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Novel, thalidomide-like, non-cereblon binding drug tetrafluorobornylphthalimide mitigates inflammation and brain injury.

BACKGROUND: Quelling microglial-induced excessive neuroinflammation is a potential treatment strategy across neurological disorders, including traumatic brain injury (TBI), and can be achieved by thalidomide-like drugs albeit this approved drug class is compromised by potential teratogenicity. Tetrafluorobornylphthalimide (TFBP) and tetrafluoronorbornylphthalimide (TFNBP) were generated to retain the core phthalimide structure of thalidomide immunomodulatory imide drug (IMiD) class. However, the classical glutarimide ring was replaced by a bridged ring structure. TFBP/TFNBP were hence designed

The Ubiquitin-Proteasome System (UPS) as a Cancer Drug Target: Emerging Mechanisms and Therapeutics

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… Pharmaceuticals | Inmunoproteasome β5i/LMP7 | Epoxyketone | Irreversible | Unspecified | Preclinical | Immunological: Arthritis, rheumatoid, psoriasis, inflammatory bowel disease, lupus erythematosus | Verbrugge et al. ( 2012 ) Cancer: haematological, unspecified FV-162 | Fluorinov Pharma | Proteasome β5 | Fluorine …

Treating Primary Aldosteronism-Induced Hypertension: Novel Approaches and Future Outlooks.

Primary aldosteronism (PA) is the most common cause of secondary hypertension and is associated with increased morbidity and mortality when compared with blood pressure-matched cases of primary hypertension. Current limitations in patient care stem from delayed recognition of the condition, limited access to key diagnostic procedures, and lack of a definitive therapy option for nonsurgical candidates. However, several recent advances have the potential to address these barriers to optimal care. From a diagnostic perspective, machine-learning algorithms have shown promise in the prediction of P

Brazilian Nutritional Consensus in Hematopoietic Stem Cell Transplantation: children and adolescents.

The Brazilian Nutritional Consensus in Hematopoietic Stem Cell Transplantation: Children and Adolescents was developed by dietitians, physicians, and pediatric hematologists from 10 Brazilian reference centers in hematopoietic stem cell transplantation. The aim was to emphasize the importance of nutritional status and body composition during treatment, as well as the main characteristics related to patient´s nutritional assessment. This consensus is intended to improve and standardize nutrition therapy during hematopoietic stem cell transplantation. The consensus was approved by the Brazilian

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… around the mouth) | Riboflavin Angular cheilitis Cheilosis (red, swollen lips) Tongue | Scarlet, inflamed tongue | Nicotinic acid Magenta tongue (purplish red) | Riboflavin Swollen tongue | Niacin Atrophy and hypertrophy of the filiform papilla | Folic acid and vitamin B12 Teeth | Tooth enamel stains | Fluorine … Review. ( 120 ) Area of care | Actions Oral hygiene and basic oral care recommendations | Brush teeth 2 to 3 times a day with soft or extra-soft bristle brushes and fluorinated toothpaste (in case of burning, use kids’ toothpaste minimally flavored) Use dental floss after each meal Rinse mouth with gentle …

The cross talk of ubiquitination and chemotherapy tolerance in colorectal cancer.

Ubiquitination, a highly adaptable post-translational modification, plays a pivotal role in maintaining cellular protein homeostasis, encompassing cancer chemoresistance-associated proteins. Recent findings have indicated a potential correlation between perturbations in the ubiquitination process and the emergence of drug resistance in CRC cancer. Consequently, numerous studies have spurred the advancement of compounds specifically designed to target ubiquitinates, offering promising prospects for cancer therapy. In this review, we highlight the role of ubiquitination enzymes associated with c

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… Consequently, this section aims to elucidate the interplay between drug resistance and ubiquitination in CRC. 5-FU 5-FU, an essential component of palliative and adjuvant systemic chemotherapy for CRC, is a synthetic fluorinated pyrimidine analog that replaces hydrogen with fluorine at the C-5 position …

Applications of synthetic biology in medical and pharmaceutical fields.

Synthetic biology aims to design or assemble existing bioparts or bio-components for useful bioproperties. During the past decades, progresses have been made to build delicate biocircuits, standardized biological building blocks and to develop various genomic/metabolic engineering tools and approaches. Medical and pharmaceutical demands have also pushed the development of synthetic biology, including integration of heterologous pathways into designer cells to efficiently produce medical agents, enhanced yields of natural products in cell growth media to equal or higher than that of the extract

Recent Insights into the Creation of Histone Deacetylase Inhibitors for the Treatment of Human Diseases.

