56USDcapsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States75413472007-04-022027-04-02
United States59088381998-02-192018-02-19
Canada13305331994-07-052011-07-05
Properties
Statesolid
Experimental Properties
PropertyValueSource
water solubility5.2E+004 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP0.05SANGSTER (1993)
Predicted Properties
PropertyValueSource
water solubility3.07e+00 g/lALOGPS
logP-0.03ALOGPS
logP-3.3ChemAxon
logS-2.2ALOGPS
pKa (strongest acidic)-2.3ChemAxon
pKa (strongest basic)8.25ChemAxon
physiological charge-1ChemAxon
hydrogen acceptor count9ChemAxon
hydrogen donor count5ChemAxon
polar surface area164.63ChemAxon
rotatable bond count3ChemAxon
refractivity122.54ChemAxon
polarizability45.9ChemAxon
number of rings4ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterNoChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Zita Mendes, Jose Rafael Antunes, Susana Marto, William Heggie, “Crystalline Minocycline Base and Processes for its Preparation.” U.S. Patent US20100286417, issued November 11, 2010.

US20100286417
General Reference
  1. Link
  2. Link
  3. Gough A, Chapman S, Wagstaff K, Emery P, Elias E: Minocycline induced autoimmune hepatitis and systemic lupus erythematosus-like syndrome. BMJ. 1996 Jan 20;312(7024):169-72. Pubmed
  4. Chen M, Ona VO, Li M, Ferrante RJ, Fink KB, Zhu S, Bian J, Guo L, Farrell LA, Hersch SM, Hobbs W, Vonsattel JP, Cha JH, Friedlander RM: Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease. Nat Med. 2000 Jul;6(7):797-801. Pubmed
  5. Tikka TM, Koistinaho JE: Minocycline provides neuroprotection against N-methyl-D-aspartate neurotoxicity by inhibiting microglia. J Immunol. 2001 Jun 15;166(12):7527-33. Pubmed
  6. Nirmalananthan N, Greensmith L: Amyotrophic lateral sclerosis: recent advances and future therapies. Curr Opin Neurol. 2005 Dec;18(6):712-9. Pubmed
  7. Song Y, Wei EQ, Zhang WP, Zhang L, Liu JR, Chen Z: Minocycline protects PC12 cells from ischemic-like injury and inhibits 5-lipoxygenase activation. Neuroreport. 2004 Oct 5;15(14):2181-4. Pubmed
External Links
ResourceLink
KEGG DrugD05045
KEGG CompoundC07225
BindingDB50046515
ChEBI50694
ChEMBLCHEMBL1434
Therapeutic Targets DatabaseDAP000405
PharmGKBPA450519
Drug Product Database2242080
RxListhttp://www.rxlist.com/cgi/generic/minocycline.htm
Drugs.comhttp://www.drugs.com/minocycline.html
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/min1270.shtml
WikipediaMinocycline
ATC CodesA01AB23J01AA08
AHFS Codes
  • 08:12.24
PDB Entries
FDA labelshow(3.02 MB)
MSDSshow(73.6 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe tetracycline, minocycline, may increase the anticoagulant effect of acenocoumarol.
AcitretinIncreased risk of intracranial hypertension.
AluminiumFormation of non-absorbable complexes
AmoxicillinPossible antagonism of action
AmpicillinPossible antagonism of action
AnisindioneThe tetracycline, minocycline, may increase the anticoagulant effect of anisindione.
AttapulgiteFormation of non-absorbable complexes
AzlocillinPossible antagonism of action
AztreonamPossible antagonism of action
BacampicillinPossible antagonism of action
BenzylpenicillinPossible antagonism of action
BexaroteneTetracycline derivatives like minocycline may enhance the adverse/toxic effect of Retinoic Acid Derivatives. Due to the risk of developing pseudotumor cerebri (also known as intracranial hypertension), avoid this combination of drugs if possible. If used concomitantly, monitor for evidence of this interaction (eg, dizziness, diplopia, headache).
Bismuth SubsalicylateFormation of non-absorbable complexes
CalciumFormation of non-absorbable complexes
Calcium AcetateCalcium salts such as calcium acetate may decrease the serum concentration of tetracycline derivatives such as minocycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives.
