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The Expression and Oncogenic Role of NTSR2 in Human Glioblastoma.

BACKGROUND/AIMS: Neurotensin receptor 2 (NTSR2) plays critical pro-tumor roles in multiple human solid tumors. However, the expression chara … ally, NTSR2 activates AKT signaling and modulates the expression of downstream effectors, including Cyclin B1/CDK4, ASCL1, POSTN, proBDNF and Caspase-3. In vivo imaging results further verified that NTSR2 knockdown markedly suppresses intracranial tumor growth. CONCLUSION: Despite decreased expression in GBM tissues, NTSR2 functions as an oncogenic driver …

CDKN2A alterations as possible molecular link between environmental pollutants and pathogenesis of liver cancer: Epidemiology, mechanisms, and insights.

Hepatocellular carcinoma (HCC) represents a global public health burden of increasing magnitude, driven by risk factors including viral hepatitis, metabolic dysfunction-associated fatty liver disease and various environmental carcinogens, which may inactivate key tumor suppressor genes or activates oncogenes. Recent studies have linked various environmental exposures with inactivation of tumor suppressor gene CDKN2A (cyclin dependent kinase inhibitor 2A) and its encoded proteins p16INK4a and p14ARF to various molecular pathways leading to hepatocarcinogenesis. Current studies suggest p16INK4a

KIF20A in Human Malignancies: Oncogenic Mechanisms and Therapeutic Targeting Strategies.

KIF20A is a key member of the kinesin family and is indispensable for the mitotic process. It governs cytokinesis, spindle dynamics, and cen … through multiple pathways. It drives G2/M phase transition by interacting with Aurora B kinase and cyclin B1. KIF20A suppresses cell apoptosis by regulating Bcl-2 family protein expression. It induces Epithelial-Mesenchymal Transition (EMT) by controlling Snail and Twist signaling. KIF20A also enhances cell migration and invasion by modulating MMP-2 and MM …

Targeting KIF11 degradation: Oxypeucedanin inhibits lung adenocarcinoma progression by disrupting the MCM2-CDK1 signaling pathway.

BACKGROUND AND PURPOSE: Lung adenocarcinoma (LUAD) is the most prevalent subtype of lung cancer and a leading cause of cancer-related mortal … tion led to destabilization of its interacting partner, MCM2, consequently downregulating the CDK1/ Cyclin B1 complex and ultimately triggering G2/M phase cell cycle arrest. CONCLUSION AND IMPLICATIONS: OPD functions as a novel molecular degrader of KIF11, exerting its anti-LUAD effects by promoting KIF11 ubiquitination and subsequent proteasomal degradati …

TRPV1 Downregulation Impairs Prostate Cancer Growth: Functional and Translational Insights from Cellular and In Vivo Models.

The transient receptor potential vanilloid 1 (TRPV1), the canonical capsaicin (CAP) receptor, has been implicated across diverse pathologies … roteomic analysis and Western blotting of TRPV1-silenced cells revealed reduced expression of PCNA, Cyclin B1, and AURKA, along with elevated levels of the cell cycle inhibitor p21. Similarly, CAP treatment resulted in comparable changes in the proteomic profile. Functional assays demonstrated that both TRPV1 knockdown and CAP exposure significantly impaire …

Synthesis and Characterization of 1,10-Phenanthroline-Linked Imidazolium Salts: Investigation of Their Cytotoxicity Properties.

This study focuses on the synthesis, characterization, and anticancer activities of 1,10-phenanthroline-linked imidazolium salts (3) bearing … e interaction of 3e with key apoptotic and cell cycle regulatory proteins (Bcl-2, Bcl-xL, CDK1, and Cyclin B1), suggesting a potential mechanism for its anticancer activity. ADME-related analyses of the lead compound 3e were conducted, providing an initial pharmacokinetic profile to support its progression as a preclinical candidate. In cancer cell lines, m …

Synthesis, Biological Evaluation, and Mechanistic Insights of Rubrolide Analogues as Antitumor Agents.

Marine natural products and their analogues have as of now been acknowledged as an important source of bioactive molecules for the treatment … ls to ultimately trigger apoptosis in tumor cells. Additionally, compound 7 was found to upregulate Cyclin B1 protein expression, causing cell cycle reticulum at the G2/M phase. In vivo studies further demonstrated that liposomal delivery of compound 7 exhibited a potent antitumor efficacy against Hela xenograft tumors. Based on these results, marine-derive …

Mechanistic insight into hyaluronic acid and platelet-rich plasma-mediated anti-inflammatory and anti-apoptotic activities in osteoarthritic mice.

