Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021‏ - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - Signal transduction and …, 2022‏ - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Entrectinib in patients with advanced or metastatic NTRK fusion-positive solid tumours: integrated analysis of three phase 1–2 trials

RC Doebele, A Drilon, L Paz-Ares, S Siena… - The lancet …, 2020‏ - thelancet.com
Background Entrectinib is a potent inhibitor of tropomyosin receptor kinase (TRK) A, B, and
C, which has been shown to have anti-tumour activity against NTRK gene fusion-positive …

NTRK fusion-positive cancers and TRK inhibitor therapy

E Cocco, M Scaltriti, A Drilon - Nature reviews Clinical oncology, 2018‏ - nature.com
N TRK gene fusions involving either NTRK1, NTRK2 or NTRK3 (encoding the neurotrophin
receptors TRKA, TRKB and TRKC, respectively) are oncogenic drivers of various adult and …

[HTML][HTML] NTRK fusion detection across multiple assays and 33,997 cases: diagnostic implications and pitfalls

JP Solomon, I Linkov, A Rosado, K Mullaney… - Modern pathology, 2020‏ - Elsevier
With the FDA approval of larotrectinib, NTRK fusion assessment has recently become a
standard part of management for patients with locally advanced or metastatic cancers …

Larotrectinib for paediatric solid tumours harbouring NTRK gene fusions: phase 1 results from a multicentre, open-label, phase 1/2 study

TW Laetsch, SG DuBois, L Mascarenhas… - The lancet …, 2018‏ - thelancet.com
Background Gene fusions involving NTRK1, NTRK2, or NTRK3 (TRK fusions) are found in a
broad range of paediatric and adult malignancies. Larotrectinib, a highly selective small …

The role of brain derived neurotrophic factor in central nervous system

Y Li, F Li, D Qin, H Chen, J Wang, J Wang… - Frontiers in Aging …, 2022‏ - frontiersin.org
Brain derived neurotrophic factor (BDNF) has multiple biological functions which are
mediated by the activation of two receptors, tropomyosin receptor kinase B (TrkB) receptor …

[HTML][HTML] NTRK gene fusions as novel targets of cancer therapy across multiple tumour types

A Amatu, A Sartore-Bianchi, S Siena - ESMO open, 2016‏ - Elsevier
The tropomyosin receptor kinase (Trk) receptor family comprises 3 transmembrane proteins
referred to as Trk A, B and C (TrkA, TrkB and TrkC) receptors that are encoded by the …

[HTML][HTML] Tropomyosin receptor kinase (TRK) biology and the role of NTRK gene fusions in cancer

A Amatu, A Sartore-Bianchi, K Bencardino… - Annals of …, 2019‏ - Elsevier
The tropomyosin receptor kinase (TRK) family of receptor tyrosine kinases are encoded by
NTRK genes and have a role in the development and normal functioning of the nervous …

Neurobiology of local and intercellular BDNF signaling

M Sasi, B Vignoli, M Canossa, R Blum - Pflügers Archiv-European Journal …, 2017‏ - Springer
Brain-derived neurotrophic factor (BDNF) is a member of the neurotrophin family of secreted
proteins. Signaling cascades induced by BDNF and its receptor, the receptor tyrosine kinase …