Small-molecule fms-like tyrosine kinase 3 inhibitors: an attractive and efficient method for the treatment of acute myeloid leukemia

Y Zhong, RZ Qiu, SL Sun, C Zhao, TY Fan… - Journal of medicinal …, 2020 - ACS Publications
Fms-like tyrosine kinase 3 (FLT3) is an important member of the class III receptor tyrosine
kinase (RTK) family, which is involved in the proliferation of hematopoietic cells and …

[HTML][HTML] Chasing the target: new phenomena of resistance to novel selective RET inhibitors in lung cancer. Updated evidence and future perspectives

S Fancelli, E Caliman, F Mazzoni, M Brugia… - Cancers, 2021 - mdpi.com
Simple Summary REarranged during Transfection (RET) is an emerging target for several
types of cancer, including non-small cell lung cancer (NSCLC). The recent US FDA approval …

Unraveling the Promise of RET Inhibitors in Precision Cancer Therapy by Targeting RET Mutations

ZX Wang, QQ Li, J Cai, JZ Wu, JJ Wang… - Journal of Medicinal …, 2024 - ACS Publications
Over the past decades, the role of rearranged during transfection (RET) alterations in
tumorigenesis has been firmly established. RET kinase inhibition is an essential therapeutic …

[HTML][HTML] Isoquinoline antimicrobial agent: Activity against intracellular bacteria and effect on global bacterial proteome

CW Karanja, N Naganna, NS Abutaleb, N Dayal… - Molecules, 2022 - mdpi.com
A new class of alkynyl isoquinoline antibacterial compounds, synthesized via Sonogashira
coupling, with strong bactericidal activity against a plethora of Gram-positive bacteria …

[HTML][HTML] Targeting proliferation signals and the cell cycle machinery in acute leukemias: novel molecules on the horizon

A Ghelli Luserna di Rorà, M Jandoubi, G Martinelli… - Molecules, 2023 - mdpi.com
Uncontrolled proliferative signals and cell cycle dysregulation due to genomic or functional
alterations are important drivers of the expansion of undifferentiated blast cells in acute …

Dual FLT3/TOPK inhibitor with activity against FLT3-ITD secondary mutations potently inhibits acute myeloid leukemia cell lines

N Dayal, C Opoku-Temeng, DE Hernandez… - Future Medicinal …, 2018 - Taylor & Francis
Aim: Approximately 30% of acute myeloid leukemia (AML) patients carry FLT3 tyrosine
kinase domain (TKD) mutations or internal tandem duplication (FLT3-ITD). Currently there is …

General paucity of genomic alteration and low tumor mutation burden in refractory and metastatic hepatoblastoma: comprehensive genomic profiling study

H Lee, T El Jabbour, S Ainechi, LM Gay, JA Elvin… - Human pathology, 2017 - Elsevier
Hepatoblastoma (HBL) is a hepatic malignancy of infants and young children, which is often
cured by combinations of surgery and chemotherapy. Management of refractory and …

Recent developments of RET protein kinase inhibitors with diverse scaffolds as hinge binders

CC Jia, W Chen, ZL Feng, ZP Liu - Future Medicinal Chemistry, 2021 - Taylor & Francis
RET is a proto-oncogene encoding a receptor tyrosine kinase. RET regulates key aspects of
cellular proliferation, differentiation and survival. The activation of RET via gene fusions or …

Identification of nicotinamide aminonaphthyridine compounds as potent RET kinase inhibitors and antitumor activities against RET rearranged lung adenocarcinoma

M Wang, N Naganna, HO Sintim - Bioorganic chemistry, 2019 - Elsevier
RET rearrangement is a recently identified oncogenic mutation in lung adenocarcinoma
(LADC) that accounts for approximately 2% of all NSCLCs. More than six fusion partners …

Nicotinamide–Ponatinib Analogues as potent anti-CML and anti-AML compounds

E Larocque, EFY Chu, N Naganna, HO Sintim - ACS omega, 2020 - ACS Publications
Ponatinib is a multikinase inhibitor that is used to treat chronic myeloid leukemia patients
harboring mutated ABL1 (T315I) kinase. Due to the potent inhibition of FLT3, RET, and …