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Small molecule inhibitors targeting the cancers.

Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer. Due to their advantages in a wide range of targets, convenient medication, and the ability to penetrate into the central nervous system, many efforts have been devoted to developing more small molecule inhibitors. To date, 88 small molecule inhibitors have been approved by the United States Food and Drug Administration to treat cancers. Despite remarkable progress, small molecule inhibitors in cancer treatme

ESMO/ASCO Recommendations for a Global Curriculum in Medical Oncology Edition 2023.

The European Society for Medical Oncology (ESMO) and ASCO are publishing a new edition of the ESMO/ASCO Global Curriculum (GC) with contributions from more than 150 authors. The purpose of the GC is to provide recommendations for the training of physicians in medical oncology and to establish a set of educational standards for trainees to qualify as medical oncologists. This edition builds on prior ones in 2004, 2010, and 2016 and incorporates scientific advances and input from an ESMO ASCO survey on GC adoption conducted in 2019, which revealed that GC has been adopted or adapted in as many a

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… resistance Give examples of certain pathognomonic chromosomal translocations that define various lymphoid malignancies and how this can be used for diagnosis Determine the importance of tumour suppressor gene functional deficiency in terms of DNA repair mechanisms as a marker for sensitivity to poly (ADP-ribose … receptors for neuroendocrine tumours, oestrogen receptors for breast cancer, and amino acid transport and metabolism for imaging brain and other cancer, and investigational targets including fibroblast activating protein, human epidermal growth factor receptor 2 (HER2), immunotherapy targets, poly (ADP-ribose …

Emerging and underexplored ginsenosides in cancer therapy (2020-2025): Beyond cytotoxic mechanisms.

Ginsenosides from Panax plants have long been studied as potential anticancer agents. In earlier years, most research focused on a few well-known ginsenosides that showed strong direct cytotoxicity, such as Rg3 and Rh2. As a result, many other ginsenosides were considered less active and received limited attention. However, studies published between 2020 and 2025 indicate that several previously underexplored ginsenosides also exhibit meaningful anticancer activity. These compounds often do not function as strongly cytotoxic agents. Instead, they act through broader and more indirect mechanism

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… species PD-1 | Programmed cell death protein 1 PD-L1 | Programmed death-ligand 1 STAT3 | Signal transducer and activator of transcription 3 IL-6 | Interleukin-6 VEGF | Vascular endothelial growth factor HIF-1α | Hypoxia-inducible factor-1 alpha MDSC | Myeloid-derived suppressor cell PARP | Poly(ADP-ribose …

Bioactivity of the Genus Turnera: A Review of the Last 10 Years.

Turnera is a genus of plants whose biological activity has been widely studied. The importance of this genus, particularly Turnera diffusa, as a source of treatment for various conditions is evidenced by the large number of new studies that have evaluated its biological activity. Accordingly, the objective of this review was to compile the information published in the last ten years concerning the biological activities reported for Turnera spp. The present work includes 92 publications that evaluate 29 bioactivities and toxicological and genotoxic information on five species of this genus. Amo

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… Inhibitory Activity of Phosphodiesterase 5 (PDE-5) Phosphodiesterases (PDEs) are a family of enzymes responsible for cleaving the 3′-ribose-phosphate bond of cyclic adenosine monophosphate and cyclic guanosine monophosphate. …

Current State and Future Challenges for PI3K Inhibitors in Cancer Therapy.

The phosphoinositide 3 kinase (PI3K)-protein kinase B (PKB/AKT)-mammalian target of the rapamycin (mTOR) axis is a key signal transduction system that links oncogenes and multiple receptor classes which are involved in many essential cellular functions. Aberrant PI3K signalling is one of the most commonly mutated pathways in cancer. Consequently, more than 40 compounds targeting key components of this signalling network have been tested in clinical trials among various types of cancer. As the oncogenic activation of the PI3K/AKT/mTOR pathway often occurs alongside mutations in other signalling

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… Given the synergy between poly(ADP-ribose) polymerase (PARP) and PI3Ki in preclinical data, Trap et al., evaluated capivasertib and the PARP inhibitor (PARPi) olaparib in a phase 1 study [ 91 ]. They observed that capivasertib was safe and well tolerated. …

Metastatic Breast Cancer: Review of Emerging Nanotherapeutics.

