Inhibitors - Science topic

Monoamine oxidase B (MAOB) is an enzyme primarily involved in the degradation of dopamine and other monoamines. It plays a significant role in neurodegenerative diseases, including Parkinson's and Alzheimer's, as well as psychiatric disorders. MAOB inhibitors are widely used as therapeutic agents in the treatment of Parkinson's disease. This review...

1991. Inhibition of early steps of de novo fatty-acid biosynthesis by different xcnobiotica.-Physiol. Plant. 81: 251-255. The importance of the early steps of de novo fatty-acid biosynthesis is discussed in terms of rate-limiting enzymic reactions with respect to their inhibition by xenobiotics. The inhibitory spectra of two classes of graminicide...

Purpose The management of the coexistence of chronic obstructive pulmonary disease (COPD) and atrial fibrillation (AF) remains unclear due to a lack of evidence. This study aimed to find the effect of beta-blockers and renin-angiotensin-aldosterone system inhibitors (RAASi) in this special population. Patients and Methods We designed an observatio...

Objective This Phase I study evaluated the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of BGT-002, a novel ATP-citrate lyase (ACLY) inhibitor, in healthy Chinese adults. Methods This study included three parts: Part I (single-ascending-dose study), Part II (multiple-ascending-dose study), and Part III (food effect study)....

The lost of family members caused by COVID-19 will result in deep anguish. The fact that other family members should self-isolate and the strict burial procedures are inhibitors for them to get involved in said burial, as a symbol of their last goodbyes. This article explains how a person grieves after the death of a family member because of COVID-...

AMP‐activated protein kinase (AMPK) is the master regulator of cellular and organismal energy homeostasis, playing an essential role in modulating metabolism and other cellular processes. Substantial efforts have been made to develop pharmacological modulators of AMPK activity due to their therapeutic potential against various diseases. Measuring A...

Although many studies have investigated the expression and role of nitric oxide (NO) in various diseases, it remains unclear whether NO has a beneficial or detrimental impact on otitis media. This review examines the literature on the expression and role of NO in different forms of otitis media, including acute otitis media, otitis media with effus...

This case report presents a rare occurrence of adrenal insufficiency induced by Zytiga (abiraterone acetate) in a patient with high-risk localized prostatic adenocarcinoma. Abiraterone acetate is a potent, selective and irreversible CYP17A1 inhibitor and is commonly used in the treatment of prostate cancer, but it can cause various endocrine side e...

In the original publication [...]

The carbapenemase-producing Gram-negative organisms represent an urgent clinical and public health concern, as they have been associated with increased mortality and high dissemination in healthcare settings. Although overall incidence rates of infections sustained by metallo-β-lactamase (MβL)-producers have remained lower than those sustained by o...

Advancements in immunotherapy, the phenomenon of hyperprogression in cancer patients, have garnered increasing attention. We herein report a case of acute adult T-cell leukemia/lymphoma (ATL) that developed after administration of the PD-L1 inhibitor durvalumab in a patient with lung cancer. Although the patient was a carrier of human T-cell leukem...

This study evaluates the corrosion inhibition potential of three molecules—TPP, TBP, and TFP—by analyzing their electronic properties and interaction energies with aluminum surfaces (Al (111), Al (110), and Al (100)). Key electronic parameters such as the Energy of Highest Occupied Molecular Orbital (E-HOMO), Energy of Lowest Unoccupied Molecular O...

Inosine-5'-monophosphate dehydrogenase 1 (IMPDH1) is a key enzyme in purine nucleotide biosynthesis, catalyzing the rate-limiting conversion of inosine monophosphate (IMP) to xanthosine monophosphate (XMP). IMPDH1 plays a crucial role in cellular proliferation, immune function, and cancer progression. This review explores the structure, enzymatic a...

Effectiveness of sodium-glucose cotransporter type 2 inhibitors and urate-lowering agents in patients with gout: data from a single-center specialised clinic.

https://www.jnephropharmacology.com/Article/npj-12762 Maghsoudi A, Dehghani Mobarakeh M. Immune checkpoint inhibitors and IgA nephropathy; A rare side effect. J Nephropharmacol. 2025;14(2):e12762x. DOI: 10.34172/npj.2025.12762.

Although phosphodiesterase 4 (PDE4) inhibitors have reached the clinic, their lack of selectivity for PDE4 enzyme isoforms leads to documented side effects. Building in enzyme selectivity has proved difficult because all PDE4 enzymes share highly conserved catalytic domains. The report by Sin et al. describes a novel approach in which a potent PDE4...

