Banner
Identification
Name Minocycline
Accession Number DB01017 (APRD00547)
Type small molecule
Groups approved
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
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms Not Available
Salts Not Available
Brand names
Name Company
Alti-Minocycline
Apo-Minocycline
Arestin
Dynacin
Gen-Minocycline
Klinomycin
Minociclina [INN-Spanish]
Minocin
Minocyclin
Minocycline HCl
Minocyclinum [INN-Latin]
Minocyn
Minomycin
Novo-Minocycline
Solodyn
Vectrin
First Prev Next Last
Brand mixtures Not Available
Categories
  • Anti-Bacterial Agents
  • Tetracyclines
CAS number 10118-90-8
Weight Average: 457.4764
Monoisotopic: 457.184900233
Chemical Formula C23H27N3O7
InChI Key InChIKey=DYKFCLLONBREIL-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
Plain Text
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
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For 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.
Pharmacodynamics Minocycline, 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 action Minocycline 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.
Absorption Rapidly absorbed from the gastrointestinal tract and absorption is not significantly impaired by ingestion of food or milk. Oral bioavailability is 100%.
Volume of distribution Not Available
Protein binding 55% to 76%
Metabolism Hepatic.
Route of elimination Not Available
Half life 11-22 hours
Clearance Not Available
Toxicity Minocycline 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
Pathway Name SMPDB ID
Smp00292 Minocycline Pathway SMP00292
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
Form Route Strength
Capsule Oral
Prices
Unit description Cost Unit
Minocin PAC 100 mg Kit Box 695.5 USD box
Minocin kit 100 mg combo 668.17 USD kit
Minocin kit 50 mg combo 334.78 USD kit
Minocin 100 mg vial 59.64 USD vial
Arestin 1 mg microsphere 30.0 USD each
Solodyn 135 mg 24 Hour tablet 24.89 USD tablet
Solodyn 45 mg 24 Hour tablet 24.89 USD tablet
Solodyn 65 mg 24 Hour tablet 24.89 USD tablet
Solodyn 90 mg 24 Hour tablet 24.89 USD tablet
Solodyn er 115 mg tablet 23.93 USD tablet
Solodyn er 135 mg tablet 23.93 USD tablet
Solodyn er 45 mg tablet 23.93 USD tablet
Solodyn er 65 mg tablet 23.93 USD tablet
Solodyn er 90 mg tablet 23.93 USD tablet
Minocycline hcl powder 21.0 USD g
Minocycline HCl 135 mg 24 Hour tablet 19.21 USD tablet
Minocycline HCl 45 mg 24 Hour tablet 19.21 USD tablet
Dynacin 100 mg tablet 13.37 USD tablet
Dynacin 75 mg tablet 13.12 USD tablet
Minocin 100 mg capsule 12.05 USD capsule
Minocin 100 mg pelletized cap 11.11 USD pellet
Dynacin 50 mg tablet 8.76 USD tablet
Dynacin 75 mg capsule 7.15 USD capsule
Minocycline hcl 100 mg tablet 6.15 USD tablet
Minocin 50 mg pelletized cap 5.56 USD pellet
Minocin 50 mg capsule 5.24 USD capsule
Minocycline hcl 75 mg tablet 5.14 USD tablet
Dynacin 50 mg capsule 3.85 USD capsule
Minocycline HCl 100 mg capsule 3.53 USD capsule
Minocycline hcl 50 mg tablet 3.5 USD tablet
Minocycline HCl 75 mg capsule 2.06 USD capsule
Minocycline 75 mg capsule 1.98 USD capsule
Minocycline HCl 50 mg capsule 1.77 USD capsule
Minocin 100 mg Capsule 1.34 USD capsule
Apo-Minocycline 100 mg Capsule 1.08 USD capsule
Minocycline 100 mg Capsule 1.08 USD capsule
Mylan-Minocycline 100 mg Capsule 1.08 USD capsule
Novo-Minocycline 100 mg Capsule 1.08 USD capsule
Pms-Minocycline 100 mg Capsule 1.08 USD capsule
Ratio-Minocycline 100 mg Capsule 1.08 USD capsule
Sandoz Minocycline 100 mg Capsule 1.08 USD capsule
Minocin 50 mg Capsule 0.69 USD capsule
Apo-Minocycline 50 mg Capsule 0.56 USD capsule
Minocycline 50 mg Capsule 0.56 USD capsule
Mylan-Minocycline 50 mg Capsule 0.56 USD capsule
Novo-Minocycline 50 mg Capsule 0.56 USD capsule
Pms-Minocycline 50 mg Capsule 0.56 USD capsule
Ratio-Minocycline 50 mg Capsule 0.56 USD capsule
Sandoz Minocycline 50 mg Capsule 0.56 USD capsule
First Prev Next Last
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
United States 7541347 2007-04-02 2027-04-02
United States 5908838 1998-02-19 2018-02-19
