matrix metalloproteinase inhibitors


Summary: Compounds that inhibit the enzyme activity or activation of MATRIX METALLOPROTEINASES.

Top Publications

  1. Xie X, Wan R, Liu Z. Recent Research Advances in Selective Matrix Metalloproteinase-13 Inhibitors as Anti-Osteoarthritis Agents. ChemMedChem. 2017;12:1157-1168 pubmed publisher
  2. Mohamed Ahmed A, Lockwood A, Li H, Bailly M, Khaw P, Brocchini S. An Ilomastat-CD Eye Drop Formulation to Treat Ocular Scarring. Invest Ophthalmol Vis Sci. 2017;58:3425-3431 pubmed publisher
    ..The purpose of this study was to develop a topical matrix metalloproteinase inhibitor preparation for antiscarring therapy...
  3. Shyu K. Serotonin 5-HT2B receptor in cardiac fibroblast contributes to cardiac hypertrophy: a new therapeutic target for heart failure?. Circ Res. 2009;104:1-3 pubmed publisher
  4. Drabsch Y, He S, Zhang L, Snaar Jagalska B, Ten Dijke P. Transforming growth factor-? signalling controls human breast cancer metastasis in a zebrafish xenograft model. Breast Cancer Res. 2013;15:R106 pubmed publisher
    ..The zebrafish-embryonic breast cancer xenograft model is applicable for the mechanistic understanding, screening and development of anti-TGF-? drugs for the treatment of metastatic breast cancer in a timely and cost-effective manner. ..
  5. Greene W, Burke T, Kaini R, Por E, Wang H. Polarized Secretion of Matrix Metalloproteinases and Their Inhibitors by Retinal Pigment Epithelium Derived from Induced Pluripotent Stem Cells During Wound Healing. J Ocul Pharmacol Ther. 2017;33:132-140 pubmed publisher
    ..After wounding, apical secretion of MMP-2 was higher compared to control. Apical secretion of all 4 TIMPs increased compared to control, while only TIMP-1 showed increased basolateral secretion compared to control. ..
  6. Chang Y, Chan Y, Chang W, Lin Y, Yang C, Su C, et al. Feedback regulation of ALDOA activates the HIF-1α/MMP9 axis to promote lung cancer progression. Cancer Lett. 2017;403:28-36 pubmed publisher
    ..The ALDOA-HIF-1α axis may provide a new therapeutic target for metastatic lung cancer treatment. ..
  7. Jain M, Harburn J, Gill J, Loadman P, Falconer R, Mooney C, et al. Rationalized Computer-Aided Design of Matrix-Metalloprotease-Selective Prodrugs. J Med Chem. 2017;60:4496-4502 pubmed publisher
    ..Proof of principle for this therapeutic approach was demonstrated in vitro against an aggressive human glioma model, with involvement of MMPs confirmed using pharmacological inhibition. ..
  8. Ellinghaus U, Cortini A, Pinder C, Le Friec G, Kemper C, Vyse T. Dysregulated CD46 shedding interferes with Th1-contraction in systemic lupus erythematosus. Eur J Immunol. 2017;47:1200-1210 pubmed publisher
    ..These data may deliver the first mechanistic explanation for the increased serum CD46 levels observed in SLE patients and indicate that targeting CD46-cleaving proteases could be a novel avenue to modulate Th1 responses. ..
  9. Gao S, Shen Y, Geng F, Li Y, Gao J. [Research progress on the animal models and treatment strategies of diabetic foot ulcer]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2017;46:97-105 pubmed