This review examines publications over the past two years devoted to histone deacetylase inhibitors for the treatment of cancer, diseases of the nervous, cardiovascular, digestive, and respiratory systems, and autoimmune diseases. The review covers various classes of histone deacetylase inhibitors depending on the zinc-binding group, in particular hydroxamic acids, benzamides, hydrazides, carboxylic acids, and cyclic peptides. The review pays special attention to the mechanisms of development of pathologies involving various isoforms of histone deacetylases. The review shows that, for the trea

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… In addition, micromolar (in the range of 25–27 μM) concentrations of compounds containing two fluorine atoms in the aromatic linker showed a highly effective antiproliferative effect on MDA-MB-231 TNBC cancer cells in the MTT test. …

Cardiovascular and Oncologic Considerations in Adult Hodgkin Lymphoma: JACC: CardioOncology State-of the-Art Review.

Classic Hodgkin lymphoma is a highly curable lymphoma that affects primarily younger patients. The therapeutic landscape has evolved and generally consists of varying combinations of chemotherapy and immunotherapy as well as radiation in selected cases. Although most patients are cured of their lymphoma, there is a risk for late treatment-related cardiotoxicity that affects long-term survival and quality of life in this population. Careful consideration of baseline cardiac function and risk factors should be undertaken prior to proceeding with anthracycline-based therapies or thoracic radiatio

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… Fluorine-18 fluorodeoxyglucose positron emission tomography (PET)/CT revealed fluorodeoxyglucose-avid disease in the mediastinum and bilateral axillary lymphadenopathy with no other sites of disease. …

Therapeutic Potential of Chlorogenic Acid in Chemoresistance and Chemoprotection in Cancer Treatment.

Chemotherapeutic drugs are indispensable in cancer treatment, but their effectiveness is often lessened because of non-selective toxicity to healthy tissues, which triggers inflammatory pathways that are harmful to vital organs. In addition, tumors' resistance to drugs causes failures in treatment. Chlorogenic acid (5-caffeoylquinic acid, CGA), found in plants and vegetables, is promising in anticancer mechanisms. In vitro and animal studies have indicated that CGA can overcome resistance to conventional chemotherapeutics and alleviate chemotherapy-induced toxicity by scavenging free radicals

Anti-Cancer Research Progress of Triptolide: Mechanisms of Action, Structural Modifications, Nanodelivery Systems and Clinical Challenges.

Triptolide is a bioactive diterpenoid lactone from traditional Chinese medicine with notable anti-tumor, immunosuppressive, and anti-inflammatory properties. However, its clinical utility is hampered by poor solubility, a narrow therapeutic index, and multi-organ toxicity. In response, extensive efforts have been made to improve its efficacy and safety profile. This review critically examines recent progress in Triptolide research, covering its mechanisms of action, derivative design, drug delivery systems, and cancer-specific applications. It also evaluates its clinical potential against panc

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… When the hydroxyl group at C-14 is substituted with a fluorine atom, the resulting compound also exhibits strong anticancer activity. The α-epoxide group at C-12 and C-13 is a crucial component of Triptolide bioactivity and represents another major site for structural modification. …

Functional pituitary adenoma imaging.

High-resolution pituitary MRI localises most pituitary neuroendocrine tumours (PitNETs), yet clinically important subgroups remain challenging: (i) very small functioning tumours, particularly corticotroph microadenomas, and (ii) post-operative remnants where scar, gland and tumour cannot be reliably separated. Functional imaging, specifically PET has matured into a problem-solving modality when conventional imaging is equivocal, provided it is used selectively and interpreted within a physiology-led framework. This review proposes an MRI-first, tiered imaging strategy and a pragmatic approach

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… Comparison of Gallium-68 and Fluorine-18 imaging characteristics in positron emission tomography. Appl Radiat Isot. 2013;76:55–62. 10.1016/j.apradiso.2012.06.034. 26. Van Weehaeghe D, Lapauw B, Fraioli F, Cecchin D, Verger A, Guedj E, et al. …

Next-Generation HDAC Inhibitors: Advancing Zinc-Binding Group Design for Enhanced Cancer Therapy.

Histone deacetylases (HDACs) are pivotal epigenetic regulators that control gene expression, cell proliferation, and differentiation, and their dysregulation is closely associated with the onset and progression of multiple cancers. The therapeutic importance of these enzymes is reflected by FDA approval of HDAC inhibitors for oncology indications. Despite this clinical success, most FDA-approved agents employ conventional zinc-binding groups (ZBGs) such as hydroxamic acid and 2-aminoanilide, which are frequently linked to metabolic instability, genotoxicity, and poor pharmacokinetic behavior.

Targeting the DNA Damage Response for Cancer Therapy.