Calcium ChlorideCalcium salts such as calcium chloride may decrease the serum concentration of tetracycline derivatives such as minocycline. In general, the coadministration of oral calcium salts and oral tetracycline derivatives should be avoided. Interactions may be able to be minimized by administering oral calcium preparations several hours before or after the dose of the oral tetracycline derivatives. Even with dose separation, therapy may still be compromised. Monitor for decreased therapeutic effect of oral tetracycline derivatives.
CarbenicillinPossible antagonism of action
ClavulanatePossible antagonism of action
CloxacillinPossible antagonism of action
ColesevelamBile acid sequestrants such as colesevelam may decrease the absorption of Tetracycline Derivatives. Monitor for decreased therapeutic effects of tetracycline derivatives if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction. The manufacturer of colesevelam suggests that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
CyclacillinPossible antagonism of action
DicloxacillinPossible antagonism of action
DicoumarolThe tetracycline, minocycline, may increase the anticoagulant effect of dicumarol.
Ethinyl EstradiolThis anti-infectious agent could decrease the effect of the oral contraceptive
EtretinateIncreased risk of intracranial hypertension
FlucloxacillinPossible antagonism of action
HetacillinPossible antagonism of action
IronFormation of non-absorbable complexes
Iron DextranFormation of non-absorbable complexes
IsotretinoinIncreased risk of intracranial hypertension
MagnesiumFormation of non-absorbable complexes
Magnesium oxideFormation of non-absorbable complexes
Magnesium salicylateFormation of non-absorbable complexes
MestranolThis anti-infectious agent could decrease the effect of the oral contraceptive
Methicillin Acyl-SerinePossible antagonism of action
MethoxyfluraneThe tetracycline, minocycline, may increase the renal toxicity of methoxyflurane.
MezlocillinPossible antagonism of action
NafcillinPossible antagonism of action
OxacillinPossible antagonism of action
Penicillin VPossible antagonism of action
PiperacillinPossible antagonism of action
PivampicillinPossible antagonism of action
PivmecillinamPossible antagonism of action
TazobactamPossible antagonism of action
TicarcillinMinocycline may reduce the effect of Ticarcillin by inhibiting bacterial growth. Ticarcillin exerts its effects on actively growing bacteria. To achieve synergism, Ticarcillin should be administered at least 2 hours prior to using Minocycline.
TretinoinMinocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Trisalicylate-cholineFormation of non-absorbable complexes
WarfarinThe tetracycline, minocycline, may increase the anticoagulant effect of warfarin.
ZincFormation of non-absorbable complexes
Food Interactions
  • Calcium and iron needs increased with long term use.
  • Do not take Aluminum or magnesium antacids or supplements while on this medication.
  • Take with food.

Targets

1. 30S ribosomal protein S9

Kind: protein

Organism: Escherichia coli (strain K12)

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
30S ribosomal protein S9 P0A7X3 Details

References:

  1. Zhanel GG, Homenuik K, Nichol K, Noreddin A, Vercaigne L, Embil J, Gin A, Karlowsky JA, Hoban DJ: The glycylcyclines: a comparative review with the tetracyclines. Drugs. 2004;64(1):63-88. Pubmed

2. 30S ribosomal protein S4

Kind: protein

Organism: Escherichia coli (strain K12)

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
30S ribosomal protein S4 P0A7V8 Details

References:

  1. Zhanel GG, Homenuik K, Nichol K, Noreddin A, Vercaigne L, Embil J, Gin A, Karlowsky JA, Hoban DJ: The glycylcyclines: a comparative review with the tetracyclines. Drugs. 2004;64(1):63-88. Pubmed

