Toll-like receptor agonists: a patent review (2011 - 2013)

Hussein, Waleed M., Liu, Tzu-Yu, Skwarczynski, Mariusz and Toth, Istvan (2014) Toll-like receptor agonists: a patent review (2011 - 2013). Expert Opinion on Therapeutic Patents, 24 4: 453-470. doi:10.1517/13543776.2014.880691

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Author Hussein, Waleed M.
Liu, Tzu-Yu
Skwarczynski, Mariusz
Toth, Istvan
Title Toll-like receptor agonists: a patent review (2011 - 2013)
Journal name Expert Opinion on Therapeutic Patents   Check publisher's open access policy
ISSN 1354-3776
Publication date 2014-04-01
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1517/13543776.2014.880691
Volume 24
Issue 4
Start page 453
End page 470
Total pages 18
Place of publication London, United Kingdom
Publisher Informa Healthcare
Language eng
Formatted abstract
Introduction: Toll-like receptors (TLRs) are a crucial part of the innate immunity and present the first line of defense against pathogens. In humans, there are ten TLRs, with TLR3, 7, 8 and 9 located in intracellular vesicles and the remaining expressed on the cell surface. These transmembrane protein receptors recognize a wide range of pathogen components. A large number of TLR agonists, either derived from pathogen components or modified synthetic molecules, were developed and investigated for their ability to stimulate an immune response.

Areas covered: This review includes an updated summary (2011 – 2013) of TLR agonists that have been published in patent applications and/or progressed to clinical studies, with an emphasis on their chemical structure, immune response, prophylactic and therapeutic outcomes.

Expert opinion: A number of factors have contributed to the design and development of TLR agonists such as solving the crystal structures of TLR bound to their ligands, improvements in our understanding of the signaling pathway activated after TLR stimulation and the identification of the native ligands of all human TLRs. Some of the TLR agonists have been approved for human use by the FDA while others have reached clinical studies in Phases I, II and III. Generally, immunotherapy based on TLR agonists is very promising for the prevention and/or treatment of several disorders including cancer, allergy and microbial infections. However, many TLR agonists were withdrawn from further studies as they either lacked efficacy or caused serious side effects.
Keyword Adjuvant
Clinical study
Immune response
Innate immunity
Toll-like receptor
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Posted online on January 24, 2014

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2015 Collection
School of Chemistry and Molecular Biosciences
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Citation counts: TR Web of Science Citation Count  Cited 17 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 19 times in Scopus Article | Citations
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Created: Fri, 14 Feb 2014, 20:29:13 EST by Mrs Louise Nimwegen on behalf of School of Chemistry & Molecular Biosciences