Metastases of breast cancer (BC) are often referred to as stage IV breast cancer due to their severity and high rate of mortality. The median survival time of patients with metastatic BC is reduced to 3 years. Currently, the treatment regimens for metastatic BC are similar to the primary cancer therapeutics and are limited to conventional chemotherapy, immunotherapy, radiotherapy, and surgery. However, metastatic BC shows organ-specific complex tumor cell heterogeneity, plasticity, and a distinct tumor microenvironment, leading to therapeutic failure. This issue can be successfully addressed b

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… BRCA-mutated TNBCs are typically treated with poly ADP ribose polymerase (PARP) inhibitors, such as olaparib or talazoparib. Hormone therapies and chemotherapeutics are also very beneficial in treating BRCA-mutated cancers [ 30 , 31 ]. …

An Appraisal of the Oleocanthal-Rich Extra Virgin Olive Oil (EVOO) and Its Potential Anticancer and Neuroprotective Properties.

Dietary consumption of olive oil represents a key pillar of the Mediterranean diet, which has been shown to exert beneficial effects on human health, such as the prevention of chronic non-communicable diseases like cancers and neurodegenerative diseases, among others. These health benefits are partly mediated by the high-quality extra virgin olive oil (EVOO), which is produced mostly in Mediterranean countries and is directly made from olives, the fruit of the olive tree (Olea europaea L.). Preclinical evidence supports the existence of antioxidant and anti-inflammatory properties exerted by t

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… Authors also documented that oleocanthal inhibited colony formation, induced apoptosis (confirmed by PARP [Poly (ADP-ribose) polymerase] cleavage, activation of caspases 3/7 and chromatin condensation), induced the expression of γH2AX histone (a well-known molecular marker of DNA damage), and led to …

Analysis of medical malpractice liability disputes related to novel antineoplastic drugs and research on risk prevention and control strategies.

OBJECTIVE: To investigate the general characteristics of litigation cases of medical malpractice liability disputes (MMLDs) related to novel antineoplastic drugs (NADs), the drugs involved, as well as the common types of medical errors related to NADs and their damages in the process of diagnosis and treatment, with the aims of improving the level of rational medication use in the clinical application of NADs and actively prevent medical disputes. METHODS: The China Judgments Online was searched for the cause of action using the key word "MMLDs" along with the name of 77 kinds of NADs. A tota

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… viral oncogene homolog B1; BTKI = Bruton’s tyrosine kinase inhibitors; EGFR = Epidermal growth factor receptor; HER = Human epidermal growth factor receptor; JAK = Janus kinases; STAT = Signal transducer and activator of transcription; MET = Mesenchymal epithelial transition factor; PARP = Poly(ADP-ribose …

Review of imaging techniques for evaluating morphological and functional responses to the treatment of bone metastases in prostate and breast cancer.

Bone metastases are very common complications associated with certain types of cancers that frequently negatively impact the quality of life and functional status of patients; thus, early detection is necessary for the implementation of immediate therapeutic measures to reduce the risk of skeletal complications and improve survival and quality of life. There is no consensus or universal standard approach for the detection of bone metastases in cancer patients based on imaging. Endorsed by the Spanish Society of Medical Oncology (SEOM), the Spanish Society of Medical Radiology (SERAM), and the

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… In this sense, quantitative biomarkers derived from diffusion-weighted sequences, such as ADC measures and tumor volume measured by means of DWI, correlate with serum biomarkers and clinical response to olaparib (inhibitor of the poly ADP-ribose polymerase enzyme) in patients with advanced PCa [ 108 …

Hypoxia-Inducible Factor-1: A Novel Therapeutic Target for the Management of Cancer, Drug Resistance, and Cancer-Related Pain.

Hypoxia-inducible factor-1 (HIF-1) is a key transcription factor that regulates the transcription of many genes that are responsible for the adaptation and survival of tumor cells in hypoxic environments. Over the past few decades, tremendous efforts have been made to comprehensively understand the role of HIF-1 in tumor progression. Based on the pivotal roles of HIF-1 in tumor biology, many HIF-1 inhibitors interrupting expression, stabilization, DNA binding properties, or transcriptional activity have been identified as potential therapeutic agents for various cancers, yet none of these inhi

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… The repair of SSBs is carried out by poly(ADP-ribose) polymerase 1 (PARP-1) or by the regulation of the XPA and XPD genes: the key enzymes involved in the base excision repair process. …

ESMO/ASCO Recommendations for a Global Curriculum in Medical Oncology Edition 2023.

