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

Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation

(2021) Wei Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization

(2021) Mu-Chun Li et al.   EUROPEAN 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

Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective κ opioid receptor antagonists

(2020) Guangchao He et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and Structure–Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors

(2020) Yunxin Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation

(2020) Yongjie Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Developing Anticancer Drugs in Orphan Molecular Entities — A Paradigm under Construction

(2018) Fabrice André   NEW ENGLAND JOURNAL OF MEDICINE

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

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

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

(2018) Wei Yan 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

Targeting TRK family proteins in cancer

(2017) Yekaterina B. Khotskaya et al.   PHARMACOLOGY & THERAPEUTICS

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

Epidemiology and risk factors: intrahepatic cholangiocarcinoma

(2017) Amar Gupta et al.   HEPATOBILIARY SURGERY AND NUTRITION

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

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications

(2016) E. Ardini et al.   MOLECULAR CANCER THERAPEUTICS

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

The TPM3-NTRK1 rearrangement is a recurring event in colorectal carcinoma and is associated with tumor sensitivity to TRKA kinase inhibition

(2014) Elena Ardini et al.   Molecular Oncology

The genomic landscape of diffuse intrinsic pontine glioma and pediatric non-brainstem high-grade glioma

(2014) Gang Wu et al.   NATURE GENETICS

The landscape of kinase fusions in cancer

(2014) Nicolas Stransky et al.   Nature Communications

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

(2014) Aria Vaishnavi et al.   Cancer Discovery

ETV6-NTRK3 is a common chromosomal rearrangement in radiation-associated thyroid cancer

(2013) Rebecca J. Leeman-Neill et al.   CANCER

The integrated landscape of driver genomic alterations in glioblastoma

(2013) Veronique Frattini et al.   NATURE GENETICS

Oncogenic and drug-sensitive NTRK1 rearrangements in lung cancer

(2013) Aria Vaishnavi et al.   NATURE MEDICINE

The Crystal Structures of TrkA and TrkB Suggest Key Regions for Achieving Selective Inhibition

(2012) T. Bertrand et al.   JOURNAL OF MOLECULAR BIOLOGY

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

Lung Cancer: Epidemiology, Etiology, and Prevention

(2011) Charles S. Dela Cruz et al.   CLINICS IN CHEST MEDICINE

Characterization of a newly identified ETV6-NTRK3 fusion transcript in acute myeloid leukemia

(2011) Johanna M Kralik et al.   Diagnostic Pathology

102 Identification and preclinical characterization of NMS-P626, a potent, selective and orally bioavailable TrkA inhibitor with anti-tumor activity in a TrkA-dependent colorectal cancer

(2010) E. Ardini et al.   EJC SUPPLEMENTS

Rearrangements of NTRK1 gene in papillary thyroid carcinoma

(2009) A. Greco et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases

(2008) Tao Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA

(2007) Soong-Hoon Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS