Literature DB >> 28435530

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX.

John H Hutchinson1, Martin W Rowbottom1, David Lonergan1, Janice Darlington1, Pat Prodanovich1, Christopher D King1, Jilly F Evans1, Gretchen Bain1.   

Abstract

Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)methanamine 20 (hLOXL2 IC50 = 126 nM), was shown to be selective for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). Compound 20 is the first published small molecule inhibitor selective for LOXL2 over LOX.

Entities:  

Keywords:  (2-chloropyridin-4-yl)methanamine; LOXL2; fibrosis; inhibitor; lysyl oxidase-like 2

Year:  2017        PMID： 28435530      PMCID： PMC5392766          DOI： 10.1021/acsmedchemlett.7b00014

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  34 in total

1.  Lysyl oxidase-like 2 (LOXL2) oxidizes trimethylated lysine 4 in histone H3.

Authors:  Nicolás Herranz; Natàlia Dave; Alba Millanes-Romero; Laura Pascual-Reguant; Lluis Morey; Víctor M Díaz; Víctor Lórenz-Fonfría; Ricardo Gutierrez-Gallego; Celia Jerónimo; Ane Iturbide; Luciano Di Croce; Antonio García de Herreros; Sandra Peiró
Journal:  FEBS J       Date:  2016-10-30       Impact factor: 5.542

2.  Simtuzumab treatment of advanced liver fibrosis in HIV and HCV-infected adults: results of a 6-month open-label safety trial.

Authors:  Eric G Meissner; Mary McLaughlin; Lindsay Matthews; Ahmed M Gharib; Bradford J Wood; Elliot Levy; Ralph Sinkus; Kimmo Virtaneva; Dan Sturdevant; Craig Martens; Stephen F Porcella; Zachary D Goodman; Bittoo Kanwar; Robert P Myers; Mani Subramanian; Colleen Hadigan; Henry Masur; David E Kleiner; Theo Heller; Shyam Kottilil; Joseph A Kovacs; Caryn G Morse
Journal:  Liver Int       Date:  2016-07-06       Impact factor: 5.828

3.  A molecular role for lysyl oxidase-like 2 enzyme in snail regulation and tumor progression.

Authors:  Héctor Peinado; Maria Del Carmen Iglesias-de la Cruz; David Olmeda; Katalin Csiszar; Keith S K Fong; Sonia Vega; Maria Angela Nieto; Amparo Cano; Francisco Portillo
Journal:  EMBO J       Date:  2005-08-18       Impact factor: 11.598

4.  Allosteric inhibition of lysyl oxidase-like-2 impedes the development of a pathologic microenvironment.

Authors:  Vivian Barry-Hamilton; Rhyannon Spangler; Derek Marshall; Scott McCauley; Hector M Rodriguez; Miho Oyasu; Amanda Mikels; Maria Vaysberg; Haben Ghermazien; Carol Wai; Carlos A Garcia; Arleene C Velayo; Brett Jorgensen; Donna Biermann; Daniel Tsai; Jennifer Green; Shelly Zaffryar-Eilot; Alison Holzer; Scott Ogg; Dung Thai; Gera Neufeld; Peter Van Vlasselaer; Victoria Smith
Journal:  Nat Med       Date:  2010-09-05       Impact factor: 53.440

Review 5.  Lysine post-translational modifications of collagen.

Authors:  Mitsuo Yamauchi; Marnisa Sricholpech
Journal:  Essays Biochem       Date:  2012       Impact factor: 8.000

6.  Lysyl oxidase, extracellular matrix remodeling and cancer metastasis.

Authors:  Qian Xiao; Gaoxiang Ge
Journal:  Cancer Microenviron       Date:  2012-04-13

7.  Lysyl oxidase (lox) gene deficiency affects osteoblastic phenotype.

Authors:  N Pischon; J M Mäki; P Weisshaupt; N Heng; A H Palamakumbura; P N'Guessan; A Ding; R Radlanski; H Renz; T A L J J Bronckers; J Myllyharju; A M Kielbassa; B M Kleber; J-P Bernimoulin; P C Trackman
Journal:  Calcif Tissue Int       Date:  2009-05-21       Impact factor: 4.333

8.  Validated assays for human cytochrome P450 activities.

Authors:  Robert L Walsky; R Scott Obach
Journal:  Drug Metab Dispos       Date:  2004-06       Impact factor: 3.922

9.  Structural snapshots from the oxidative half-reaction of a copper amine oxidase: implications for O2 activation.

Authors:  Bryan J Johnson; Erik T Yukl; Valerie J Klema; Judith P Klinman; Carrie M Wilmot
Journal:  J Biol Chem       Date:  2013-08-12       Impact factor: 5.157

Review 10.  Pharmacological Treatment of Idiopathic Pulmonary Fibrosis: Current Approaches, Unsolved Issues, and Future Perspectives.