3. 16S rRNA

Kind: nucleotide

Organism: Enteric bacteria and other eubacteria

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

4. Interleukin-1 beta

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: modulator

Components

Name UniProt ID Details
Interleukin-1 beta P01584 Details

References:

  1. Sadowski T, Steinmeyer J: Minocycline inhibits the production of inducible nitric oxide synthase in articular chondrocytes. J Rheumatol. 2001 Feb;28(2):336-40. Pubmed
  2. Oringer RJ, Al-Shammari KF, Aldredge WA, Iacono VJ, Eber RM, Wang HL, Berwald B, Nejat R, Giannobile WV: Effect of locally delivered minocycline microspheres on markers of bone resorption. J Periodontol. 2002 Aug;73(8):835-42. Pubmed
  3. Amin AR, Attur MG, Thakker GD, Patel PD, Vyas PR, Patel RN, Patel IR, Abramson SB: A novel mechanism of action of tetracyclines: effects on nitric oxide synthases. Proc Natl Acad Sci U S A. 1996 Nov 26;93(24):14014-9. Pubmed
  4. Steinmeyer J, Daufeldt S, Taiwo YO: Pharmacological effect of tetracyclines on proteoglycanases from interleukin-1-treated articular cartilage. Biochem Pharmacol. 1998 Jan 1;55(1):93-100. Pubmed

5. Arachidonate 5-lipoxygenase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Arachidonate 5-lipoxygenase P09917 Details

References:

  1. Song Y, Wei EQ, Zhang WP, Zhang L, Liu JR, Chen Z: Minocycline protects PC12 cells from ischemic-like injury and inhibits 5-lipoxygenase activation. Neuroreport. 2004 Oct 5;15(14):2181-4. Pubmed
  2. Song Y, Wei EQ, Zhang WP, Ge QF, Liu JR, Wang ML, Huang XJ, Hu X, Chen Z: Minocycline protects PC12 cells against NMDA-induced injury via inhibiting 5-lipoxygenase activation. Brain Res. 2006 Apr 26;1085(1):57-67. Epub 2006 Mar 30. Pubmed
  3. Chu LS, Fang SH, Zhou Y, Yu GL, Wang ML, Zhang WP, Wei EQ: Minocycline inhibits 5-lipoxygenase activation and brain inflammation after focal cerebral ischemia in rats. Acta Pharmacol Sin. 2007 Jun;28(6):763-72. Pubmed

6. Matrix metalloproteinase-9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Matrix metalloproteinase-9 P14780 Details

References:

  1. Brundula V, Rewcastle NB, Metz LM, Bernard CC, Yong VW: Targeting leukocyte MMPs and transmigration: minocycline as a potential therapy for multiple sclerosis. Brain. 2002 Jun;125(Pt 6):1297-308. Pubmed
  2. Sutton TA, Kelly KJ, Mang HE, Plotkin Z, Sandoval RM, Dagher PC: Minocycline reduces renal microvascular leakage in a rat model of ischemic renal injury. Am J Physiol Renal Physiol. 2005 Jan;288(1):F91-7. Epub 2004 Sep 7. Pubmed
  3. Koistinaho M, Malm TM, Kettunen MI, Goldsteins G, Starckx S, Kauppinen RA, Opdenakker G, Koistinaho J: Minocycline protects against permanent cerebral ischemia in wild type but not in matrix metalloprotease-9-deficient mice. J Cereb Blood Flow Metab. 2005 Apr;25(4):460-7. Pubmed
  4. Lee CZ, Yao JS, Huang Y, Zhai W, Liu W, Guglielmo BJ, Lin E, Yang GY, Young WL: Dose-response effect of tetracyclines on cerebral matrix metalloproteinase-9 after vascular endothelial growth factor hyperstimulation. J Cereb Blood Flow Metab. 2006 Sep;26(9):1157-64. Epub 2006 Jan 4. Pubmed
  5. Machado LS, Kozak A, Ergul A, Hess DC, Borlongan CV, Fagan SC: Delayed minocycline inhibits ischemia-activated matrix metalloproteinases 2 and 9 after experimental stroke. BMC Neurosci. 2006 Jul 17;7:56. Pubmed

