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Advances in kinase targeting : current clinical use and clinical trials

Rask-Andersen, Mathias (author)
Uppsala universitet,Funktionell farmakologi
Zhang, Jin (author)
Uppsala universitet,Umeå universitet,Kemiska institutionen,Funktionell farmakologi
Fabbro, Doriano (author)
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Schiöth, Helgi B (author)
Uppsala universitet,Funktionell farmakologi
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 (creator_code:org_t)
Elsevier BV, 2014
2014
English.
In: TIPS - Trends in Pharmacological Sciences. - : Elsevier BV. - 0165-6147 .- 1873-3735. ; 35:11, s. 60-76
  • Research review (peer-reviewed)
Abstract Subject headings
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  • Phosphotransferases, also known as kinases, are the most intensively studied protein drug target category in current pharmacological research, as evidenced by the vast number of kinase-targeting agents enrolled in active clinical trials. This development has emerged following the great success of small-molecule, orally available protein kinase inhibitors for the treatment of cancer, starting with the introduction of imatinib (Gleevec (R)) in 2003. The pharmacological utility of kinase-targeting has expanded to include treatment of inflammatory diseases, and rapid development is ongoing for kinase-targeted therapies in a broad array of indications in ophthalmology, analgesia, central nervous system (CNS) disorders, and the complications of diabetes, osteoporosis, and otology. In this review we highlight specifically the kinase drug targets and kinase-targeting agents being explored in current clinical trials. This analysis is based on a recent estimate of all established and clinical trial drug mechanisms of action, utilizing private and public databases to create an extensive dataset detailing aspects of more than 3000 approved and experimental drugs.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Neurovetenskaper (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Neurosciences (hsv//eng)

Keyword

clinical trials
phosphotransferase
drug targets
protein kinase
serine/threonine-protein kinase
rosine-protein kinase

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Zhang, Jin
Fabbro, Doriano
Schiöth, Helgi B
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MEDICAL AND HEALTH SCIENCES
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Umeå University
Uppsala University

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