The European Society for Medical Oncology (ESMO) and ASCO are publishing a new edition of the ESMO/ASCO Global Curriculum (GC) with contributions from more than 150 authors. The purpose of the GC is to provide recommendations for the training of physicians in medical oncology and to establish a set of educational standards for trainees to qualify as medical oncologists. This edition builds on prior ones in 2004, 2010, and 2016 and incorporates scientific advances and input from an ESMO/ASCO survey on GC adoption conducted in 2019, which revealed that GC has been adopted or adapted in as many a

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… resistance Give examples of certain pathognomonic chromosomal translocations that define various lymphoid malignancies and how this can be used for diagnosis Determine the importance of tumour suppressor gene functional deficiency in terms of DNA repair mechanisms as a marker for sensitivity to poly (ADP-ribose … receptors for neuroendocrine tumours, oestrogen receptors for breast cancer, and amino acid transport and metabolism for imaging brain and other cancer, and investigational targets including fibroblast activating protein, human epidermal growth factor receptor 2 (HER2), immunotherapy targets, poly (ADP-ribose …

BCL-2 and BCL-xL in Cancer: Regulation, Function, and Therapeutic Targeting.

The BCL-2 family of proteins plays a central role in the regulation of apoptosis, with BCL-2 and BCL-xL representing two of its most prominent antiapoptotic members. This review explores the molecular regulation of BCL-2 and BCL-xL genes, emphasizing the structural domains that define the functions of the broader BCL-2 family. Beyond their canonical roles in preventing mitochondrial outer membrane permeabilization, both proteins contribute significantly to cancer development. Their overexpression enhances invasiveness and tumor progression, supports angiogenesis, and critically modulates cellu

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… Furthermore, prostate cancer cells overexpressing BCL-2 are susceptible to Poly (ADP-Ribose) polymerase (PARP) inhibition combined with radiotherapy. Overexpression of BCL-2 blocks Ku80 from entering the nucleus. Ku80 is essential for the non-homologous end joining DNA repair pathway. …

" Nucleolus in Human Beasons: Ribosome Biogenesis " , " Nucleolar Survey " и " Terrapeutic Opportunities " .

Nucleolus превратился в динамичную и многофункциональную субядерную органилию, интегрирующую рибосомный биогенез с клеточным ростом и сигнализацией стресса. Регулирование нуклеолярной функции все чаще признается в качестве главного движителя человеческих заболеваний, связывающего изменённое рибосомное производство и нуклеолярное наблюдение с раком, рибосомопатиями, синдромами преждевременного старения, нейродегенерацией и иммунными расстройствами. В этом обзоре мы интегрируем структурные, молекулярные и болезнетворные перспективы нуклеолярной биологии для определения того, как рипосомный биоге

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… Pre-rRNAs associate co-transcriptionally with RPs and snoRNPs, undergoing folding, chemical modification (primarily 2′-O-ribose methylation and pseudouridylation catalysed by C/D and H/ACA box snoRNPs), and sequential endo- and exonuclease cleavage at multiple spacer sites to generate processing intermediates … For example, poly(ADP-ribose) polymerase 1 (PARP1) associates with the NoRC subunit TIP5 to silence rDNA transcription and interacts with the RecQ helicases Bloom syndrome protein (BLM) and Werner syndrome helicase (WRN) [ 140 , 141 , 142 ]. …

Ocular toxicity associated with antibody-drug conjugates in cancer therapy: a comprehensive review.

Ocular toxicity from anti-cancer drugs is frequently overlooked, largely because it is non-life-threatening, whereas clinical priorities often center on adverse events that pose immediate risks to survival. Antibody-drug conjugates (ADCs) have emerged as an important therapeutic modality in oncology, offering potent cytotoxicity against tumor cells through the targeted delivery of payloads. However, this potency also introduces a spectrum of toxicities, among which ocular toxicity has gained increasing attention. ADC-induced ocular toxicity can impair visual function and significantly compromi

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… Studies reporting any ocular AEs associated with ADCs were included, whereas those evaluating ADCs in combination with ICIs, EGFR inhibitors, human epidermal growth factor receptor 2 (HER2) inhibitors, ALK inhibitors, BCR-ABL inhibitors, phosphoinositide 3-kinase/protein kinase B inhibitors and poly (ADP-ribose …

Ferroptosis: Frenemy of Radiotherapy.

Recently, it was established that ferroptosis, a type of iron-dependent regulated cell death, plays a prominent role in radiotherapy-triggered cell death. Accordingly, ferroptosis inducers attracted a lot of interest as potential radio-synergizing drugs, ultimately enhancing radioresponses and patient outcomes. Nevertheless, the tumor microenvironment seems to have a major impact on ferroptosis induction. The influence of hypoxic conditions is an area of interest, as it remains the principal hurdle in the field of radiotherapy. In this review, we focus on the implications of hypoxic conditions

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… Well-established radiosensitizers, like poly ADP-ribose polymerase (PARP)-inhibitors, are nowadays considered to enhance radio-efficacy via ferroptosis stimulation, in addition to their traditional mechanism of action, which involves inhibiting DNA repair within cancer cells. …

Clinical outcomes of chemotherapy in cancer patients with different ethnicities.