7. Vascular endothelial growth factor A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Vascular endothelial growth factor A P15692 Details

References:

  1. Sasamura H, Takahashi A, Miyao N, Yanase M, Masumori N, Kitamura H, Itoh N, Tsukamoto T: Inhibitory effect on expression of angiogenic factors by antiangiogenic agents in renal cell carcinoma. Br J Cancer. 2002 Mar 4;86(5):768-73. Pubmed
  2. Yao JS, Chen Y, Zhai W, Xu K, Young WL, Yang GY: Minocycline exerts multiple inhibitory effects on vascular endothelial growth factor-induced smooth muscle cell migration: the role of ERK1/2, PI3K, and matrix metalloproteinases. Circ Res. 2004 Aug 20;95(4):364-71. Epub 2004 Jul 15. Pubmed
  3. Rocchetti R, Talevi S, Margiotta C, Calza R, Corallini A, Possati L: Antiangiogenic drugs for chemotherapy of bladder tumours. Chemotherapy. 2005 Oct;51(6):291-9. Epub 2005 Oct 13. Pubmed

8. Caspase-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: negative modulator

Components

Name UniProt ID Details
Caspase-1 P29466 Details

References:

  1. Chen M, Ona VO, Li M, Ferrante RJ, Fink KB, Zhu S, Bian J, Guo L, Farrell LA, Hersch SM, Hobbs W, Vonsattel JP, Cha JH, Friedlander RM: Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease. Nat Med. 2000 Jul;6(7):797-801. Pubmed
  2. Sanchez Mejia RO, Ona VO, Li M, Friedlander RM: Minocycline reduces traumatic brain injury-mediated caspase-1 activation, tissue damage, and neurological dysfunction. Neurosurgery. 2001 Jun;48(6):1393-9; discussion 1399-401. Pubmed
  3. Vincent JA, Mohr S: Inhibition of caspase-1/interleukin-1beta signaling prevents degeneration of retinal capillaries in diabetes and galactosemia. Diabetes. 2007 Jan;56(1):224-30. Pubmed
  4. Kim HS, Suh YH: Minocycline and neurodegenerative diseases. Behav Brain Res. 2009 Jan 23;196(2):168-79. Epub 2008 Oct 11. Pubmed

9. Caspase-3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: negative modulator

Components

Name UniProt ID Details
Caspase-3 P42574 Details

References:

  1. Chen M, Ona VO, Li M, Ferrante RJ, Fink KB, Zhu S, Bian J, Guo L, Farrell LA, Hersch SM, Hobbs W, Vonsattel JP, Cha JH, Friedlander RM: Minocycline inhibits caspase-1 and caspase-3 expression and delays mortality in a transgenic mouse model of Huntington disease. Nat Med. 2000 Jul;6(7):797-801. Pubmed
  2. Arvin KL, Han BH, Du Y, Lin SZ, Paul SM, Holtzman DM: Minocycline markedly protects the neonatal brain against hypoxic-ischemic injury. Ann Neurol. 2002 Jul;52(1):54-61. Pubmed
  3. Dommergues MA, Plaisant F, Verney C, Gressens P: Early microglial activation following neonatal excitotoxic brain damage in mice: a potential target for neuroprotection. Neuroscience. 2003;121(3):619-28. Pubmed
  4. Lee SM, Yune TY, Kim SJ, Park DW, Lee YK, Kim YC, Oh YJ, Markelonis GJ, Oh TH: Minocycline reduces cell death and improves functional recovery after traumatic spinal cord injury in the rat. J Neurotrauma. 2003 Oct;20(10):1017-27. Pubmed
  5. Baptiste DC, Hartwick AT, Jollimore CA, Baldridge WH, Seigel GM, Kelly ME: An investigation of the neuroprotective effects of tetracycline derivatives in experimental models of retinal cell death. Mol Pharmacol. 2004 Nov;66(5):1113-22. Epub 2004 Aug 10. Pubmed
  6. Kim HS, Suh YH: Minocycline and neurodegenerative diseases. Behav Brain Res. 2009 Jan 23;196(2):168-79. Epub 2008 Oct 11. Pubmed

