Structural and dynamic determinants for highly selective RET kinase inhibition reveal cryptic druggability

Structural and dynamic determinants for highly selective RET kinase inhibition reveal cryptic druggability

Introduction: The structural and dynamic determinants that confer highly selective RET kinase inhibition are poorly understood. Objectives: To explore the druggability landscape of the RET active site in order to uncover structural and dynamic vulnerabilities that can be therapeutically exploited. M...

Full description

Bibliographic Details
Main Authors:	Moustafa A. Shehata, Julia Contreras, Ana Martín-Hurtado, Aurane Froux, Hossam Taha Mohamed, Ahmed A. El-Sherif, Iván Plaza-Menacho
Format:	Article
Language:	English
Published:	Elsevier 2023-03-01
Series:	Journal of Advanced Research
Subjects:	Protein kinases Oncogene Structure-function Targeted-therapies Drug-discovery
Online Access:	http://www.sciencedirect.com/science/article/pii/S2090123222001163

Similar Items

Tyrosine kinase – Role and significance in Cancer
Published: (2004-06-01)

Redox takes control
by: Iván Plaza-Menacho
Published: (2024-06-01)

REThinking the role of the RET oncogene in breast cancer
by: Giuseppe Di Grazia, et al.
Published: (2024-08-01)

What Does the “AKT” Stand for in the Name “AKT Kinase”? Some Historical Comments
by: Jiuyong Xie, et al.
Published: (2020-08-01)

Mapping kinase domain resistance mechanisms for the MET receptor tyrosine kinase via deep mutational scanning
by: Gabriella O Estevam, et al.
Published: (2025-02-01)

High resolution crystal structure of the FAK FERM domain reveals new insights on the Druggability of tyrosine 397 and the Src SH3 binding site
by: Timothy Marlowe, et al.
Published: (2019-05-01)

A kinase-independent function of AKT promotes cancer cell survival
by: Igor Vivanco, et al.
Published: (2014-12-01)

Dasatinib targets c-Src kinase in cardiotoxicity
by: Manar Elmadani, et al.
Published: (2023-01-01)

Druggable Transient Pockets in Protein Kinases
by: Koji Umezawa, et al.
Published: (2021-01-01)

Discovering Deleterious Single Nucleotide Polymorphisms of Human AKT1 Oncogene: An In Silico Study
by: Ruojun Zhang, et al.
Published: (2023-07-01)

GDNF and the RET Receptor in Cancer: New Insights and Therapeutic Potential
by: Lois M. Mulligan
Published: (2019-01-01)

Targeting RAS-driven human cancer cells with antibodies to upregulated and essential cell-surface proteins
by: Alexander J Martinko, et al.
Published: (2018-01-01)

Polo-like kinase-1, Aurora kinase A and WEE1 kinase are promising druggable targets in CML cells displaying BCR::ABL1-independent resistance to tyrosine kinase inhibitors
by: Manuela Mancini, et al.
Published: (2022-08-01)

Revealing druggable cryptic pockets in the Nsp1 of SARS-CoV-2 and other β-coronaviruses by simulations and crystallography
by: Alberto Borsatto, et al.
Published: (2022-11-01)

An Update on the Effectiveness of Probiotics in the Prevention and Treatment of Cancer
by: Vidya Sankarapandian, et al.
Published: (2022-01-01)

Child with RET proto-oncogene codon 634 mutation
by: Dilek İnce, et al.
Published: (2017-10-01)

Evolvable signaling networks of receptor tyrosine kinases: relevance of robustness to malignancy and to cancer therapy
by: Ido Amit, et al.
Published: (2007-12-01)

Systematic Exploration of Privileged Warheads for Covalent Kinase Drug Discovery
by: Zheng Zhao, et al.
Published: (2022-10-01)

An Intriguing Purview on the Design of Macrocyclic Inhibitors for Unexplored Protein Kinases through Their Binding Site Comparison
by: Swapnil P. Bhujbal, et al.
Published: (2023-07-01)

Regulating the regulator: a survey of mechanisms from transcription to translation controlling expression of mammalian cell cycle kinase Aurora A
by: Roberta Cacioppo, et al.
Published: (2022-09-01)

Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors
by: Wagner Ricardo Montor, et al.
Published: (2018-02-01)

Familial Medullary Thyroid Cancer: Five-year Review of the Most Frequent Mutations in the RET Gene: An Update
by: Blanca Estela Díaz Castañeda, et al.
Published: (2022-09-01)

Update and elucidation of Plasmodium kinomes: Prioritization of kinases as potential drug targets for malaria
by: Joyce Villa Verde Bastos Borba, et al.
Published: (2022-01-01)

Editorial: Diverse roles of MAP4K4 in MAP kinase signaling and its implication for cancer therapeutics
by: Ruchi Roy, et al.
Published: (2023-07-01)

Metformin as an activator of AMP-activated protein kinase. Known and new mechanisms of action
by: A. M. Mkrtumyan, et al.
Published: (2023-12-01)

Analysis of some flavonoids for inhibitory mechanism against cancer target phosphatidylinositol 3-kinase (PI3K) using computational tool
by: Mohd Suhail, et al.
Published: (2023-10-01)

Boronic Acid-Containing 3<i>H</i>- pyrazolo[4,3-<i>f</i>]quinoline Compounds as Dual CLK/ROCK Inhibitors with Anticancer Properties
by: Neetu Dayal, et al.
Published: (2024-12-01)

A new role for an old enemy
by: Richard M Monaghan, et al.
Published: (2015-02-01)

Characterization of LDD-2633 as a Novel RET Kinase Inhibitor with Anti-Tumor Effects in Thyroid Cancer
by: Hyo Jeong Lee, et al.
Published: (2021-01-01)

Successful response to imatinib in two dogs with inoperable grade III infiltrating mast cell tumours: a case report
by: J.H. Kim, et al.
Published: (2016-08-01)

Regulation, targets and functions of CHK
by: Shudong Zhu, et al.
Published: (2022-12-01)

Phosphoproteomics of short-term hedgehog signaling in human medulloblastoma cells
by: Tamara Scheidt, et al.
Published: (2020-06-01)

Surgical and clinical strategies in the management of thyroid medullary carcinoma in children with and without ret proto-oncogene mutations
by: Özlem Boybeyi-Türer, et al.
Published: (2016-08-01)

Unlocking the potential of approved drugs for the allosteric inhibition of tropomyosin-receptor kinase A using molecular docking and molecular dynamics studies
by: Rua M. Mukhtar, et al.
Published: (2023-06-01)

miRNA-Dependent Regulation of AKT1 Phosphorylation
by: Mallory I. Frederick, et al.
Published: (2022-02-01)

Point Mutations in RET Proto-Oncogene Exon 10 in Patients with Medullary Thyroid Carcinoma
by: Marjan Zarif-Yeganeh, et al.
Published: (2015-05-01)

Bioactive Phytoconstituents as Potent Inhibitors of Tyrosine-Protein Kinase Yes (YES1): Implications in Anticancer Therapeutics
by: Chunmin Yang, et al.
Published: (2022-05-01)

Data-driven analysis and druggability assessment methods to accelerate the identification of novel cancer targets
by: G. Beis, et al.
Published: (2023-01-01)

Clinical development of RET inhibitors in RET-rearranged non-small cell lung cancer: update
by: Luis Mendoza
Published: (2018-07-01)

Efficacy of first‐line immune checkpoint inhibitors in patients with advanced NSCLC with KRAS, MET, FGFR, RET, BRAF, and HER2 alterations
by: Yuji Uehara, et al.
Published: (2022-06-01)