A5011240907- Drug Transport and Resistance Mechanisms
- Pharmacological Effects and Toxicity Studies
- Pharmacogenetics and Drug Metabolism
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Liver Disease Diagnosis and Treatment
- Metabolism and Genetic Disorders
- HIV/AIDS drug development and treatment
- Antiplatelet Therapy and Cardiovascular Diseases
- Adenosine and Purinergic Signaling
- Drug-Induced Hepatotoxicity and Protection
- Hepatitis C virus research
- Colorectal Cancer Treatments and Studies
- Lung Cancer Treatments and Mutations
- Folate and B Vitamins Research
- Computational Drug Discovery Methods
- Cancer Treatment and Pharmacology
- Hepatitis B Virus Studies
- RNA modifications and cancer
- Estrogen and related hormone effects
- Mitochondrial Function and Pathology
- Receptor Mechanisms and Signaling
- HIV Research and Treatment
- Neonatal Health and Biochemistry
- Synthesis of β-Lactam Compounds
Bristol-Myers Squibb (United States)
2016-2025
Shihezi University
2023-2025
Second Affiliated Hospital of Zhejiang University
2023-2025
Syngene International (India)
2016-2023
Biocon (India)
2013-2023
Bristol-Myers Squibb (India)
2013-2023
Shanghai Jiao Tong University
2014-2023
Nanjing Agricultural University
2023
Xiangya Hospital Central South University
2022-2023
Central South University
2022-2023
In the present study, an open-label, three-treatment, three-period clinical study of rosuvastatin (RSV) and rifampicin (RIF) when administered alone in combination was conducted 12 male healthy subjects to determine if coproporphyrin I (CP-I) III (CP-III) could serve as biomarkers for organic anion transporting polypeptide 1B1 (OATP1B1) 1B3 that belong solute carrier gene subfamily. Genotyping human OATP1B1 performed all confirmed absence OATP1B1*5 OATP1B1*15 mutations. Average plasma...
We investigate the localization of multiple signal sources based on sensors performing time-of-arrival (TOA) measurement in wireless sensor networks. Moving beyond widely studied single source problem, concurrently active substantially complicate problem since anchored nodes are unaware associations between measured signals and nodes. At same time, as total number possible source-measurement grows exponentially with nodes, it is inefficient to attempt conventional single-source algorithm for...
Inhibition of organic anion-transporting polypeptide (OATP)1B function can lead to serious clinical drug-drug interactions, thus a thorough evaluation the potential for this type interaction must be completed during drug development. Therefore, sensitive and specific biomarkers OATP that could used in conjunction with studies are currently demand. In present study, preclinical evaluations were conducted characterize suitability coproporphyrins (CPs) I III as markers hepatic functional...
Poultry lacks carbamoyl phosphate synthetase, which is a key enzyme in the endogenous synthesis of arginine, thus poultry must obtain arginine from their diet. Citrulline ( L -Cit), as precursor produces same biological effects and may even be more effective. In these experiments, we discovered that addition -Cit significantly increased production performance, antioxidant immune properties, modulated intestinal microbiota. The study involved 240 1-day-old male yellow-feathered broilers...
Multiple endogenous compounds have been proposed as candidate biomarkers to monitor organic anion transporting polypeptide (OATP) function in preclinical species or humans. Previously, we demonstrated that coproporphyrins (CPs) I and III are appropriate clinical markers evaluate OATP inhibition recapitulate drug-drug interactions (DDIs). In the present study, investigated bile acids (BAs) dehydroepiandrosterone sulfate (DHEAS), hexadecanedioate (HDA), tetradecanedioate (TDA) plasma probes...
The contribution of organic anion transporter OAT2 (SLC22A7) to the renal tubular secretion creatinine and its exact localization in kidney are reportedly controversial. In present investigation, transport was assessed human embryonic (HEK) cells that stably expressed (OAT2-HEK) isolated proximal tubule (HRPTCs). human, monkey, rat characterized. overexpression significantly enhanced uptake OAT2-HEK cells. Under physiologic conditions (creatinine concentrations 41.2 123.5 <i>µ</i>M), initial...
