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

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

Designing Out PXR Activity on Drug Discovery Projects: A Review of Structure-Based Methods, Empirical and Computational Approaches

(2021) Adrian Hall et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer

(2021) Zongliang Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects

(2021) Tong Li et al.   BIOORGANIC & 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

Development of small-molecule tropomyosin receptor kinase (TRK) inhibitors for NTRK fusion cancers

(2020) Tingting Jiang et al.   Acta Pharmaceutica Sinica B

Fragment Linking Strategies for Structure-Based Drug Design

(2020) Alexandre Bancet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histology-agnostic drug development — considering issues beyond the tissue

(2020) Roberto Carmagnani Pestana et al.   Nature Reviews Clinical Oncology

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

TRK xDFG mutations trigger a sensitivity switch from type I to II kinase inhibitors

(2020) Emiliano Cocco et al.   Cancer Discovery

Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors

(2020) Minghao Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants

(2020) Beilei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models

(2019) Ryohei Katayama et al.   Nature Communications

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

(2019) Robert C Doebele et al.   LANCET ONCOLOGY

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

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

Structure-Based Drug Design Strategies and Challenges

(2018) Xin Wang et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations

(2018) Alexander Drilon et al.   Cancer Discovery

NTRK fusion-positive cancers and TRK inhibitor therapy

(2018) Emiliano Cocco et al.   Nature Reviews Clinical Oncology

Recent Advances in Structure-Based Drug Design Targeting Class A G Protein-Coupled Receptors Utilizing Crystal Structures and Computational Simulations

(2017) Yoonji Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain

(2016) Sarah E. Skerratt et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

(2014) Aria Vaishnavi et al.   Cancer Discovery

Identification of GZD824 as an Orally Bioavailable Inhibitor That Targets Phosphorylated and Nonphosphorylated Breakpoint Cluster Region–Abelson (Bcr-Abl) Kinase and Overcomes Clinically Acquired Mutation-Induced Resistance against Imatinib

(2013) Xiaomei Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

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

Rearrangements of NTRK1 gene in papillary thyroid carcinoma

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