10. Cytochrome c

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: negative modulator

Components

Name UniProt ID Details
Cytochrome c P99999 Details

References:

  1. Zhu S, Stavrovskaya IG, Drozda M, Kim BY, Ona V, Li M, Sarang S, Liu AS, Hartley DM, Wu DC, Gullans S, Ferrante RJ, Przedborski S, Kristal BS, Friedlander RM: Minocycline inhibits cytochrome c release and delays progression of amyotrophic lateral sclerosis in mice. Nature. 2002 May 2;417(6884):74-8. Pubmed
  2. Matsuki S, Iuchi Y, Ikeda Y, Sasagawa I, Tomita Y, Fujii J: Suppression of cytochrome c release and apoptosis in testes with heat stress by minocycline. Biochem Biophys Res Commun. 2003 Dec 19;312(3):843-9. Pubmed
  3. Chu HC, Lin YL, Sytwu HK, Lin SH, Liao CL, Chao YC: Effects of minocycline on Fas-mediated fulminant hepatitis in mice. Br J Pharmacol. 2005 Jan;144(2):275-82. Pubmed
  4. Heo K, Cho YJ, Cho KJ, Kim HW, Kim HJ, Shin HY, Lee BI, Kim GW: Minocycline inhibits caspase-dependent and -independent cell death pathways and is neuroprotective against hippocampal damage after treatment with kainic acid in mice. Neurosci Lett. 2006 May 8;398(3):195-200. Epub 2006 Feb 15. Pubmed
  5. Mansson R, Hansson MJ, Morota S, Uchino H, Ekdahl CT, Elmer E: Re-evaluation of mitochondrial permeability transition as a primary neuroprotective target of minocycline. Neurobiol Dis. 2007 Jan;25(1):198-205. Epub 2006 Oct 24. Pubmed
  6. Kim HS, Suh YH: Minocycline and neurodegenerative diseases. Behav Brain Res. 2009 Jan 23;196(2):168-79. Epub 2008 Oct 11. Pubmed

Transporters

1. Solute carrier family 22 member 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

References:

  1. Babu E, Takeda M, Narikawa S, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Sakthisekaran D, Endou H: Human organic anion transporters mediate the transport of tetracycline. Jpn J Pharmacol. 2002 Jan;88(1):69-76. Pubmed

2. Solute carrier family 22 member 8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

References:

  1. Babu E, Takeda M, Narikawa S, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Sakthisekaran D, Endou H: Human organic anion transporters mediate the transport of tetracycline. Jpn J Pharmacol. 2002 Jan;88(1):69-76. Pubmed

3. Solute carrier family 22 member 11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Babu E, Takeda M, Narikawa S, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Sakthisekaran D, Endou H: Human organic anion transporters mediate the transport of tetracycline. Jpn J Pharmacol. 2002 Jan;88(1):69-76. Pubmed

4. Solute carrier family 22 member 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 7 Q9Y694 Details

References:

  1. Babu E, Takeda M, Narikawa S, Kobayashi Y, Yamamoto T, Cha SH, Sekine T, Sakthisekaran D, Endou H: Human organic anion transporters mediate the transport of tetracycline. Jpn J Pharmacol. 2002 Jan;88(1):69-76. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13