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Literature summary for 3.4.24.B4 extracted from

  • Li, J.J.; Nahra, J.; Johnson, A.R.; Bunker, A.; OBrien, P.; Yue, W.S.; Ortwine, D.F.; Man, C.F.; Baragi, V.; Kilgore, K.; Dyer, R.D.; Han, H.K.
    Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis (2008), J. Med. Chem., 51, 835-841.
    View publication on PubMed
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Application

Application Comment Organism
medicine orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. Two series, quinazolinones and pyrido[3,4-d]pyrimidin-4-ones, that are potent and specific MMP-13 inhibitors, some of which are orally bioavailable. These specific MMP-13 inhibitors, occupying the unique S1'-specificity pocket, do not bind to the Zn2+ ion, effectively preventing cartilage damage in animal models of osteoarthritis without inducing musculoskeletal side effects when given at extremely high doses to rats Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
additional information orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. Two series, quinazolinones and pyrido[3,4-d]pyrimidin-4-ones, that are potent and specific MMP-13 inhibitors, some of which are orally bioavailable. These specific MMP-13 inhibitors, occupying the unique S1'-specificity pocket, do not bind to the Zn2+ ion, effectively preventing cartilage damage in animal models of osteoarthritis without inducing musculoskeletal side effects when given at extremely high doses to rats Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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