Canada 1330533 1994-07-05 2011-07-05
Properties
State solid
Experimental Properties
Property Value Source
water solubility 5.2E+004 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 0.05 SANGSTER (1993)
Predicted Properties
Property Value Source
water solubility 3.07e+00 g/l ALOGPS
logP -0.03 ALOGPS
logP -3.3 ChemAxon
logS -2.2 ALOGPS
pKa (strongest acidic) -2.3 ChemAxon
pKa (strongest basic) 8.25 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 9 ChemAxon
hydrogen donor count 5 ChemAxon
polar surface area 164.63 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 122.54 ChemAxon
polarizability 45.9 ChemAxon
References
Synthesis Reference Not Available
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
Resource Link
KEGG Drug D05045 Link_out
KEGG Compound C07225 Link_out
BindingDB 50046515 Link_out
ChEBI 50694 Link_out
ChEMBL 50694 Link_out
Therapeutic Targets Database DAP000405 Link_out
PharmGKB PA450519 Link_out
Drug Product Database 2242080 Link_out
RxList http://www.rxlist.com/cgi/generic/minocycline.htm Link_out
Drugs.com http://www.drugs.com/minocycline.html Link_out
PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/min1270.shtml Link_out
Wikipedia http://en.wikipedia.org/wiki/Minocycline Link_out
ATC Codes
  • A01AB23
  • J01AA08
AHFS Codes
  • 08:12.24
PDB Entries
FDA label show (3.02 MB)
MSDS show (73.6 KB)
Interactions
Drug Interactions
Drug Interaction
Acenocoumarol The tetracycline, minocycline, may increase the anticoagulant effect of acenocoumarol.
Acitretin Increased risk of intracranial hypertension.
Aluminium Formation of non-absorbable complexes
Amoxicillin Possible antagonism of action
Ampicillin Possible antagonism of action
Anisindione The tetracycline, minocycline, may increase the anticoagulant effect of anisindione.
Attapulgite Formation of non-absorbable complexes
Azlocillin Possible antagonism of action
Aztreonam Possible antagonism of action
Bacampicillin Possible antagonism of action
Bexarotene Tetracycline 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 Subsalicylate Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Calcium Acetate Calcium 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 Chloride Calcium 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.
Carbenicillin Possible antagonism of action
Clavulanate Possible antagonism of action
Cloxacillin Possible antagonism of action
Colesevelam Bile 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.
Cyclacillin Possible antagonism of action
Dicloxacillin Possible antagonism of action
Dicumarol The tetracycline, minocycline, may increase the anticoagulant effect of dicumarol.
Ethinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptive
Etretinate Increased risk of intracranial hypertension
Flucloxacillin Possible antagonism of action
Hetacillin Possible antagonism of action
Iron Formation of non-absorbable complexes
Iron Dextran Formation of non-absorbable complexes
Isotretinoin Increased risk of intracranial hypertension
Magnesium Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium salicylate Formation of non-absorbable complexes
Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Methicillin Acyl-Serine Possible antagonism of action
Methoxyflurane The tetracycline, minocycline, may increase the renal toxicity of methoxyflurane.
Mezlocillin Possible antagonism of action
Nafcillin Possible antagonism of action
Oxacillin Possible antagonism of action
Penicillin G Possible antagonism of action
Penicillin V Possible antagonism of action
Piperacillin Possible antagonism of action
Pivampicillin Possible antagonism of action
Pivmecillinam Possible antagonism of action
Tazobactam Possible antagonism of action
Ticarcillin Minocycline 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.
Tretinoin Minocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Trisalicylate-choline Formation of non-absorbable complexes
Warfarin The tetracycline, minocycline, may increase the anticoagulant effect of warfarin.
Zinc Formation 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

