Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.

Author: BaskaFerenc, CserepesMihály T, DobosJudit, DézsiLászló, GaramvölgyiRita, HamarPéter, KrekóMarcell, NemesZoltán, SiposAnna, SzabóEszter, Szántai-KisCsaba, SzénásiGábor, TóváriJózsef, ŐrfiLászló, ŐrfiZoltán

Paper Details 
Original Abstract of the Article :
Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20-30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as novel potent inhibitors of the FLT3-ITD and FLT3-D83...See full text at original site
Dr.Camel IconDr.Camel's Paper Summary Blogラクダ博士について

ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。

* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。


引用元:
https://doi.org/10.1016/j.ejmech.2019.111710

データ提供:米国国立医学図書館(NLM)

Targeting the FLT3 Kinase: A New Weapon Against Leukemia

Acute myeloid leukemia (AML) is a serious blood cancer that can be quite challenging to treat. This study focuses on a specific target, the FLT3 kinase, which plays a crucial role in the development of AML. The researchers have identified a new family of compounds, called (phenylethenyl)quinazolines, that act as powerful inhibitors of the FLT3 kinase. It's like finding a hidden oasis in a vast desert of cancer research, offering a promising new path to combatting this deadly disease.

A Targeted Strike Against Cancer Cells

These compounds exhibited remarkable selectivity for the FLT3 kinase, effectively targeting the mutated forms of the protein that drive the growth of AML cells. The compounds effectively triggered apoptosis, or programmed cell death, in AML cells, while having little to no effect on healthy cells. The researchers have shown that these compounds could potentially be developed into effective therapeutics for treating AML, especially in cases where the cancer has become resistant to other therapies.

A Hopeful Oasis for Leukemia Patients

This research offers a glimmer of hope for patients battling AML. The identification of these highly selective inhibitors of the FLT3 kinase presents a potential new avenue for treatment, giving patients more options to combat this challenging disease. The compounds’ ability to overcome drug resistance is particularly promising, offering a potential solution for patients whose cancer has become resistant to standard therapies.

Dr. Camel's Conclusion

This study, like a camel navigating a treacherous desert, has uncovered a potentially vital source of water for those battling AML. The compounds identified could offer a new path toward effective treatment, providing a much-needed oasis in the fight against this devastating disease.

Date :
  1. Date Completed 2020-02-18
  2. Date Revised 2020-02-18
Further Info :

Pubmed ID

31614258

DOI: Digital Object Identifier

10.1016/j.ejmech.2019.111710

Related Literature

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

This site uses cookies. Visit our privacy policy page or click the link in any footer for more information and to change your preferences.