Abstract:
INTRODUCTION:Tropomyosin receptor kinases (TrkA/B/C) play crucial roles in the development and maintenance of the nervous system, and aberrant expression of Trk has been implicated in neurological disorders as well as neural and non-neural neoplasms. Patent activity encompassing Trk inhibitors has grown substantially over the last 6 years, recognized by a rise in the number of pharmaceutical entrants to the field and the escalation of novel inhibitor chemotypes. Area covered: In Part I of this two part review, a biological and structural overview of Trk is provided in the context of Trk as a therapeutic target for cancer and pain, followed by the report of recent patent literature claiming small molecule inhibitors of Trk family kinases or which describe inhibitors developed for other kinase targets but include noteworthy Trk inhibition/application. The discussion of the patent literature continues in Part II of this review, which includes an in-depth view of the current clinical applications of Trk inhibitors. Expert opinion: Substantial synthetic efforts in Trk inhibitor development has propagated numerous and diverse inhibitor chemotypes, including TrkA-specific inhibitors. While many novel Trk inhibitors remain the original progeny of Trk-specific development programs, kinase inhibitors initially developed for other kinases have also been successfully repositioned for Trk.
journal_name
Expert Opin Ther Patjournal_title
Expert opinion on therapeutic patentsauthors
Bailey JJ,Schirrmacher R,Farrell K,Bernard-Gauthier Vdoi
10.1080/13543776.2017.1297796subject
Has Abstractpub_date
2017-06-01 00:00:00pages
733-751issue
6eissn
1354-3776issn
1744-7674journal_volume
27pub_type
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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更新日期:2009-01-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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更新日期:2011-02-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
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doi:10.1517/13543776.2013.743993
更新日期:2013-02-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1080/13543776.2020.1708900
更新日期:2020-02-01 00:00:00
abstract:INTRODUCTION:Neuropeptide S (NPS) is a 20-residue peptide and endogenous ligand of the NPS receptor (NPSR). This receptor was a formerly orphan GPCR whose activation increases calcium and cyclic adenosine monophosphate levels. The NPS/NPSR system is expressed in several brain regions where it controls important biologi...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1080/13543776.2017.1254195
更新日期:2017-03-01 00:00:00
abstract:INTRODUCTION:Around 3% of the world population is infected with HCV, with 3 - 4 million newly infected subjects added to this reservoir every year. At least 10% of these people will develop liver cirrhosis or cancer over time, while no approved vaccine against HCV infection is available to date. AREAS COVERED:This pap...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1517/13543776.2011.630662
更新日期:2011-12-01 00:00:00
abstract:INTRODUCTION:Transglutaminases (TGases) are a class of enzymes that play multifunctional roles. Their protein-crosslinking activity has been linked to fibrosis and Huntington's disease, their glutamine deamidation activity has been related to celiac disease and their GTP-binding activity has been implicated in cancer. ...
journal_title:Expert opinion on therapeutic patents
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abstract:INTRODUCTION:TANK-binding kinase 1 (TBK1) is a noncanonical IκB kinase family member that regulates the innate immune response. Misregulation of TBK1 activity can promote inflammatory disorders and oncogenesis; therefore, TBK1 inhibitors are considered a promising therapy for inflammation and cancer. AREAS COVERED:In ...
journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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