Osteoarthritis (OA) poses a major clinical challenges owing to limited regenerative ability of diseased or traumatized chondrocytes in artic … caspase-3 and PARP, p53 and p21 and MMP-1; whereas, cell cycle modulatory proteins including p-ERK, cyclin B1, D1, and E2 were upregulated. The sub-G1 population and TUNEL assay confirmed the higher abundance of healthy chondrocytes in HA+PRP group. A significantly decreased ARS staining in HA+PRP group was also noted, indicating reduced cartilaginous matri …

The clinicopathological and prognostic impact of 14-3-3 sigma expression on vulvar squamous cell carcinomas.

BACKGROUND: 14-3-3 sigma promotes G2/M cell cycle arrest by sequestering cyclin B1-CDC2 complex in cytoplasm. Down-regulation of 14-3-3sigma, which has been demonstrated in various carcinomas, may contribute to malignant transformation. However, the exact role of 14-3-3sigma in the pathogenesis of vulvar carcinoma is not fully characterized, and the prognostic impact of 14-3-3sigma protein expression is still unknown. METHODS: We investigated the 14-3-3sigma expression in a series of 302 vulvar squamous cell carcinomas using immunohistochemistry and its associations with clinicopathological f…

Anti-adult T‑cell leukemia/lymphoma activity of cerdulatinib, a dual SYK/JAK kinase inhibitor.

Adult T‑cell leukemia/lymphoma (ATLL) constitutes an aggressive malignancy caused by human T‑cell leukemia virus type 1 (HTLV‑1) that is resistant to available chemotherapeutics. The constitutive activation of Janus kinase (JAK)-signal transducer and activator of transcription (STAT) signaling is an important feature of ATLL, and spleen tyrosine kinase (SYK) is overexpressed in HTLV‑1-transformed T‑cell lines. In this study, we evaluated the effects of SYK- (PRT060318) or JAK- (JAK inhibitor 1) selective inhibitors and the dual SYK/JAK inhibitor, cerdulatinib, on the viability of HTLV‑1-transf

Reexpression of oncoprotein MafB in proliferative β-cells and Men1 insulinomas in mouse.

MafB, a member of the large Maf transcription factor family, is essential for the embryonic and terminal differentiation of pancreatic α- an … oci formation both in culture medium and on soft agar, accompanied with the increased expression of Cyclin B1 and D2. Conversely, MafB downregulation by siRNA transfection reduced BrdU incorporation in INS-1E cells. Taken together, our data reveal that Men1 inactivation leads to MafB reexpression in mouse β-cells in vivo, and provides evidence that deregula …

Alterations in steroid hormone receptors, angiogenic, cell proliferation, apoptotic, and Ras-related factors during estrous cycle in porcine corpus luteum.

This study aimed to examine the association of Ras signaling with steroid hormone receptors, angiogenic factors, cell cycle/cell proliferati … factors revealed increased extracellular signal-regulated kinase 1, cyclin dependent kinase 1, and cyclin B1 mRNA expression in MP, whereas CCNB1 protein expression increased in EP. tumor necrosis factor receptor 1 mRNA was the highest in LP, Bax and caspase 3 mRNA increased in the MP group, and Bcl2 mRNA increased at EP. At the protein level, Casp3 was ma …

Inhibitors of anti-apoptotic Bcl-2 family proteins exhibit potent and broad-spectrum anti-mammarenavirus activity via cell cycle arrest at G0/G1 phase.

UNLABELLED: Targeting host factors is a promising strategy to develop broad-spectrum antiviral drugs. Drugs targeting anti-apoptotic Bcl-2 f … Bcl-2 correlated with reduced expression levels of thymidine kinase 1 (TK1), cyclin A2 (CCNA2), and cyclin B1 (CCNB1) cell cycle regulators. In addition, siRNA-mediated knock down of TK1, CCNA2, and CCNB1 resulted in reduced levels of LCMV multiplication. The antiviral activity exerted by Bcl-2 inhibitors correlated with reduced levels of viral RNA synthesi …

Ингибиторы антиапоптотической продукции Bcl-2 - выставка на выставке протеинов и широкополосная антиаммаренавирусная активность с помощью клеточного цикла в фазе G0/G1.