Protein arginylation, regulated by arginyltransferase 1 (ATE1), is crucial for controlling various cellular processes in eukaryotes by affecting protein stability, function, and interactions. Due to its significant role, ATE1 has become an attractive target for therapeutic interventions, especially for conditions like obesity and cancer. However, n...

This multicenter retrospective study examines 18 patients with difficult‐to‐treat inflammatory bowel diseases who received advanced combination treatment (ACT) with selective JAK1 inhibitors and biologics, totaling 11.8 patient‐years of exposure. Treatment was discontinued in three patients due to adverse events. At 3 months, 77.8% achieved steroid...

Philadelphia-chromosome negative (Ph-) myeloproliferative neoplasms (MPNs) carry a variable risk of progression towards accelerated phase (AP) or blast phase (BP)1,2. Progression to MPNAP/BP is associated with poor outcomes; our group previously characterized outcomes of MPNAP/BP in the current era of myeloid therapies and reported a median overall...

This multicenter study aimed to investigate the efficacy and safety of PD‐1/PD‐L1 inhibitors plus chemotherapy (ICI‐Chemo group) versus chemotherapy alone (Chemo group) for patients with cancer of unknown primary (CUP) in the first‐line setting. We included patients with unfavorable CUP across four medical centers in China. Between January 2014 and...

The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) regulates transcription in response to ligand binding at an orthosteric pocket within the ligand-binding domain (LBD). We previously showed that two covalent ligands, T0070907 and GW9662—extensively used as PPARγ inhibitors to assess off-target activity—weaken but do not...

Inhibitor of Nuclear Factor Kappa-B Kinase Subunit Beta (IKBKB) plays a crucial role in immune response by mediating the activation of the NF-κB signaling pathway, which regulates inflammation, immune responses, and cell survival. Mutations and dysregulation of IKBKB have been linked to various cancers, autoimmune diseases, and metabolic disorders....

Background Immune checkpoint inhibitors (ICIs) are responsible for causing immune-related adverse events (irAEs). The frequency and severity of irAEs depend on various factors, but the role of the molecule used remains unclear. Our aim was to assess the comparative safety profile of different programmed cell death-1 inhibitors (anti-PD1) and progra...

The cell cycle is a crucial process for cell proliferation, differentiation, and development. Numerous genes and proteins play pivotal roles at specific cell cycle stages to ensure precise regulation of these events. Understanding the stage-specific regulations of the cell cycle requires the accumulation of cell populations at desired cell cycle st...

This news section offers Cancer readers timely information on events, public policy analysis, topical issues, and personalities. In this issue, findings show that the effectiveness of blood‐based screening tests eroded substantially as the follow‐up rate with colonoscopy decreased. Also, patients treated with immune checkpoint inhibitors have an in...

A library of known aspartic protease inhibitors was screened to identify compounds that inhibit plasmepsin V from Plasmodium vivax. This screen revealed compounds with an imino‐pyrimidinone‐fused pyrrolidine (IPF) scaffold that exhibited sub‐micromolar inhibitory activity against plasmepsin V. Further screening of IPF analogs against the related as...

Objective The objective of this study was to assess the effectiveness and safety of CDK4/6 inhibitors in the treatment of hormone receptor-positive (HR+) breast cancer by using meta-analysis. Methods To gather comprehensive and reliable data for our analysis, we systematically searched multiple databases for relevant studies. We utilized RevMan5.3...

Protein aggregation is a critical factor in the development and progression of several human diseases, including Alzheimer's disease (AD), Huntington's disease, Parkinson's disease, and type 2 diabetes. Among these conditions,...

Social desirability affects several aspects of human life. However, the neuropsychological mechanisms underlying individual differences in social desirability remain unclear. This study explored the neuroanatomical basis of individual differences in social desirability using regional gray matter density (rGMD) as a brain indicator in a sample of 15...

We present a case of oligohydramnios induced by NSAID use (Etoricoxib and Diclofenac) in the second trimester. A 20-year-old primigravidae with an uncomplicated early trimester, was advised at 21 weeks to take Etoricoxib for five days due to knee bursitis after which she self-medicated with Diclofenac for a week. Due to complaints of reduced fetal...

Background: Administration of SGLT2 inhibitors leads to a reduction in the dosage of loop diuretics in heart failure (HF) patients; however, it is unclear in what patients the dosage can be reduced. We investigated the factors related to the reduction in loop diuretics in patients who have started receiving dapagliflozin, an SGLT2 inhibitor. Method...

