Intrinsic drug potential of oxazolo[5,4‐d]pyrimidines and oxazolo[4,5‐d]pyrimidines DOI
Victor Zhirnov, Yevheniia Velihina, Oleg P. Mitiukhin

et al.

Chemical Biology & Drug Design, Journal Year: 2021, Volume and Issue: 98(4), P. 561 - 581

Published: June 20, 2021

The oxazole and pyrimidine rings are widely displayed in natural products synthetic molecules. They known as the prime skeletons for drug discovery. On account of structural chemical diversity, pyrimidine-based molecules, central scaffolds, not only provide different types interactions with various receptors enzymes, showing broad biological activities, but also occupy a core position medicinal chemistry, their importance development discovery newer potential therapeutic agents (Curr Top Med Chem, 16, 2016, 3133; Int J Pharm Sci, 8, 8; BMC 13, 2019, 44). For long time, relatively little attention has been paid to fused that oxazolopyrimidines, whose structure is similar purines because probably none these compounds were found or activities turned out be unexpressed (Bull Chem Soc Jpn, 43, 1970, 187). Recently, however, significant number studies have published on properties oxazolo[5,4-d]pyrimidines, activity agonists antagonists signaling pathways involved regulation cell life cycle, whereas oxazolo[4,5-d]pyrimidines, contrary, represent poorly studied class compounds. Limited access this scaffold resulted corresponding lack research (Eur Organ 18, 2018, 2148). Actually, oxazolo[5,4-d]pyrimidine versatile used design bioactive ligands against enzymes receptors. This review focuses targets associated pathogenetic mechanisms, well pathological disorders can modified by well-known oxazolopyrimidines proven date. Many molecular details processes omitted here, which interested reader will find cited literature. work does cover methods synthesis exhaustively described De Coen et al. discuss structure-activity relationship, detail original works deliberately, whenever possible, cites primary sources, mostly relevant articles, so who wants delve into particular problem immediately receive more complete information. It expected information presented help readers better understand purpose possibility drugs treatment wide range diseases.

Language: Английский

Cannabis sativa: Much more beyond Δ9-tetrahydrocannabinol DOI
Patrícia Alves, Cristina Amaral, Natércia Teixeira

et al.

Pharmacological Research, Journal Year: 2020, Volume and Issue: 157, P. 104822 - 104822

Published: April 23, 2020

Language: Английский

Citations

106
Cannabis Use in Patients With Cancer: A Clinical Review DOI Open Access
Brooke Worster, Emily Hajjar, Nathan Handley

et al.

JCO Oncology Practice, Journal Year: 2022, Volume and Issue: 18(11), P. 743 - 749

Published: June 24, 2022

Cannabis use and interest continues to increase among patients with cancer caregivers. High-quality research remains scant in many areas, causing hesitancy or discomfort most clinical providers. Although we have limitations on hard outcomes, can provide some guidance more proactively engage conversations family about cannabis. Several studies support the efficacy of cannabis for various treatment-related symptoms, such as chemotherapy-induced nausea pain. formulations dosing guidelines clinicians do not formally exist at present, attention tetrahydrocannabinol concentration understanding risks inhalation reduce risk. Conflicting information exists interaction between immunotherapy well estrogen receptor interactions. Motivational interviewing help productive, less stigmatized conversations.

Language: Английский

Citations

39
MASCC guideline: cannabis for cancer-related pain and risk of harms and adverse events DOI

Josephine To,

Mellar P. Davis, Andrea Sbrana

et al.

Supportive Care in Cancer, Journal Year: 2023, Volume and Issue: 31(4)

Published: March 6, 2023

Language: Английский

Citations

32
Baicalein resensitizes tamoxifen‐resistant breast cancer cells by reducing aerobic glycolysis and reversing mitochondrial dysfunction via inhibition of hypoxia‐inducible factor‐1α DOI Creative Commons
Yan Chen, Jingyu Zhang,

Minqin Zhang

et al.