Pharmacological action: yes
Actions: inhibitor

The C-terminal tail plays a role in the affinity of the 30S P site for different tRNAs. Mutations that decrease this affinity are suppressed in the 70S ribosome

Organism class: bacterial
UniProt ID: P0A7X3 Link_out
Gene: rpsI
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: yes
Actions: inhibitor

Also functions as a rho-dependent antiterminator of rRNA transcription, increasing the synthesis of rRNA under conditions of excess protein, allowing a more rapid return to homeostasis. Binds directly to RNA polymerase

Organism class: bacterial
UniProt ID: P0A7V8 Link_out
Gene: rpsD
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: inhibitor

In prokaryotes, the 16S rRNA is essential for recognizing the 5' end of mRNA and hence positioning it correctly on the ribosome. The 16S rRNA has a characteristic secondary structure in which half of the nucleotides are base-paired. The 16S rRNA sequence has been highly conserved and is often used for evolutionary and species comparative analysis.

Gene Sequence: FASTA

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

Pharmacological action: unknown
Actions: modulator

Produced by activated macrophages, IL-1 stimulates thymocyte proliferation by inducing IL-2 release, B-cell maturation and proliferation, and fibroblast growth factor activity. IL-1 proteins are involved in the inflammatory response, being identified as endogenous pyrogens, and are reported to stimulate the release of prostaglandin and collagenase from synovial cells

Organism class: human
UniProt ID: P01584 Link_out
Gene: IL1B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: inhibitor
Organism class: human
UniProt ID: P09917 Link_out
Gene: ALOX5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: inhibitor

May play an essential role in local proteolysis of the extracellular matrix and in leukocyte migration. Could play a role in bone osteoclastic resorption. Cleaves KiSS1 at a Gly-|-Leu bond

Organism class: human
UniProt ID: P14780 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA

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

Pharmacological action: unknown
Actions: inhibitor

Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis, and induces permeabilization of blood vessels. Binds to the VEGFR1/Flt-1 and VEGFR2/Kdr receptors, heparan sulfate and heparin. Neuropilin-1 binds isoforms VEGF-165 and VEGF-145

Organism class: human
UniProt ID: P15692 Link_out
Gene: VEGF Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: negative modulator

Thiol protease that cleaves IL-1 beta between an Asp and an Ala, releasing the mature cytokine which is involved in a variety of inflammatory processes. Specifically inhibited by the cowpox virus Crma protein

Organism class: human
UniProt ID: P29466 Link_out
Gene: CASP1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: negative modulator

Involved in the activation cascade of caspases responsible for apoptosis execution. At the onset of apoptosis it proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp-|-Gly-217' bond. Cleaves and activates sterol regulatory element binding proteins (SREBPs) between the basic helix-loop- helix leucine zipper domain and the membrane attachment domain. Cleaves and activates caspase-6, -7 and -9. Involved in the cleavage of huntingtin

Organism class: human
UniProt ID: P42574 Link_out
Gene: CASP3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Pharmacological action: unknown
Actions: negative modulator

Plays a role in apoptosis. Suppression of the anti- apoptotic members or activation of the pro-apoptotic members of the Bcl-2 family leads to altered mitochondrial membrane permeability resulting in release of cytochrome c into the cytosol. Binding of cytochrome c to Apaf-1 triggers the activation of caspase-9, which then accelerates apoptosis by activating other caspases

Organism class: human
UniProt ID: P99999 Link_out
Gene: CYCS Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inhibitor
UniProt ID: Q4U2R8 Link_out
Gene: hROAT1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inhibitor

Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone- 3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA)

UniProt ID: Q8TCC7 Link_out
Gene: SLC22A8 Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inhibitor

Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds

UniProt ID: Q9NSA0 Link_out
Gene: SLC22A11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: inhibitor

Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulfate, allopurinol, 5-fluorouracil, paclitaxel, L-ascorbic acid, salicylate, ethotrexate, and alpha- ketoglutarate

UniProt ID: Q9Y694 Link_out
Gene: SLC22A7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19