Authors:  Michael Kreuter; Francesco Bonella; Marlies Wijsenbeek; Toby M Maher; Paolo Spagnolo
Journal:  Biomed Res Int       Date:  2015-12-08       Impact factor: 3.411
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  15 in total

Review 1.  Matrix biomechanics and dynamics in pulmonary fibrosis.

Authors:  Andrew J Haak; Qi Tan; Daniel J Tschumperlin
Journal:  Matrix Biol       Date:  2017-12-21       Impact factor: 11.583

Review 2.  Mechano-therapeutics: Targeting Mechanical Signaling in Fibrosis and Tumor Stroma.

Authors:  Daniel J Tschumperlin; David Lagares
Journal:  Pharmacol Ther       Date:  2020-05-11       Impact factor: 12.310

3.  Mass Spectrometry-Based Disulfide Mapping of Lysyl Oxidase-like 2.

Authors:  Alex A Meier; Eden P Go; Hee-Jung Moon; Heather Desaire; Minae Mure
Journal:  Int J Mol Sci       Date:  2022-05-24       Impact factor: 6.208

4.  LOXL2 small molecule inhibitor restrains malignant transformation of cervical cancer cells by repressing LOXL2-induced epithelial-mesenchymal transition (EMT).

Authors:  Ting Peng; Shitong Lin; Yifan Meng; Peipei Gao; Ping Wu; Wenhua Zhi; Wencheng Ding; Canhui Cao; Peng Wu
Journal:  Cell Cycle       Date:  2022-05-11       Impact factor: 5.173

5.  Proteolytic processing of lysyl oxidase-like-2 in the extracellular matrix is required for crosslinking of basement membrane collagen IV.

Authors:  Alberto J López-Jiménez; Trayambak Basak; Roberto M Vanacore
Journal:  J Biol Chem       Date:  2017-09-01       Impact factor: 5.157

Review 6.  Periostin and its interacting proteins in the construction of extracellular architectures.

Authors:  Isao Kii; Harumi Ito
Journal:  Cell Mol Life Sci       Date:  2017-09-08       Impact factor: 9.261

Review 7.  Magnetic-Assisted Treatment of Liver Fibrosis.

Authors:  Kateryna Levada; Alexander Omelyanchik; Valeria Rodionova; Ralf Weiskirchen; Matthias Bartneck
Journal:  Cells       Date:  2019-10-19       Impact factor: 6.600

8.  Cu(I)- and Pd(0)-Catalyzed Arylation of Oxadiamines with Fluorinated Halogenobenzenes: Comparison of Efficiency.

Authors:  Maria S Lyakhovich; Alexei D Averin; Olga K Grigorova; Vitaly A Roznyatovsky; Olga A Maloshitskaya; Irina P Beletskaya
Journal:  Molecules       Date:  2020-02-28       Impact factor: 4.411

9.  Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.

Authors:  Leo Leung; Dan Niculescu-Duvaz; Deborah Smithen; Filipa Lopes; Cedric Callens; Robert McLeary; Grazia Saturno; Lawrence Davies; Mohammed Aljarah; Michael Brown; Louise Johnson; Alfonso Zambon; Tim Chambers; Delphine Ménard; Natasha Bayliss; Ruth Knight; Laura Fish; Rae Lawrence; Mairi Challinor; HaoRan Tang; Richard Marais; Caroline Springer
Journal:  J Med Chem       Date:  2019-05-23       Impact factor: 7.446

10.  Targeting lysyl oxidase (LOX) overcomes chemotherapy resistance in triple negative breast cancer.

Authors:  Ozge Saatci; Aysegul Kaymak; Umar Raza; Pelin G Ersan; Ozge Akbulut; Carolyn E Banister; Vitali Sikirzhytski; Unal Metin Tokat; Gamze Aykut; Suhail A Ansari; Hayriye Tatli Dogan; Mehmet Dogan; Pouria Jandaghi; Aynur Isik; Fatma Gundogdu; Kemal Kosemehmetoglu; Omer Dizdar; Sercan Aksoy; Aytekin Akyol; Aysegul Uner; Phillip J Buckhaults; Yasser Riazalhosseini; Ozgur Sahin
Journal:  Nat Commun       Date:  2020-05-15       Impact factor: 14.919
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