4wk7 › Citations

Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.

Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR
J Med Chem 57 10476-85 (2014)
Related entries: 4wke, 4wki

Cited: 18 times
EuropePMC logo PMID: 25415648

Abstract

A disintegrin and metalloproteinase with thrombospondin motifs-4 (ADAMTS-4) and ADAMTS-5 are zinc metalloproteases commonly referred to as aggrecanase-1 and aggrecanase-2, respectively. These enzymes are involved in the degradation of aggrecan, a key component of cartilage. Inhibitors of these enzymes could be potential osteoarthritis (OA) therapies. A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were identified from a screening campaign and optimized through structure-based drug design to give hydantoin 13. Hydantoin 13 had excellent selectivity over other zinc metalloproteases such as TACE, MMP2, MMP3, MMP13, and MMP14. The compound also produced efficacy in both a chemically induced and surgical model of OA in rats.

Reviews - 4wk7 mentioned but not cited (1)

  1. Targeting Aggrecanases for Osteoarthritis Therapy: From Zinc Chelation to Exosite Inhibition. Cuffaro D, Ciccone L, Rossello A, Nuti E, Santamaria S. J Med Chem 65 13505-13532 (2022)

Articles - 4wk7 mentioned but not cited (7)

  1. Crystal structure and substrate-induced activation of ADAMTS13. Petri A, Kim HJ, Xu Y, de Groot R, Li C, Vandenbulcke A, Vanhoorelbeke K, Emsley J, Crawley JTB. Nat Commun 10 3781 (2019)
  2. ADAMTS13 and von Willebrand factor interactions. Zander CB, Cao W, Zheng XL. Curr Opin Hematol 22 452-459 (2015)
  3. Proteomic discovery of substrates of the cardiovascular protease ADAMTS7. Colige A, Monseur C, Crawley JTB, Santamaria S, de Groot R. J Biol Chem 294 8037-8045 (2019)
  4. Study on the potential active components and molecular mechanism of Xiao Huoluo Pills in the treatment of cartilage degeneration of knee osteoarthritis based on bioinformatics analysis and molecular docking technology. Chen W, Lin T, He Q, Yang P, Zhang G, Huang F, Wang Z, Peng H, Li B, Liang D, Wang H. J Orthop Surg Res 16 460 (2021)
  5. Identification of biomarkers of acne based on transcriptome analysis and combined with network pharmacology to explore the therapeutic mechanism of Jinhuang ointment. Li M, Gao X, Miao T, Sun H. Medicine (Baltimore) 102 e35642 (2023)
  6. Network Pharmacology and Experimental Verification Reveal the Regulatory Mechanism of Chuanbeimu in Treating Chronic Obstructive Pulmonary Disease. Xian M, Xu J, Zheng Y, Zhang L, Zhao J, Chen J, Li S, Lin L, Zhong Y, Yang Z, Xie T, Huang L, Ding Y. Int J Chron Obstruct Pulmon Dis 19 799-813 (2024)
  7. Mechanisms underlying the therapeutic effects of 4-octyl itaconate in treating sepsis based on network pharmacology and molecular docking. Chen M, Su W, Chen F, Lai T, Liu Y, Yu D. Front Genet 13 1056405 (2022)


Reviews citing this publication (1)

  1. Vitamin K-Dependent Proteins in Skeletal Development and Disease. Stock M, Schett G. Int J Mol Sci 22 9328 (2021)

Articles citing this publication (9)

  1. Therapeutic effects of an anti-ADAMTS-5 antibody on joint damage and mechanical allodynia in a murine model of osteoarthritis. Miller RE, Tran PB, Ishihara S, Larkin J, Malfait AM. Osteoarthritis Cartilage 24 299-306 (2016)
  2. Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT). Ding Y, O'Keefe H, DeLorey JL, Israel DI, Messer JA, Chiu CH, Skinner SR, Matico RE, Murray-Thompson MF, Li F, Clark MA, Cuozzo JW, Arico-Muendel C, Morgan BA. ACS Med Chem Lett 6 888-893 (2015)
  3. Identification of differentially expressed microRNAs in knee anterior cruciate ligament tissues surgically removed from patients with osteoarthritis. Li B, Bai L, Shen P, Sun Y, Chen Z, Wen Y. Int J Mol Med 40 1105-1113 (2017)
  4. Coronary Disease Association With ADAMTS7 Is Due to Protease Activity. Mizoguchi T, MacDonald BT, Bhandary B, Popp NR, Laprise D, Arduini A, Lai D, Zhu QM, Xing Y, Kaushik VK, Kathiresan S, Ellinor PT. Circ Res 129 458-470 (2021)
  5. Colony housing promotes structural and functional changes during surgically induced osteoarthritis in rats. Brenneis C, Menges S, Westhof A, Lindemann S, Thudium CS, Kleinschmidt-Doerr K. Osteoarthr Cartil Open 2 100100 (2020)
  6. PLXNC1 interference alleviates the inflammatory injury, apoptosis and extracellular matrix degradation of IL-1β-exposed chondrocytes via suppressing GRP78 expression. Meng N, Mao L, Jiang Q, Yuan J, Liu L, Wang L. J Orthop Surg Res 18 784 (2023)
  7. BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor. Meibom D, Wasnaire P, Beyer K, Broehl A, Cancho-Grande Y, Elowe N, Henninger K, Johannes S, Jungmann N, Krainz T, Lindner N, Maassen S, MacDonald B, Menshykau D, Mittendorf J, Sanchez G, Schaefer M, Stefan E, Torge A, Xing Y, Zubov D. J Med Chem 67 2907-2940 (2024)
  8. Discovery of Isoindoline Amide Derivatives as Potent and Orally Bioavailable ADAMTS-4/5 Inhibitors for the Treatment of Osteoarthritis. Zhao P, Liu D, Song C, Li D, Zhang X, Horecny I, Zhang F, Yan Y, Zhuang L, Li J, Liu S, Mao Y, Feng J, Liu J, Tao W. ACS Pharmacol Transl Sci 5 458-467 (2022)
  9. Network pharmacology and bioinformatics were used to construct a prognostic model and immunoassay of core target genes in the combination of quercetin and kaempferol in the treatment of colorectal cancer. Gu C, Tang L, Hao Y, Dong S, Shen J, Xie F, Han Z, Luo W, He J, Yu L. J Cancer 14 1956-1980 (2023)


Quick links