Clinical and Translational Medicine, Journal Year: 2021, Volume and Issue: 11(11)

Published: Nov. 1, 2021

Abstract Drug resistance is a major hurdle for the effectiveness of tamoxifen (TAM) to provide clinical benefit. Therefore, it essential identify sensitizer that could be used improve TAM efficacy in treating TAM‐resistant breast cancer. Here, we investigated ability baicalein reverse resistance. We found increased inhibiting proliferation and inducing apoptosis cells. It also enhanced TAM‐induced growth reduction resistant cells from NOD/SCID mouse mammary fat pads, without causing obvious systemic toxicity. Analyses using CellMiner tool Kaplan–Meier plotter database showed HIF‐1α expression was inversely correlated with therapeutic response NCI‐60 cancer patients. due an increase mRNA levels reduced ubiquitin‐mediated degradation. Baicalein by promoting its interaction PHD2 pVHL, thus facilitating ubiquitin ligase‐mediated proteasomal degradation thereby suppressing nuclear translocation, binding hypoxia‐response element, transcriptional activity HIF‐1α. As result, downregulated aerobic glycolysis restricting glucose uptake, lactate production, ATP generation, lactate/pyruvate ratio HIF‐1α‐targeted glycolytic genes, enhancing antiproliferative TAM. Furthermore, interfered inhibition mitochondrial biosynthesis, which DNA content numbers, restored generation reactive oxygen species mitochondria, apoptotic pathway. The stabilizer dimethyloxallyl glycine prevented baicalein‐induced downregulation biosynthesis effects on reversing Our results indicate promising candidate help overcome sensitizing apoptosis. mechanism underlying consists HIF‐1α–mediated dysfunction.

Language: Английский

Citations

56
A Coala‐T‐Cannabis Survey Study of breast cancer patients' use of cannabis before, during, and after treatment DOI Open Access
Marisa C. Weiss,

Julianne Hibbs,

Meghan Buckley

et al.

Cancer, Journal Year: 2021, Volume and Issue: 128(1), P. 160 - 168

Published: Oct. 12, 2021

Background The goal of this study was to characterize cannabis use among patients with breast cancer, including their reasons for and timing use, sources information products, satisfaction the found, perceptions its safety, dialogue about physicians. Methods United States–based members Breastcancer.org Healthline.com communities a self‐reported diagnosis cancer within 5 years (age ≥ 18 years) were invited participate in an anonymous online survey. After informed consent obtained, nonidentifiable data collected analyzed. Results Of all participants (n = 612), 42% 257) reported using relief symptoms, which included pain (78%), insomnia (70%), anxiety (57%), stress (51%), nausea/vomiting (46%). Furthermore, 49% users believed that medical could be used treat itself. those taking cannabis, 79% had it during treatment, systemic therapies, radiation, surgery. At same time, few (39%) discussed any Conclusions A significant percentage survey (42%) address symptoms; approximately half these Most active treatment despite potential adverse event vulnerable time. most safe unaware product quality varied widely depended on source. This reviews research medicinal setting findings help physicians recognize risks benefits cancer. Lay Summary Almost commonly manage common symptoms side effects: pain, anxiety, insomnia, nausea. However, do not discuss Instead, internet family/friends are information. believe products safety many is untested.

Language: Английский

Citations

45
Current and Potential Use of Biologically Active Compounds Derived from Cannabis sativa L. in the Treatment of Selected Diseases DOI Open Access
Bożena Bukowska

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(23), P. 12738 - 12738

Published: Nov. 27, 2024

Cannabis sativa L. contains numerous compounds with antioxidant and anti-inflammatory properties, including the flavonoids cannabinoids, particularly Δ-9-tetrahydrocannabinol (THC) cannabidiol (CBD). Cannabinoids have an effect on endocannabinoid system (ECS), a cellular communication network, are, hence, widely studied for medical applications. Epidiolex®, 99% pure oral CBD extract, has been approved by FDA treatment of epilepsy. Nabiximols (Sativex) is oromucosal spray containing equal volume THC CBD, it commonly used as add-on unresponsive spasticity in multiple sclerosis (MS) patients. Several vitro vivo studies also shown that cannabinoids can be to treat various types cancer, such melanoma brain glioblastoma; first positive clinical trials anticancer THC:CBD blend temozolomide (TMZ) highly invasive cancer are very promising. The exert their properties investigations induction cell death, mainly apoptosis cytotoxic autophagy, inhibition proliferation. In several studies, found induce tumor regression inhibit angiogenic mechanisms vivo, well two low-numbered epidemiological studies. They exhibit antiviral effects inhibiting ACE2 transcription, blocking viral replication fusion, acting agents; indeed, prior consumption (a study 93,565 persons Chicago) associated much lower incidence SARS-CoV-2 infections. It postulated cannabis extracts many other diseases systemic lupus erythematosus, type 1 diabetes, or neurological disorders, e.g., Alzheimer’s disease. aim this review outline current state knowledge regarding currently medicinal preparations derived from C. selected diseases, present latest research potential applications its secondary metabolites.