Нацеливание на принимающие факторы является перспективной стратегией разработки широких спектральных антивирусных препаратов. Согласно сообщениям, лекарственные средства, направленные против апоптотических белков семейства Bcl-2, которые изначально были разработаны в качестве опухолей, препятствуют умножению различных типов вирусов. Однако механизмы, с помощью которых ингибиторы Bcl-2 осуществляют свою антивирусную деятельность, по-прежнему плохо понимаются. В этом исследовании мы изучили механизмы, с помощью которых ингибиторы обнацлакса (OLX) и ABT-737 Bcl-2 продемонстрировали мощную антивир

Совпадение в аннотации оригинала
Targeting host factors is a promising strategy to develop broad-spectrum antiviral drugs. Drugs targeting anti-apoptotic Bcl-2 family protei … Bcl-2 correlated with reduced expression levels of thymidine kinase 1 (TK1), cyclin A2 (CCNA2), and cyclin B1 (CCNB1) cell cycle regulators. In addition, small interfering RNA (siRNA)-mediated knockdown of TK1, CCNA2, and CCNB1 resulted in reduced levels of LCMV multiplication. The antiviral activity exerted by Bcl-2 inhibitors correlated with reduced level …

Caloric restriction and IGF-I administration promote rabbit fecundity: Possible interrelationships and mechanisms of action.

The aim of these in vivo and in vitro studies was to examine the influence of caloric restriction (CR), and the administration of insulin-li … for 2 d with and without IGF-I (100 ng/mL). Accumulation of markers of cell proliferation (PCNA and cyclin B1), apoptosis (bax), MAP/ERK1,2 kinase (MAPK), protein kinase A (PKA) and IGF-I were evaluated by immunocytochemistry. In addition, E2 release by cells isolated from ovaries of animals subjected or not to CR and cultured with and without IGF-I (1, 10, …

[Blueberry anthocyanins combined with oxaliplatin regulate the GSK-3β pathway to enhance chemosensitivity in colon cancer cells].

OBJECTIVE: To investigate the effect and potential mechanism of blueberry anthocyanins(BA) in enhancing the chemosensitivity of colon cancer … etry. Western blot was performed to detect the expression of cell cycle-related proteins(Cyclin D1, Cyclin B1, CDK4), proliferating cell nuclear antigen(PCNA), and glycogen synthase kinase-3β(GSK-3β). After pretreatment with 50 μmol/L lithium chloride(LiCl) for 6 hours, HCT116 cell viability was assessed by CCK-8 assay, and GSK-3β protein expression was mea …

A novel designed fully peptide-based PROTAC, FPP29, demonstrates its potent cytotoxic effects to liver cancer HCCLM3 cells by targeting FOXM1.

FOXM1 (Forkhead box M1), a key transcription factor in the Forkhead box (FOX) family, is overexpressed across multiple cancer types and impl … FPP29 can stably bind to FOXM1 and regulate the expression of FOXM1 and its related genes including cyclin B1, CDC25B, and c-Myc. In addition, FPP29 can enhance FOXM1 poly-ubiquitination and induce its degradation through the ubiquitin-proteasome system. In vivo studies in xenograft mice showed that 15 mg/kg FPP29 inhibited tumor growth by 75 % with no appa …

Design and synthesis of Riluzole-Ciprofloxacin hybrids as selective MST3 inhibitors for cancer treatment.

The MST3 isozyme is integral to the modulation of cellular proliferation and apoptosis, with its dysregulation critically implicated in the … Bcl-2, resulted in inducing HepG2 cells apoptosis. Meanwhile, it decreased the expression level of cyclin B1 in a concentration-dependent manner, leading to cell cycle at the G2/M transition. The in vivo experiments demonstrated that LD-1 significantly suppressed tumor growth (TGI = 47.64 %) at a dosage of 40 mg/kg, coupled none obvious adverse reactions w …

Melatonin inhibits tongue squamous cell carcinoma: Interplay of ER stress-induced apoptosis and autophagy with cell migration.

Tongue squamous cell carcinoma (TSCC) occupies a high proportion of oral squamous cell carcinoma. TSCC features high lymph node metastasis rates and chemotherapy resistance with a poor prognosis. Therefore, an effective therapy strategy is needed to improve patient prognosis. Melatonin (MT) is a natural indole compound shown to have anti-tumor effects in several cancers. This study focused on the role and mechanism of MT in TSCC cells. The results of the study suggest that MT could inhibit cell proliferation in CRL-1623 cells. Western blot analysis showed the down-regulate of cyclin B1 and the…

Trifluoromethyl quinoline derivative targets inhibiting HDAC1 for promoting the acetylation of histone in cervical cancer cells.

Cervical cancer is the leading cause of death among gynecological malignant tumors, especially due to the poor prognosis of patients with ad … /M phase, and regulated the expression of the apoptotic and cell cycle-related proteins Bcl-2, Bax, cyclin B1, and CDC2. We used online databases to obtain HDAC1 as one of the possible targets of FKL117 and the target binding and binding affinity were modeled by molecular docking. The results showed that FKL117 formed a hydrogen bond with HDAC1 and had good …