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Research ArticleInflammation, Immunopharmacology, and Asthma

Inhibition of Toll-Like Receptor-Mediated Inflammation In Vitro and In Vivo by a Novel Benzoxaborole

Chen Dong, Holly Sexton, Ana Gertrudes, Tsutomu Akama, Shamra Martin, Charlotte Virtucio, Chiao-Wen Chen, Xiaoqin Fan, Anne Wu, Wei Bu, Liang Liu, Lisa Feng, Kurt Jarnagin and Yvonne R. Freund
Journal of Pharmacology and Experimental Therapeutics February 2013, 344 (2) 436-446; DOI: https://doi.org/10.1124/jpet.112.200030
Chen Dong
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Holly Sexton
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Ana Gertrudes
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Tsutomu Akama
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Shamra Martin
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Charlotte Virtucio
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Chiao-Wen Chen
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Xiaoqin Fan
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Anne Wu
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Wei Bu
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Liang Liu
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Lisa Feng
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Kurt Jarnagin
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Yvonne R. Freund
Anacor Pharmaceuticals, Inc. Palo Alto, California
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Abstract

Pro-inflammatory cytokines play a critical role in the development of autoimmune and inflammatory diseases. Targeting the cytokine environment has proven efficient for averting inflammation. In this study, we reported that 6-[4-(aminomethyl)-2-chlorophenoxyl]benzo[c][1,2]oxaborol-1(3H)-ol (AN3485), a benzoxaborole analog, inhibited TLR2-, TLR3-, TLR4-, and TLR5-mediated TNF-α, IL-1β, and IL-6 release from human PBMCs and isolated monocytes with IC50 values ranging from 18 to 580 nM, and the inhibition was mediated at the transcriptional level. Topical administration of AN3485 significantly reduced PMA-induced contact dermatitis and oxazolone-induced delayed-type hypersensitivity in mice, indicating its capability of penetrating skin and potential topical application in skin inflammation. Oral administration of AN3485 showed dose-dependent suppression of LPS-induced TNF-α and IL-6 production in mice with an ED90 of 30 mg/kg. Oral AN3485, 35 mg/kg, twice a day, suppressed collagen-induced arthritis in mice over a 20-day period. The potent anti-inflammatory activity in in vitro and in vivo disease models makes AN3485 an attractive therapeutic lead for a variety of cutaneous and systemic inflammatory diseases.

Footnotes

  • dx.doi.org/10.1124/jpet.112.200030.

  • ↵Embedded ImageThis article has supplemental material available at jpet.aspetjournals.org.

  • Received September 20, 2012.
  • Accepted November 27, 2012.
  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 344 (2)
Journal of Pharmacology and Experimental Therapeutics
Vol. 344, Issue 2
1 Feb 2013
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Research ArticleInflammation, Immunopharmacology, and Asthma

AN3485 Inhibits TLR-Mediated Inflammation In Vitro and In Vivo

Chen Dong, Holly Sexton, Ana Gertrudes, Tsutomu Akama, Shamra Martin, Charlotte Virtucio, Chiao-Wen Chen, Xiaoqin Fan, Anne Wu, Wei Bu, Liang Liu, Lisa Feng, Kurt Jarnagin and Yvonne R. Freund
Journal of Pharmacology and Experimental Therapeutics February 1, 2013, 344 (2) 436-446; DOI: https://doi.org/10.1124/jpet.112.200030

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Research ArticleInflammation, Immunopharmacology, and Asthma

AN3485 Inhibits TLR-Mediated Inflammation In Vitro and In Vivo

Chen Dong, Holly Sexton, Ana Gertrudes, Tsutomu Akama, Shamra Martin, Charlotte Virtucio, Chiao-Wen Chen, Xiaoqin Fan, Anne Wu, Wei Bu, Liang Liu, Lisa Feng, Kurt Jarnagin and Yvonne R. Freund
Journal of Pharmacology and Experimental Therapeutics February 1, 2013, 344 (2) 436-446; DOI: https://doi.org/10.1124/jpet.112.200030
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