Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3

被引：33
|
作者：
Reiter, LA [1 ]
Mitchell, PG [1 ]
Martinelli, GJ [1 ]
Lopresti-Morrow, LL [1 ]
Yocum, SA [1 ]
Eskra, JD [1 ]
机构：
[1] Pfizer Inc, Global Res & Dev, Groton Labs, Groton, CT 06340 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 14期
关键词：
D O I：
10.1016/S0960-894X(03)00413-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Phosphinic acid-based inhibitors of MMP-13 have been investigated with the aim of identifying potent inhibitors with high selectivity versus MMP-1. Independent variation of the substituents on a P-1' phenethyl group and a P-2 benzyl group improved potencies in both cases around 3-fold over the unsubstituted parent. Combining improved P-1' and P-2 groups into a single molecule gave an inhibitor with a 4.5 nM IC50 against MMP-13 and which is 270-fold selective over MMP-1. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：2331 / 2336
页数：6
相关论文
共 50 条
  • [21] MMP-1、MMP-3和MMP-13在慢性睡眠剥夺所致颞下颌关节损伤中的变化
    吕晓伟
    吴高义
    何玉宏
    王培欢
    朱国雄
    现代生物医学进展, 2015, 15 (27) : 5212 - 5215
  • [22] Cyclosporine A Downregulates MMP-3 and MMP-13 Expression in Cultured Pterygium Fibroblasts
    Kim, Yeoun-Hee
    Jung, Jae-Chang
    Jung, Soon-Young
    Kim, Yong Il
    Lee, Kyoo Won
    Park, Young Jeung
    CORNEA, 2015, 34 (09) : 1137 - 1143
  • [23] 胃癌组织MMP-3及MMP-13蛋白的表达
    黄钢丁
    姜海行
    覃山羽
    黄振宁
    聂海明
    广东医学, 2007, (10) : 1631 - 1633
  • [24] MMP-3 mRNA and MMP-3 and MMP-1 proteins in bladder cancer: A comparison with clinicopathologic features and survival
    Nakopoulou, L
    Gakiopoulou, H
    Zervas, A
    Giannopoulou, I
    Constantinides, C
    Lazaris, AC
    Liapis, H
    Kyriakou, G
    Dimopoulos, C
    APPLIED IMMUNOHISTOCHEMISTRY & MOLECULAR MORPHOLOGY, 2001, 9 (02) : 130 - 137
  • [25] An improved collagen zymography approach for evaluating the collagenases MMP-1, MMP-8, and MMP-13
    Inanc, Seniz
    Keles, Didem
    Oktay, Gulgun
    BIOTECHNIQUES, 2017, 63 (04) : 174 - 180
  • [26] Matrix metalloproteinases MMP-1, MMP-2, and MMP-13 are overexpressed in primary nodular melanoma
    Zamolo, Gordana
    Grahovac, Maja
    Zauhar, Gordana
    Vucinic, Damir
    Kovac, Leo
    Brajenic, Nika
    Grahovac, Blazenka
    JOURNAL OF CUTANEOUS PATHOLOGY, 2020, 47 (02) : 139 - 145
  • [27] MMP-1、MMP-3、MMP-13在兔骨关节炎软骨及滑膜中的表达
    吕伟
    时剑辉
    崔巍
    单静
    中国卫生标准管理, 2015, 6 (23) : 191 - 192
  • [28] Icariin inhibits MMP-1, MMP-3 and MMP-13 expression through MAPK pathways in IL-1β-stimulated SW1353 chondrosarcoma cells
    Zeng, Li
    Rong, Xiao-Feng
    Li, Rong-Heng
    Wu, Xing-Ye
    MOLECULAR MEDICINE REPORTS, 2017, 15 (05) : 2853 - 2858
  • [29] Association of Promoter Polymorphism of MMP-1 rs1799750 and MMP-3 rs30254358 with circulating levels of MMP-1 and MMP-3 in patients with Rheumatoid Arthritis
    Aparna, Sagare
    Sucheta, Dandekar
    Anjali, Rajadhyaksha
    RESEARCH JOURNAL OF BIOTECHNOLOGY, 2022, 17 (03): : 111 - 118
  • [30] The association of MMP-1, MMP-3 and MMP-9 genotypes with prognosis of hepatocellular carcinoma
    Okamoto, K
    Mimura, K
    Murawaki, Y
    Yuasa, I
    JOURNAL OF HEPATOLOGY, 2004, 40 : 81 - 81
12345