Organic anion–transporting polypeptides (OATP) 1B1, 1B3, and 2B1 can serve as the loci of drug–drug interactions (DDIs). In present work, cynomolgus monkey was evaluated a potential model for studying OATP-mediated DDIs. Three OATPs (cOATPs), with high degree amino acid sequence identity (91.9, 93.5, 96.6% OATP1B1, 2B1, respectively) to their human counterparts, were cloned, expressed, characterized. The cOATPs stably transfected in embryonic kidney cells functionally similar corresponding...
This study evaluated coproporphyrin I (CPI) as a selective endogenous biomarker of OATP1B-mediated drug-drug interactions (DDIs) relative to clinical probe rosuvastatin using nonlinear mixed-effect modeling. Plasma and urine CPI data in the presence/absence rifampicin were modeled describe synthesis, elimination clearances, obtain vivo OATP Ki. The showed stable interoccasion baseline concentrations low interindividual variability (<25%) subjects with wildtype SLCO1B1. Biliary excretion was...
Understanding transporter‐mediated drug–drug interactions is an integral part of risk assessment in drug development. Recent studies support the use hexadecanedioate ( HDA ), tetradecanedioate TDA coproporphyrin CP )‐I, and ‐ III as clinical biomarkers for evaluating organic anion‐transporting polypeptide OATP )1B1 SLCO 1B1) inhibition. The current study investigated effect 1B1 genotype c.521T>C 1B1‐Val174Ala) on extent interaction between cyclosporin A CsA ) pravastatin, associated...
Glucose transporter 4 (GLUT4) is a principal glucose in response to insulin, and impaired translocation or decreased expression of GLUT4 believed be one the major pathological features type 2 diabetes mellitus (T2DM). Therefore, induction or/and promising strategy for anti-T2DM drug discovery. Here we report that natural product (+)-Rutamarin (Rut) functions as an efficient dual inducer on both insulin-induced expression. Rut-treated 3T3-L1 adipocytes exhibit efficiently enhanced uptake,...
In a recent study, limited to South Asian Indian subjects (<i>n</i> = 12), coproporphyrin (CP) I and CPIII demonstrated properties appropriate for an organic anion-transporting polypeptide (OATP) 1B endogenous probe. The current studies were conducted in healthy volunteers of mixed ethnicities, including black, white, Hispanic subjects, better understand the utility these biomarkers broader populations. After oral administration with 600 mg rifampin, <i>AUC</i><sub>(0–24h)</sub> values 2.8-,...
Plasma pyridoxic acid (PDA) and homovanillic (HVA) were recently identified as novel endogenous biomarkers of organic anion transporter (OAT) 1/3 function in monkeys. Consequently, this clinical study assessed the dynamic changes utility plasma PDA HVA an initial evaluation OAT1/3 inhibition early-phase drug development. The was designed a single-dose randomized, three-phase, crossover study; 14 Indian healthy volunteers received probenecid (PROB) (1000 mg orally) alone, furosemide (FSM) (40...
Perturbation of organic anion transporter (OAT) 1- and OAT3-mediated transport can alter the exposure, efficacy, safety drugs. Although there have been reports endogenous biomarkers for OAT1/3, none these all characteristics required a clinical useful biomarker. Cynomolgus monkeys were treated with intravenous probenecid (PROB) at dose 40 mg/kg in this study. As expected, PROB increased area under plasma concentration-time curve (AUC) coadministered furosemide, known substrate OAT1 OAT3, by...
Antibody-drug conjugates (ADCs) are composed of an antibody linked to cytotoxic anticancer payloads. ADCs recognize tumor-specific cell surface antigens and internalized into lysosomes where proteolytic enzymes release the Efflux transporters on plasma membrane that play a significant role multi-drug resistance in chemotherapy can be lysosomal sequester In present study, ATP binding cassette (ABC) efflux including breast cancer protein (BCRP), P-glycoprotein (P-gp-MDR1), multidrug (MRP) 2,...
Background: Vitamins and carotenoids may be involved in the pathogenesis of non-alcoholic fatty liver disease (NAFLD). Previously related publications mainly focused on vitamin D E, studies other vitamins NAFLD are scarce. Methods: This study aimed to explore clinical relevance A, B (vitamin B1, B2, niacin, B6, folate, B12, choline), C (α-carotene, β-carotene, β-cryptoxanthin, lycopene, lutein + zeaxanthin) with steatosis fibrosis 2017-2018 NHANES (N = 4,352). Liver were detected by...