Immune checkpoint inhibitors are increasingly being utilized for the treatment of advanced neoplastic disease, and Sintilimab as a selective anti–PD-1 antibody that inhibits interactions between PD-1 and its ligand, is a typical representative of them. Among all the adverse effects(AEs) of sintilimab, skin AEs had affected many people. Though excee...

Apart from the genetic mutations in mutant EGFR and KRAS, and ALK fusion gene that characterize NSCLC, several other genetic mutations also distinguish NSCLC. The paper reviews the pathogenic mechanisms of these gene alterations and the principles generalized for new generations of agents against EGFR, KRAS, and ALK TKIs. Ways to future reduce resi...

Induction chemo‐immunotherapy has emerged as a potential treatment option for locoregionally advanced nasopharyngeal carcinoma (LANPC). This study aimed to evaluate the efficacy and safety of camrelizumab combined with modified TPF (nab‐paclitaxel, cisplatin, and S‐1) as induction chemo‐immunotherapy in LANPC. Patients with stage T1‐4N2‐3M0 NPC who...

The emergence and spread of artemisinin-resistant, malaria-causing P. falciparum provide the impetus for the development of novel antimalarials. Pantothenamides are potent inhibitors of malaria parasite proliferation, however their clinical use is hindered by pantetheinase-mediated degradation in human serum. Here we report the synthesis and biolog...

Anifrolumab, a type I interferon receptor inhibitor, is commonly used in systemic lupus erythematosus (SLE), particularly in cutaneous and musculoskeletal symptoms. However, its efficacy in patients with severe hematologic manifestations remains undocumented. We report a case of hemophagocytic lymphohistiocytosis (HLH) secondary to SLE, successfull...

This study confirms that immersion time and inhibitor concentration significantly affect the corrosion rate of galvanized steel in seawater. Without an inhibitor (0% concentration), the corrosion rate progressively increases, reaching a maximum of 0.4395 mpy after 30 days. In contrast, the addition of jackfruit seed extract effectively reduces corr...

Bronchial asthma is a complex and heterogeneous disease with ongoing airway inflammation and increased airway responsiveness. Key characteristics of the disease include persistent airway inflammation, airway hyperresponsiveness, and airway remodeling. Asthma’s chronic and recurrent characteristics contribute to airway remodeling and inflammation, w...

Ribociclib, a cyclin-dependent kinase (CDK) 4/6 inhibitor, is widely used in the treatment of metastatic breast cancer. However, its dermatologic adverse effects, particularly vitiligo-like lesions, have been recently reported. The pathomechanisms underlying these lesions remain unclear, but immune-mediated melanocyte destruction has been proposed....

Heart failure with preserved ejection fraction has attracted more and more attention in recent years because its mechanism is different from heart failure with reduced ejection fraction, and accounts for a high proportion of heart failure. At present, there are only sodium-glucose cotransporter 2 inhibitors for their IA drugs in the guidelines. The...

Although benzbromarone is a highly potent inhibitor of URAT1, the toxicity of its metabolite has led to the restricted use. In this study, to decrease its toxicity, thirteen benzbromarone derivatives were designed and synthesized via blocking metabolic site. Among them, most of the compounds had moderate to strong inhibitory activity against URAT1,...

Purpose To evaluate alternative ibrutinib dosing regimens that maintain Bruton’s tyrosine kinase (BTK) receptor occupancy over the entire dosing interval for CLL patients using a model-based approach. Methods Ibrutinib inhibits B-cell proliferation via irreversible binding of BTK. As IC50 is not an appropriate parameter to describe the potency of...

In this study, various phosphate glasses (PGs) within the CaO-Na2O-P2O5 and SiO2-CaO-Na2O-P2O5 systems were synthesized using both conventional and microwave melt-quenching techniques. The physical, thermal, and structural properties of these phosphate glasses, as well as their dissolution behaviors under varying temperatures and solvent conditions...

There is an increasing recognition that comprehensive tumour profiling (CTP) represents an important adjunct to the diagnosis of malignancy providing not only an assessment of how many mutations there are in any given tumour which reflects the probability of immune checkpoint inhibitor success, but also which mutations are associated with targeted...

Breast cancer is the most common type of cancer in women and the second leading cause of death by cancer. Despite recent advances, the mortality rate remains high, underlining the need to develop new therapeutic approaches. The complex interaction between cancer cells and the tumor microenvironment (TME) is crucial in determining tumor progression,...

