Review of various NAMPT inhibitors for the treatment of cancer

Y Wei, H Xiang, W Zhang - Frontiers in Pharmacology, 2022 - frontiersin.org
Nicotinamide phosphoribosyltransferase (NAMPT) is a rate-limiting enzyme in the NAD
salvage pathway of mammalian cells and is overexpressed in numerous types of cancers …

Recent advances of targeting nicotinamide phosphoribosyltransferase (NAMPT) for cancer drug discovery

H Tang, L Wang, T Wang, J Yang, S Zheng… - European Journal of …, 2023 - Elsevier
Highlights•NAMPT is overexpressed in cancers, associating with a poor prognosis and
tumor progression.•Extensive efforts have been made to improve efficacy and safety of early …

Novel RICTOR amplification harbouring entities: FISH validation of RICTOR amplification in tumour tissue after next-generation sequencing

D Sztankovics, I Krencz, D Moldvai, T Dankó, Á Nagy… - Scientific Reports, 2023 - nature.com
Alterations in mTOR signalling molecules, including RICTOR amplification, have been
previously described in many cancers, particularly associated with poor prognosis. In this …

NAD+ Metabolism Generates a Metabolic Vulnerability in Endocrine-Resistant Metastatic Breast Tumors in Females

AN Mogol, Q Zuo, JY Yoo, AZ Kaminsky, OB Imir… - …, 2023 - academic.oup.com
Approximately 70% of human breast cancers express estrogen receptor-α (ERα), providing
a potential target for endocrine therapy. However, 30% to 40% of patients with ER+ breast …

Drug discovery targeting nicotinamide phosphoribosyltransferase (NAMPT): Updated progress and perspectives

F Wen, G Gui, X Wang, L Ye, A Qin, C Zhou… - Bioorganic & Medicinal …, 2024 - Elsevier
Nicotinamide phosphoribosyltransferase (NAMPT) is a key rate-limiting enzyme in the
nicotinamide adenine dinucleotide (NAD+) salvage pathway, primarily catalyzing the …

[HTML][HTML] Synthesis and structure-activity relationship of new nicotinamide phosphoribosyltransferase inhibitors with antitumor activity on solid and haematological …

S Fratta, P Biniecka, AJ Moreno-Vargas… - European Journal of …, 2023 - Elsevier
Cancer cells are highly dependent on Nicotinamide phosphoribosyltransferase (NAMPT)
activity for proliferation, therefore NAMPT represents an interesting target for the …

Recent advances on development of p21-activated kinase 4 inhibitors as anti-tumor agents

Y Li, Q Lu, C Xie, Y Yu, A Zhang - Frontiers in pharmacology, 2022 - frontiersin.org
The p21-activated kinase 4 (PAK4) is a member of the PAKs family. It is overexpressed in
multiple tumor tissues. Pharmacological inhibition of PAK4 attenuates proliferation …

[HTML][HTML] A novel PAK4 inhibitor suppresses pancreatic cancer growth and enhances the inhibitory effect of gemcitabine

H He, C Dumesny, CS Ang, L Dong, Y Ma, J Zeng… - Translational …, 2022 - Elsevier
Over 95% of Pancreatic ductal adenocarcinomas (PDA) carry mutations in the oncogene
KRas which has been proven to be a difficult drug target. P21-activated kinase 4 (PAK4) …

Novel therapeutic strategies exploiting the unique properties of neuroendocrine neoplasms

M Safari, L Scotto, T Litman, LA Petrukhin, H Zhu… - Cancers, 2023 - mdpi.com
Simple Summary The screening of experimental and repurposing drugs has enormous
potential for rapid clinical impact, particularly when new therapeutic strategies are sought …

[HTML][HTML] PAK4 inhibition significantly potentiates Gemcitabine activity in PDAC cells via inhibition of Wnt/β-catenin, p-ERK/MAPK and p-AKT/PI3K pathways

C Samant, R Kale, A Bokare, M Verma, KSR Pai… - … and Biophysics Reports, 2023 - Elsevier
Abstract Pancreatic Ductal Adenocarcinoma (PDAC) remains one of the most difficult to treat
cancers. Gemcitabine is still the standard of care treatment for PDAC but with modest …