Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo

Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold

(2022) Tianxiao Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural Optimization and Structure–Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant Mutants

(2022) Shulei Pan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors

(2021) Tianxiao Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation

(2021) Lin-Sheng Zhuo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of Larotrectinib in TRK Fusion–Positive Cancers in Adults and Children

(2018) Alexander Drilon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibiting TRK Proteins in Clinical Cancer Therapy

(2018) Allison Lange et al.   Cancers

Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application

(2018) Wei Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors

(2017) Chenzhou Hao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers

(2017) Miho J. Fuse et al.   MOLECULAR CANCER THERAPEUTICS

Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1)

(2017) Alexander Drilon et al.   Cancer Discovery

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion–Positive Solid Tumors

(2017) Alexander Drilon et al.   Cancer Discovery

What hides behind the MASC: clinical response and acquired resistance to entrectinib afterETV6-NTRK3identification in a mammary analogue secretory carcinoma (MASC)

(2016) A. Drilon et al.   ANNALS OF ONCOLOGY

TPX-0005, a novel ALK/ROS1/TRK inhibitor, effectively inhibited a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants

(2016) J.J. Cui et al.   EUROPEAN JOURNAL OF CANCER

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor

(2016) Maria Menichincheri et al.   JOURNAL OF MEDICINAL CHEMISTRY

Acquired Resistance to the TRK Inhibitor Entrectinib in Colorectal Cancer

(2015) M. Russo et al.   Cancer Discovery

An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101

(2015) R. C. Doebele et al.   Cancer Discovery

Functional characterization ofNTRK1mutations identified in melanoma

(2015) Claudia Miranda et al.   GENES CHROMOSOMES & CANCER

TRKing Down an Old Oncogene in a New Era of Targeted Therapy

(2014) Aria Vaishnavi et al.   Cancer Discovery

Infusion of BDNF into the nucleus accumbens of aged rats improves cognition and structural synaptic plasticity through PI3K-ILK-Akt signaling

(2012) Min Li et al.   BEHAVIOURAL BRAIN RESEARCH

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors

(2012) Tao Wang et al.   ACS Medicinal Chemistry Letters

Role and Relevance of TrkB Mutations and Expression in Non-Small Cell Lung Cancer

(2011) T. Harada et al.   CLINICAL CANCER RESEARCH

Dysregulated TRK signalling is a therapeutic target in CYLD defective tumours

(2011) N Rajan et al.   ONCOGENE

Functional Characterization of Human Cancer-Derived TRKB Mutations

(2011) Thomas R. Geiger et al.   PLoS One

Brain-Derived Neurotrophic Factor (BDNF) has Proliferative Effects on Neural Stem Cells through the Truncated TRK-B Receptor, MAP Kinase, AKT, and STAT-3 Signaling Pathways

(2009) Omedul Islam et al.   CURRENT NEUROVASCULAR RESEARCH

TrkA overexpression enhances growth and metastasis of breast cancer cells

(2009) C Lagadec et al.   ONCOGENE

Somatic mutations and germline sequence variants in the expressed tyrosine kinase genes of patients with de novo acute myeloid leukemia

(2008) M. H. Tomasson et al.   BLOOD

Frequent mutations in the neurotrophic tyrosine receptor kinase gene family in large cell neuroendocrine carcinoma of the lung

(2008) Antonio Marchetti et al.   HUMAN MUTATION