Purpose of Review Treatment-emergent neuroendocrine prostate cancer (NEPC) is aggressive and lethal. As androgen receptor signaling inhibitors (ARSIs) are increasingly used in earlier disease settings, treatment-emergent NEPC becomes more prevalent, and effective therapies are urgently needed. The purpose of this review was to summarize recent prog...

Objective Relapsed/refractory gestational trophoblastic neoplasia (RR‐GTN) presents a significant therapeutic challenge, with limited options available for patients who fail first‐line treatments. In the present study we describe a few unique cases of RR‐GTN and various options available for such situations. Methods We identified three cases of RR...

Modulation of enzyme activity by metabolites represents the most efficient and rapid way of controlling metabolism. Investigating enzyme–metabolite interactions can deepen our understanding of metabolic control and aid in identifying enzyme modulators with potential therapeutic applications. These interactions vary in strength, with dissociation co...

Cabozantinib is an oral multikinase inhibitor approved for treatment in metastatic renal cell carcinoma (RCC). We conducted a phase 2, nonrandomized, single-arm clinical trial (NCT04022343) of cabozantinib treatment for 12 weeks in 17 patients with locally advanced, biopsy-proven, nonmetastatic clear cell RCC before surgical resection. The primary...

Introduction As the use of immune checkpoint inhibitors (ICIs) continues to expand, it is important to be mindful of rare but serious side effects such as myocarditis. Multiple analyses of adverse effect databases have demonstrated an association between ICIs and myocarditis; however, given the rapid implementation of therapeutic use, introduction...

Background/Objectives: The risk of fractures associated with immune checkpoint inhibitors (ICIs) is increasing; however, the relationship between fracture risk and potential factors, such as osteoporosis and hyperthyroidism, remains unclear. Methods: Using VigiBase, the World Health Organization's global pharmacovigilance database, we investigated...

The goal of this work is to limit mild steel corrosion in an HCl solution by employing an ionic liquid (1-butyl-1-methylpyrolidinum tetrafluoroborate) as an inhibitor. To determine the molecular components and functional groups, the ionic liquids of 1-butyl-1-methylpyrolidinum tetrafluoroborate were produced and described. The quantization method w...

Immune checkpoint inhibitors (ICI), have transformed the management of several types of cancers; however, immune‐related adverse events (irAEs) may cause treatment interruptions, chronic toxic effects, and death. Elderly patients are at high risk of cancer. Compared with traditional chemotherapy, immunotherapy has become a better alternative choice...

Background: New triazoloquinazoline derivatives were synthesized to explore their cytotoxic activity on various cancer cell lines, prompted by the need for effective anticancer agents. Research design and methods: All synthesized compounds were confirmed by spectroscopic methods and tested in vitro for their inhibitory activities against hepatoc...

Aboriginal people in remote Northern Territory communities experience the highest burden of type 2 diabetes (T2D) globally. Sodium–glucose cotransporter‐2 inhibitors (SGLT2i) improve cardiac and renal outcomes in selected populations. However, safety in this context is unknown. We investigated SGLT2i use and outcomes in remote Aboriginal people wit...

Staphylococcus aureus is a bacterium classified among the ESKAPE pathogens, which are anticipated to pose a significant global health emergency in the coming decades. The FabI enzyme, present in both Gram-positive and Gram-negative bacteria, is a key enzyme involved in fatty acid synthesis II (FAS-II). In this study, we utilized transformation rule...

Cyclin E1 (CCNE1) amplification is associated with poor prognosis of ovarian carcinomas across histological subtypes. Inhibitors targeting PLK1 or WEE1 are emerging as promising therapeutic agents for cancer treatment that disrupt the critical G2/M checkpoint, leading to cancer cell death. However, biomarkers that predict the response to these inhi...

Objetives We aimed to examine the effects of newly started SGLT2 inhibitors on thiamine levels. Background High glucose in the renal tubular epithelium causes increased renal clearance of thiamine. Therefore, we hypothesized that glucosuria induced by SGLT2 inhibitors may result in thiamine deficiency. Methods The SGLT2 inhibitors group included...

Over the past several years, the therapeutic landscape for patients with advanced, unresectable, or metastatic hepatocellular carcinoma has been transformed by the incorporation of checkpoint inhibitor immunotherapy into the treatment paradigm. Frontline systemic treatment options have expanded beyond anti-angiogenic tyrosine kinase inhibitors, suc...