Results 31 to 40 of about 634,915 (204)

Development of cancer targeted Nampt inhibitors [PDF]

open access: yes, 2021
The purpose of this research is the discovery of a highly potent pharmaceutical that can selectively cause apoptosis in various cancer cells. To utilize hydrophobic properties of carboranes, 1,7-dicarba-closo-dodecaborane (m-CB) has been selected as a template to synthesize new targeted antitumor agent.
openaire   +2 more sources

Dependence of Tumor Cell Lines and Patient-Derived Tumors on the NAD Salvage Pathway Renders Them Sensitive to NAMPT Inhibition with GNE-618

open access: yesNeoplasia: An International Journal for Oncology Research, 2013
Nicotinamide adenine dinucleotide (NAD) is a critical metabolite that is required for a range of cellular reactions. A key enzyme in the NAD salvage pathway is nicotinamide phosphoribosyl transferase (NAMPT), and here, we describe GNE-618, an NAMPT ...
Yang Xiao   +14 more
doaj   +1 more source

Discovery of Novel Inhibitors and Fluorescent Probe Targeting NAMPT [PDF]

open access: yesScientific Reports, 2015
AbstractNicotinamide phosphoribosyltransferase (NAMPT) is a promising antitumor target. Novel NAMPT inhibitors with diverse chemotypes are highly desirable for development of antitumor agents. Using high throughput screening system targeting NAMPT on a chemical library of 30000 small-molecules, we found a non-fluorescent compound F671-0003 and a ...
Xia Wang   +12 more
openaire   +2 more sources

AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells

open access: yesFrontiers in Cell and Developmental Biology, 2022
BRD4, a chromatin modifier frequently upregulated in a variety of neoplasms including hepatocellular cancer (HCC), promotes cancer cell growth by activating oncogenes through its interaction with acetylated histone tails of nucleosomes.
Cho-Hao Lin   +12 more
doaj   +1 more source

Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors [PDF]

open access: yesMolecular Cancer Therapeutics, 2017
Abstract Cancer cells are highly reliant on NAD+-dependent processes, including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme for NAD+ salvage from nicotinamide, has been investigated as a target for anticancer therapy ...
Julie L, Wilsbacher   +32 more
openaire   +2 more sources

NAD+ supplement potentiates tumor-killing function by rescuing defective TUB-mediated NAMPT transcription in tumor-infiltrated T cells

open access: yesCell Reports, 2021
Summary: Although tumor-infiltrating lymphocytes (TILs) maintain their ability to proliferate, persist, and eradicate tumors, they are frequently dysfunctional in situ.
Yuetong Wang   +16 more
doaj   +1 more source

Oxygen-dependent interactions between the ruthenium cage and the photoreleased inhibitor in NAMPT-targeted photoactivated chemotherapy [PDF]

open access: yes
Photoactivated chemotherapy agents show a promising ability to kill cancer cells under the action of light, including those in chronic hypoxic conditions.
Jaap, Wildeman   +13 more
core   +2 more sources

Structural elements determining NAMPT activity [PDF]

open access: yes, 2023
Nikotinamidadenindinukleotid (NAD) er en hydridbærer involvert i redoksreaksjoner i metabolismen. I tillegg er NAD+ et substrat av enzymer som medierer vitale NAD+-avhengige prosesser, der dinukleotidet spaltes, og frigjør en nikotinamiddel (Nam ...
Houry, Dorothée
core   +1 more source

Overexpression of Nampt in gastric cancer and chemopotentiating effects of the Nampt inhibitor FK866 in combination with fluorouracil

open access: yesOncology Reports, 2011
Nicotinamide phosphoribosyltransferase (Nampt), an enzyme involved in the NAD⁺ salvage pathway, is over-expressed and important in the carcinogenesis in several types of cancers. The expression of Nampt and its role in gastric cancer remain largely unknown. In this study, using real-time PCR and Western blotting we found that Nampt was overexpressed at
Tie-Qiang, Bi   +6 more
openaire   +3 more sources

miR-146a impedes the anti-aging effect of AMPK via NAMPT suppression and NAD+/SIRT inactivation

open access: yesSignal Transduction and Targeted Therapy, 2022
Nicotinamide adenine dinucleotide (NAD+) is indispensable for the anti-aging activity of the sirtuin (SIRT) family enzymes. AMP-activated protein kinase (AMPK) upregulates NAD+ synthesis and SIRT activity in a nicotinamide phosphoribosyltransferase ...
Hui Gong   +15 more
doaj   +1 more source

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