More Information


  1. Bendeck M, Irvin C, Reidy M. Inhibition of matrix metalloproteinase activity inhibits smooth muscle cell migration but not neointimal thickening after arterial injury. Circ Res. 1996;78:38-43 pubmed
    ..Thus, it appears that inhibiting SMC migration with MMP inhibitors is not sufficient to inhibit lesion growth, and lesion size eventually catches up to control via increased SMC replication. ..
  2. Scannevin R, Alexander R, Haarlander T, Burke S, Singer M, Huo C, et al. Discovery of a highly selective chemical inhibitor of matrix metalloproteinase-9 (MMP-9) that allosterically inhibits zymogen activation. J Biol Chem. 2017;292:17963-17974 pubmed publisher
    ..Targeting zymogen activation in this manner may also allow for pharmaceutical exploration of other enzymes previously viewed as intractable drug targets. ..
  3. Lingling J, Qianbing W. [Progress on matrix metalloproteinase inhibitors]. Hua Xi Kou Qiang Yi Xue Za Zhi. 2017;35:208-214 pubmed publisher
    ..This review summarizes progress on matrix metalloproteinase inhibitors (including chlorhexidine, ethylenediaminetetraacetic acid, quaternary ammonium salt, tetracycline ..
  4. Brilha S, Wysoczanski R, Whittington A, Friedland J, Porter J. Monocyte Adhesion, Migration, and Extracellular Matrix Breakdown Are Regulated by Integrin ?V?3 in Mycobacterium tuberculosis Infection. J Immunol. 2017;199:982-991 pubmed publisher
    ..This leads to increased monocyte recruitment and collagenase activity, which will drive inflammatory tissue damage. ..
  5. Klymenko Y, Kim O, Loughran E, Yang J, Lombard R, Alber M, et al. Cadherin composition and multicellular aggregate invasion in organotypic models of epithelial ovarian cancer intraperitoneal metastasis. Oncogene. 2017;36:5840-5851 pubmed publisher
    ..Collectively, our data emphasize the role of Ncad in intraperitoneal seeding of EOC and provide the rationale for future studies targeting Ncad in preclinical models of EOC metastasis. ..
  6. Gao Q, Wang Y, Hou J, Yao Q, Zhang J. Multiple receptor-ligand based pharmacophore modeling and molecular docking to screen the selective inhibitors of matrix metalloproteinase-9 from natural products. J Comput Aided Mol Des. 2017;31:625-641 pubmed publisher
    ..The found MMP-9 inhibitors of natural products could serve as the lead compounds for designing the new MMP-9 inhibitors by carrying out structural modifications in the future. ..
  7. Kenney M, Chwa M, Opbroek A, Brown D. Increased gelatinolytic activity in keratoconus keratocyte cultures. A correlation to an altered matrix metalloproteinase-2/tissue inhibitor of metalloproteinase ratio. Cornea. 1994;13:114-24 pubmed
    ..These data suggest that a possible alteration in the interaction between MMP-2 and TIMP may play a role in the increased gelatinolytic activity seen in keratoconus tissues. ..
  8. Liu H, Kenning M, Jobling A, McBrien N, Gentle A. Reduced Scleral TIMP-2 Expression Is Associated With Myopia Development: TIMP-2 Supplementation Stabilizes Scleral Biomarkers of Myopia and Limits Myopia Development. Invest Ophthalmol Vis Sci. 2017;58:1971-1981 pubmed publisher
    ..It follows that replenishment of this TIMP-2 significantly reduced the rate of both scleral collagen degradation and myopia development. ..
  9. Nelson A, Fingleton B, Rothenberg M, Matrisian L. Matrix metalloproteinases: biologic activity and clinical implications. J Clin Oncol. 2000;18:1135-49 pubmed
  10. Moz S, Aita A, Basso D, Ramonda R, Plebani M, Punzi L. Spondyloarthritis: Matrix Metalloproteinasesas Biomarkers of Pathogenesis and Response to Tumor Necrosis Factor (TNF) Inhibitors. Int J Mol Sci. 2017;18: pubmed publisher
    ..The current review focuses on MMPs' role in SpA pathogenesis, diagnosis and therapeutic implications. ..
  11. Chen Y, Peng W, Raffetto J, Khalil R. Matrix Metalloproteinases in Remodeling of Lower Extremity Veins and Chronic Venous Disease. Prog Mol Biol Transl Sci. 2017;147:267-299 pubmed publisher
    ..Modulation of endogenous tissue inhibitors of metalloproteinases (TIMPs), and exogenous synthetic MMP inhibitors may provide new approaches in the management of VVs. ..
  12. Zhang Y, Chen Q. Relationship between matrix metalloproteinases and the occurrence and development of ovarian cancer. Braz J Med Biol Res. 2017;50:e6104 pubmed publisher
    ..The investigation of MMP mechanism in ovarian cancer will facilitate the development of effective anti-tumor drugs, and thereby improve the survival rate of patients with ovarian cancer. ..
  13. Huang R, Liang G, Huang X, Zhang B, Zhou M, Liao Z, et al. Discovery of dehydroabietic acid sulfonamide based derivatives as selective matrix metalloproteinases inactivators that inhibit cell migration and proliferation. Eur J Med Chem. 2017;138:979-992 pubmed publisher
    ..Thus, we conclude that DHAA dipeptide derivatives containing the sulfonamide moiety may be the potential MMPs inhibitors with the ability to suppress cells migration. ..