Over the course of long-term evolution, cells have developed intricate defense mechanisms in response to DNA damage; these mechanisms play a pivotal role in maintaining genomic stability. Defects in the DNA damage response pathways can give rise to various diseases, including cancer. The DNA damage response (DDR) system is instrumental in safeguarding genomic stability. The accumulation of DNA damage and the weakening of DDR function both promote the initiation and progression of tumors. Simultaneously, they offer opportunities and targets for cancer therapeutics. This article primarily elucid

Unlocking the Microbial Symphony: The Interplay of Human Microbiota in Cancer Immunotherapy Response.

IntroductionThe emergence of cancer immunotherapy has revolutionized cancer treatment, offering remarkable outcomes for patients across various malignancies. However, the heterogeneous response to immunotherapy underscores the necessity of understanding additional factors influencing treatment efficacy. Among these factors, the human microbiota has garnered significant attention for its potential role in modulating immune response. Body: This review explores the intricate relationship between the human microbiota and cancer immunotherapy, highlighting recent advances and potential mechanisms u

Proceedings of ICIS SGCR-WIRES 2024, held jointly with the 23rd International Cancer Imaging Society Annual Conference, collaborating with the Singapore Radiological Society and College of Radiologists Singapore.

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… The resulting tumours were imaged with MRS (hyperpolarized [1-13C]pyruvate metabolism), MRI (Dynamic Contrast Enhanced (DCE)) and with PET (measurements o2f—deoxy-2-[fluorine-18]fluoro-D-glucose uptake). …

Controlled Drug Delivery Systems for Oral Cancer Treatment-Current Status and Future Perspectives.

Oral squamous cell carcinoma (OSCC), which encompasses the oral cavity-derived malignancies, is a devastating disease causing substantial morbidity and mortality in both men and women. It is the most common subtype of the head and neck squamous cell carcinoma (HNSCC), which is ranked the sixth most common malignancy worldwide. Despite promising advancements in the conventional therapeutic approaches currently available for patients with oral cancer, many drawbacks are still to be addressed; surgical resection leads to permanent disfigurement, altered sense of self and debilitating physiologica

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… Further, the composition of nanoparticles was confirmed by Energy-dispersive X-ray (EDX) spectroscopy showing formation of Na (Sodium), Y (Yttrium), F (Fluorine), Yb (Ytterbium), and Tm (Thulium) from the core nanocrystals and Ti (Titanium), Si (Silicon) and O (Oxygen) from the shell [ 107 ]. …

Novel therapeutic strategies targeting resistance mechanisms in hematologic malignancies: from BCL2 inhibition to immunomodulatory approaches.

BACKGROUND: Hematologic malignancies, including chronic lymphocytic leukemia (CLL), acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma (MM), are characterized by high relapse rates due to intrinsic and acquired drug resistance. Resistance mechanisms often involve dysregulation of apoptosis pathways, such as B-cell lymphoma 2 (BCL2) family overexpression, and immune evasion through microenvironment modulation. PURPOSE: This review synthesizes recent advances (2020-2025) in therapeutic strategies targeting these mechanisms, focusing on BCL2 inhibition and immunomodul

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… The molecular structure includes various carbon rings and elements like fluorine and nitrogen. | Servier / Novarti | • Highest Stage: Phase I (for hematologic malignancies) | ​ Chemical structure diagram of MIK665/S64315, labeled as an MCL-1 inhibitor. …

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

Selenium Compounds as Novel Potential Anticancer Agents.

The high number of new cancer incidences and the associated mortality continue to be alarming, leading to the search for new therapies that would be more effective and less burdensome for patients. As there is evidence that Se compounds can have chemopreventive activity, studies have begun to establish whether these compounds can also affect already existing cancers. This review aims to discuss the different classes of Se-containing compounds, both organic and inorganic, natural and synthetic, and the mechanisms and molecular targets of their anticancer activity. The chemical classes discussed

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… A simulation of molecular docking of diselenide 11 demonstrated that this compound selectively binds to the minor groove of DNA via hydrogen bonds in which fluorine atoms are involved. …

Intravenous Vitamin C for Cancer Therapy - Identifying the Current Gaps in Our Knowledge.

The use of intravenous vitamin C (IVC) for cancer therapy has long been an area of intense controversy. Despite this, high dose IVC has been administered for decades by complementary health care practitioners and physicians, with little evidence base resulting in inconsistent clinical practice. In this review we pose a series of questions of relevance to both researchers and clinicians, and also patients themselves, in order to identify current gaps in our knowledge. These questions include: Do oncology patients have compromised vitamin C status? Is intravenous the optimal route of vitamin C a

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… Fluorine-18-Labeled thymidine positron emission tomography (FLT-PET) as an index of cell proliferation after pharmacological ascorbate-based therapy. Radiat. Res. 185 31 – 38 . 10.1667/RR14203.1 26720803 PMC4720529 Cimmino L. Dolgalev I. Wang Y. Yoshimi A. Martin G. H. Wang J. ( 2017 ). …