Results 171 to 180 of about 3,327,333 (431)

Stochastic variation in the FOXM1 transcription program mediates replication stress tolerance

open access: yesMolecular Oncology, EarlyView.
Cellular heterogeneity is a major cause of drug resistance in cancer. Segeren et al. used single‐cell transcriptomics to investigate gene expression events that correlate with sensitivity to the DNA‐damaging drugs gemcitabine and prexasertib. They show that dampened expression of transcription factor FOXM1 and its target genes protected cells against ...
Hendrika A. Segeren   +4 more
wiley   +1 more source

A transient inflammatory response contributes to oxaliplatin neurotoxicity in mice

open access: yesAnnals of Clinical and Translational Neurology, Volume 9, Issue 12, Page 1985-1998, December 2022., 2022
Abstract Objectives Peripheral neuropathy is a relevant dose‐limiting adverse event that can affect up to 90% of oncologic patients with colorectal cancer receiving oxaliplatin treatment. The severity of neurotoxicity often leads to dose reduction or even premature cessation of chemotherapy.
Aina Calls   +9 more
wiley   +1 more source

In Vitro High Throughput Screening, What Next? Lessons from the Screening for Aurora Kinase Inhibitors

open access: yesBiology, 2014
Based on in vitro assays, we performed a High Throughput Screening (HTS) to identify kinase inhibitors among 10,000 small chemical compounds. In this didactic paper, we describe step-by-step the approach to validate the hits as well as the major pitfalls
Thi-My-Nhung Hoang   +4 more
doaj   +1 more source

Empowering AlphaFold2 for protein conformation selective drug discovery with AlphaFold2-RAVE [PDF]

open access: yes
Small molecule drug design hinges on obtaining co-crystallized ligand-protein structures. Despite AlphaFold2's strides in protein native structure prediction, its focus on apo structures overlooks ligands and associated holo structures. Moreover, designing selective drugs often benefits from the targeting of diverse metastable conformations. Therefore,
arxiv   +1 more source

CircCCNB1 inhibits vasculogenic mimicry by sequestering NF90 to promote miR‐15b‐5p and miR‐7‐1‐3p processing in nasopharyngeal carcinoma

open access: yesMolecular Oncology, EarlyView.
CircCCNB1 expression is down‐regulated in nasopharyngeal carcinoma (NPC); thus, less NF90 protein is bound to circCCNB1 and more binds to pri‐miRNAs, blocking their (pri‐miRNAs) binding to DGCR8 and inhibiting the processing and generation of miR‐15b‐5p/miR‐7‐1‐3p. Furthermore, decreased miR‐15b‐5p/miR‐7‐1‐3p promotes the expression of the target genes
Chunmei Fan   +6 more
wiley   +1 more source

Rho-Kinase Activity And Cutaneous Vasoconstriction Is Upregulated In Essential Hypertensive Humans [PDF]

open access: yes, 2013
Essential hypertension (HT) is associated with endothelial dysfunction augmented vasoconstriction (VC) which may be secondary to increased Rho/Rho-Kinase (ROCK)-dependent mechanisms.
NC DOCKS at Appalachian State University   +1 more
core  

Thermal proteome profiling and proteome analysis using high‐definition mass spectrometry demonstrate modulation of cholesterol biosynthesis by next‐generation galeterone analog VNPP433‐3β in castration‐resistant prostate cancer

open access: yesMolecular Oncology, EarlyView.
Elevated level of cholesterol is positively correlated to prostate cancer development and disease severity. Cholesterol‐lowering drugs, such as statins, are demonstrated to inhibit prostate cancer. VNPP433‐3β interrupts multiple signaling and metabolic pathways, including cholesterol biosynthesis, AR‐mediated transcription of several oncogenes, mRNA 5′
Retheesh S. Thankan   +10 more
wiley   +1 more source

Prediction of Small Molecule Kinase Inhibitors for Chemotherapy Using Deep Learning [PDF]

open access: yesarXiv, 2019
The current state of cancer therapeutics has been moving away from one-size-fits-all cytotoxic chemotherapy, and towards a more individualized and specific approach involving the targeting of each tumor's genetic vulnerabilities. Different tumors, even of the same type, may be more reliant on certain cellular pathways more than others.
arxiv  

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