  14. Nagase H. A personal journey with matrix metalloproteinases. Biol Chem. 2016;397:805-13 pubmed publisher
  15. Trojanek J. [Role of matrix metalloproteinases and tissue inhibitors of metalloproteinases in hypertension. Pathogenesis of hypertension and obesity]. Postepy Biochem. 2015;61:356-63 pubmed
    ..The fat tissue of obese people is in the state of low intensity chronic inflammation and undergoes continual process of remodeling. Obesity is one of the direct cause of hypertension. ..
  16. Nicolai E, Sinibaldi F, Sannino G, Lagana G, Basoli F, Licoccia S, et al. Omega-3 and Omega-6 Fatty Acids Act as Inhibitors of the Matrix Metalloproteinase-2 and Matrix Metalloproteinase-9 Activity. Protein J. 2017;36:278-285 pubmed publisher
    ..This observation is of interest since it assigns to these compounds a key role as MMPs inhibitors, and stimulates further study to better define their therapeutic potentialities in carious decay. ..
  17. Choi J, Fuerst R, Knapinska A, Taylor A, Smith L, Cao X, et al. Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors. J Med Chem. 2017;60:5816-5825 pubmed publisher
    ..These compounds exhibit at least 500-fold selectivity versus other MMPs. ..
  18. Iredale J, Benyon R, Pickering J, McCullen M, Northrop M, Pawley S, et al. Mechanisms of spontaneous resolution of rat liver fibrosis. Hepatic stellate cell apoptosis and reduced hepatic expression of metalloproteinase inhibitors. J Clin Invest. 1998;102:538-49 pubmed
  19. Wang S, Liu C, Liu X, He Y, Shen D, Luo Q, et al. Effects of matrix metalloproteinase inhibitor doxycycline and CD147 antagonist peptide-9 on gallbladder carcinoma cell lines. Tumour Biol. 2017;39:1010428317718192 pubmed publisher
    ..This study provides new information and tries to implement the design of adjuvant therapy method for gallbladder carcinoma...
  20. Kim J, Jeong Y, Lee E, Park J, Seo H, Kim H. Suppression of neuroinflammation by matrix metalloproteinase-8 inhibitor in aged normal and LRRK2 G2019S Parkinson's disease model mice challenged with lipopolysaccharide. Biochem Biophys Res Commun. 2017;493:879-886 pubmed publisher
    ..Collectively, the data suggested that M8I has a therapeutic potential in treating neurodegenerative diseases that are aggravated by systemic inflammation. ..
  21. Wang X, Liu J, Wu Q, Wu S, Hao D. The in vitro and in vivo effects of microRNA-133a on intervertebral disc destruction by targeting MMP9 in spinal tuberculosis. Life Sci. 2017;188:198-205 pubmed publisher
    ..MiR-133a could inhibit Collagen degradation by down-regulating MMP-9 expression to attenuate the destructive effects of spinal TB on intervertebral disc. ..
  22. Zucker S, Cao J. Selective matrix metalloproteinase (MMP) inhibitors in cancer therapy: ready for prime time?. Cancer Biol Ther. 2009;8:2371-3 pubmed
  23. Panezai J, Bergdahl E, Sundqvist K. T-cell regulation through a basic suppressive mechanism targeting low-density lipoprotein receptor-related protein 1. Immunology. 2017;152:308-327 pubmed publisher
    ..The disappearance of LRP1 from the cell surface may provide basic immunosuppression at the T-cell level. ..
  24. Mazzoni A, Angeloni V, Sartori N, Duarte S, Maravić T, Tjäderhane L, et al. Substantivity of Carbodiimide Inhibition on Dentinal Enzyme Activity over Time. J Dent Res. 2017;96:902-908 pubmed publisher
  25. DeLeon Pennell K, Meschiari C, Jung M, Lindsey M. Matrix Metalloproteinases in Myocardial Infarction and Heart Failure. Prog Mol Biol Transl Sci. 2017;147:75-100 pubmed publisher
    ..This chapter focuses on the role of MMPs post-MI, the efficiency of MMPs as biomarkers for MI or heart failure, and the future of MMPs and their cleavage products as targets for prevention of post-MI heart failure. ..
  26. Ricci S, Grandgirard D, Wenzel M, Braccini T, Salvatore P, Oggioni M, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014;14:726 pubmed publisher
    ..MMPs significantly contribute to brain damage associated with experimental MM. Inhibition of MMPs reduces intracranial complications in mice suffering from MM, representing a potential adjuvant strategy in MM post-infection sequelae. ..
  27. Caria C, Gotardo E, Santos P, Acedo S, de Morais T, Ribeiro M, et al. Extracellular matrix remodeling and matrix metalloproteinase inhibition in visceral adipose during weight cycling in mice. Exp Cell Res. 2017;359:431-440 pubmed publisher
    ..Our results suggest that MMPs inhibition could be an interesting target to improve adipose tissue inflammation during WL and to support weight cyclers. ..
  28. Sun C, Feng S, Cao Z, Bei J, Chen Q, Zhao W, et al. Up-Regulated Expression of Matrix Metalloproteinases in Endothelial Cells Mediates Platelet Microvesicle-Induced Angiogenesis. Cell Physiol Biochem. 2017;41:2319-2332 pubmed publisher
    ..The findings of our study indicate that PMVs promote angiogenesis by up-regulating MMP expression in ECs via mechanism extending beyond the direct delivery of angiogenic factors. ..