BackgroundChoosing the most effective chemotherapeutic agent with safest side effect profile is a common challenge in cancer treatment. Although there are standardized chemotherapy protocols in place, protocol changes made after extensive clinical trials demonstrate significant improvement in the efficacy and tolerability of certain drugs. The pharmacokinetics, pharmacodynamics, and tolerance of anti-cancer medications are all highly individualized. A driving force behind these differences lies within a person's genetic makeup.Recent findingsPharmacogenomics, the study of how an individual's g

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… ‐125, cancer antigen 125; EGFR, epidermal growth factor receptor; ERG, erythroblast‐transformation‐specific (ETS) Related Gene; HER2, human epidermal growth factor receptor 2; KRAS, Kirsten rat sarcoma viral oncogene; MSI, microsatellite instability; PI3K, phosphoinositide 3‐kinases; PRAP, poly ADP ribose …

Malignant mesothelioma tumours: molecular pathogenesis, diagnosis, and therapies accompanying clinical studies.

The pathetic malignant mesothelioma (MM) is a extremely uncommon and confrontational tumor that evolves in the mesothelium layer of the pleural cavities (inner lining- visceral pleura and outer lining- parietal pleura), peritoneum, pericardium, and tunica vaginalis and is highly resistant to standard treatments. In mesothelioma, the predominant pattern of lesions is a loss of genes that limit tumour growth. Despite the worldwide ban on the manufacture and supply of asbestos, the prevalence of mesothelioma continues to increase. Mesothelioma presents and behaves in a variety of ways, making dia

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… The therapy with a combination of a poly ADP ribose polymerase (PARP) blocker with Ig antibody for the platin-sensitive condition, a vascular endothelial growth factor (VEGF) blocker with a programmed cell death ligand-1 (PDL1) blocker for PDL1 upregulation positive conditions, an AXL blocker combined …

Definitions, Biology, and Current Therapeutic Landscape of Myelodysplastic/Myeloproliferative Neoplasms.

Myelodysplastic/myeloproliferative neoplasms (MDS/MPN) are hematological disorders characterized by both proliferative and dysplastic features. According to the 2022 International Consensus Classification (ICC), MDS/MPN consists of clonal monocytosis of undetermined significance (CMUS), chronic myelomonocytic leukemia (CMML), atypical chronic myeloid leukemia (aCML), MDS/MPN with SF3B1 mutation (MDS/MPN-T-SF3B1), MDS/MPN with ring sideroblasts and thrombocytosis not otherwise specified (MDS/MPN-RS-T-NOS), and MDS/MPN-NOS. These disorders exhibit a diverse range of genetic alterations involving

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… Poly (ADP-Ribose) Polymerase Inhibitor Hypersensitivity in Aggressive Myeloproliferative Neoplasms. Clin. Cancer Res. 2016;22:3894–3902. doi: 10.1158/1078-0432.CCR-15-2351. 90. Dréan A., Lord C.J., Ashworth A. PARP inhibitor combination therapy. Crit. Rev. Oncol. …

Proteasome Inhibitors and Their Potential Applicability in Osteosarcoma Treatment.

Osteosarcoma (OS) is the most common type of bone cancer, with ~30% of patients developing secondary/metastatic tumors. The molecular complexity of tumor metastasis and the lack of effective therapies for OS has cultivated interest in exploiting the proteasome as a molecular target for anti-cancer therapy. As our understanding towards the behavior of malignant cells expands, it is evident that cancerous cells display a greater reliance on the proteasome to maintain homeostasis and sustain efficient biological activities. This led to the development and approval of first- and second-generation

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… Downstream signaling of RelA activity then increases Bcl-2 expression, while also suppressing the apoptotic-related genes poly-ADP ribose polymerase (PARP) and caspase-3 [ 44 ]. …

Non-Curcuminoids from Turmeric and Their Potential in Cancer Therapy and Anticancer Drug Delivery Formulations.

Over the past decades curcuminoids have been extensively studied for their biological activities such as antiulcer, antifibrotic, antiviral, antibacterial, antiprotozoal, antimutagenic, antifertility, antidiabetic, anticoagulant, antivenom, antioxidant, antihypotensive, antihypocholesteremic, and anticancer activities. With the perception of limited toxicity and cost, these compounds forms an integral part of cancer research and is well established as a potential anticancer agent. However, only few studies have focused on the other bioactive molecules of turmeric, known as non-curcuminoids, wh

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… This initiation led to the cleavage of poly (ADP-ribose) polymerase (PARP) colorectal adenocarcinoma and Hela cells along with the activation of caspase-3. …