Language: Английский

Citations

8
Causal relationship between cannabis use and cancer: a genetically informed perspective DOI
Peng Huang, Pengfei Zhang,

Qiu Li

et al.

Journal of Cancer Research and Clinical Oncology, Journal Year: 2023, Volume and Issue: 149(11), P. 8631 - 8638

Published: April 26, 2023

Language: Английский

Citations

16
Endocannabinoid System and Metabolism: The Influences of Sex DOI Open Access

Isabel Forner-Piquer,

Christian Giommi, Fiorenza Sella

et al.

International Journal of Molecular Sciences, Journal Year: 2024, Volume and Issue: 25(22), P. 11909 - 11909

Published: Nov. 6, 2024

The endocannabinoid system (ECS) is a lipid signaling involved in numerous physiological processes, such as endocrine homeostasis, appetite control, energy balance, and metabolism. ECS comprises endocannabinoids, their cognate receptors, the enzymatic machinery that tightly regulates levels within tissues. This has been identified various organs, including brain liver, multiple mammalian non-mammalian species. However, information regarding sex-specific regulation of remains limited, even though increasing evidence suggests interactions between sex steroid hormones may ultimately modulate hepatic metabolism homeostasis. Within this framework, we will review sexual dimorphism animal models, providing crosstalk endocannabinoids via different metabolic pathways. Additionally, underscore importance understanding how endocrine-disrupting chemicals exogenous cannabinoids influence ECS-dependent pathways manner.

Language: Английский

Citations

5
The Preventive Role of Regular Physical Training in Ventricular Remodeling, Serum Cardiac Markers, and Exercise Performance Changes in Breast Cancer in Women Undergoing Trastuzumab Therapy—An REH-HER Study DOI Open Access
Katarzyna Hojan, Danuta Procyk,

Dorota Horyńska-Kęstowicz

et al.

Journal of Clinical Medicine, Journal Year: 2020, Volume and Issue: 9(5), P. 1379 - 1379

Published: May 7, 2020

Cardiotoxicity is known as a severe clinical problem in oncological practice that reduces the options for cancer therapy. Physical exercise recognized well-established protective measure many heart and diseases. In our study, we hypothesized supervised moderate-intensity training would prevent failure its consequences induced by trastuzumab The aim of this study was to examine effect physical on ventricular remodeling, serum cardiac markers, performance women with human epidermal growth receptor 2 (HER2+) breast (BC) undergoing This prospective, randomized, controlled trial. Forty-six BC were randomized into either an intervention group (IG) or control (CG). An program performed after 3–6 months therapy at 5 d/week (to 80% maximum rate (HRmax)) 9 weeks. We then evaluated their function using echocardiography, 6-Minute Walk Test (6MWT), plasma parameters (C-reactive protein (CRP), myoglobin (MYO), interleukin-6 (IL-6), alanine aminotransferase (ALT), aspartate (AST), creatine kinase (CK)). After program, did not observe any significant changes left (LV) ejection fraction (LVEF) 6MWT (p > 0.05) IG compared CG (decrease p < 0.05). differences blood To conclude, prevented decrease LVEF capacity during HER2+ BC. Further research needed validate results.

Language: Английский

Citations

37
Unveiling the mechanism of action behind the anti-cancer properties of cannabinoids in ER+ breast cancer cells: Impact on aromatase and steroid receptors DOI
Cristina Amaral,

Fabien Marc Trouille,

Cristina Ferreira Almeida

et al.

The Journal of Steroid Biochemistry and Molecular Biology, Journal Year: 2021, Volume and Issue: 210, P. 105876 - 105876

Published: March 18, 2021

Language: Английский

Citations

29