Selective Kv1.3 channel blocker as therapeutic for obesity and insulin resistance

No abstract is available for this paper.

• Publication year

  2013

• Venue

  Proceedings of the National Academy of Sciences of the United States of America

• Publication date

  2013-05-31

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1073/pnas.1221206110PMID 23729813PMCID PMC3683782
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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  2003cited by this paper
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  2003cited by this paper
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  1993cited by this paper
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  1968cited by this paper

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