NKRT inhibitors



The NTRK,  neurotrophin receptor tyrosine kinase gene encodes the tropomyosin receptor kinase.



Tropomyosin receptor kinase B (TrkB), also known as tyrosine receptor kinase B, is a protein that in humans is encoded by the NTRK2 gene.



TrkB is a receptor for brain-derived neurotrophic factor (BDNF).



Gene location chromosome 9 for NTRK2Genomic location for NTRK2.



Tropomyosin receptor kinase B is the high affinity receptor for several neurotrophins.



Neurotropins are small protein growth factors that induce the survival and differentiation of distinct cell populations. 



The neurotrophins that activate Tropomyosin receptor kinase B  are: BDNF (Brain Derived Neurotrophic Factor), neurotrophin-4 (NT-4), and neurotrophin-3 (NT-3).



TrkB mediates the multiple effects of neurotrophic factors: neuronal differentiation and survival. 



The TrkB receptor is part of the large family of receptor tyrosine kinases: an enzyme which is capable of adding a phosphate group to certain tyrosines on target proteins, or substrates.



A receptor tyrosine kinase is located at the cellular membrane, and is activated by binding of a ligand to the receptor’s extracellular domain. 



TrkB is part of a sub-family of protein kinases which includes also TrkA and TrkC. 



The Trk family has a role in human cancers because of the identification of NTRK1 (TrkA), NTRK2 (TrkB) and NTRK3 (TrkC) gene fusions and other oncogenic alterations in a number of tumors.



Trk inhibitors have shown early promise in shrinking human tumors.



Entrectinib has potential antitumor activity. 



Entrectinib is a selective pan-trk receptor tyrosine kinase inhibitor (TKI) targeting gene fusions in trkA, trkB, and trkC.



TRK Inhibition-related adverse effects include: weight gain, dizziness, and withdrawal pain .




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