2024藥學院優秀論文(3)

論文發表榮譽榜  |   |  150

Dr. Kunal

Nepali

Amandeep Thakur, Mandeep Rana, Anshul Mishra, Charanjit Kaur, Chun-Hsu Pan, Kunal Nepali*(corresponding). Recent advances and future directions on small molecule VEGFR inhibitors in oncological conditions. In: European Journal of Medicinal Chemistry. 2024, Published.

IF =  6.700; Ranking 11.7 % (CATEGORY:CHEMISTRY, MEDICINAL)

Introduction

A journey of mixed emotions” is a quote that best describes the progress chart of vascular endothelial growth factor receptor (VEGFR) inhibitors as cancer therapeutics in the last decade. The review perspicuously underscores the earnest attempts of the researchers to extract the antiproliferative potential of VEGFR inhibitors through the design of mechanistically diverse structural assemblages. Moreover, the review encompasses sections on structural/molecular properties and physiological functions of VEGFR, FDA-approved VEGFR inhibitors, and hurdles restricting the activity range/clinical applicability of VEGFR targeting antitumor agents. A clear-cut viewpoint transmitted through this compilation can provide practical directions to push the cart of VEGFR inhibitors to advanced-stage clinical investigations in diverse malignancies.

 

Dr. Chun-Hsu Pan Dr. Kunal Nepali

(corresponding)

Amandeep Thakur, Yi-Hsuan Chu, N. Vijayakameswara Rao, Jacob Mathew, Ajmer Singh Grewal, Prabhita Prabakaran, Santosh Guru, Jing Ping Liou, Chun-Hsu Pan*(corresponding), Kunal Nepali*(corresponding). Leveraging a rationally designed veliparib-based anilide eliciting anti-leukemic effects for the design of pH-responsive polymer nanoformulation. In: European Journal of Medicinal Chemistry. 2024, Accepted; Articles in press.

IF = 6.700 ; Ranking 11.7 % (CATEGORY:CHEMISTRY, MEDICINAL)

Introduction

Careful recruitment of the components of the HDAC inhibitory template culminated in veliparib-based anilide 8 that elicited remarkable cell growth inhibitory effects against HL-60 cell lines mediated via dual modulation of PARP and HDAC. Polymer nanoformulation (mPEG-PCl copolymeric micelles loaded with compound 8) was prepared which manifested pH-sensitive behaviour as a greater release was observed at 6.2 pH as compared to 7.4 pH mimicking physiological settings. The findings indicate that the acidic pH of the tumour microenvironment might stimulate the nanomedicine release which in turn can attenuate the off-target effects precedentially claimed to be associated with HDAC inhibitors.