Search Results - "Fan, Peter"
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Characterization of Differential Tissue Abundance of Major Non-CYP Enzymes in Human
Published in Molecular pharmaceutics (02-11-2020)“…The availability of assays that predict the contribution of cytochrome P450 (CYP) metabolism allows for the design of new chemical entities (NCEs) with minimal…”
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Investigation of Drug Delivery in Rats via Subcutaneous Injection: Case Study of Pharmacokinetic Modeling of Suspension Formulations
Published in Journal of pharmaceutical sciences (01-01-2019)“…With the rising cost of drug research, "do more with less" has become a new emphasis in the pharmaceutical industry. Consequently, the early analysis of…”
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Regional proteomic quantification of clinically relevant non-cytochrome P450 enzymes along the human small intestine
Published in Drug metabolism and disposition (01-07-2020)“…Current challenges in accurately predicting intestinal metabolism arise from the complex nature of the intestine, leading to limited applicability of available…”
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Comparison of Tissue Abundance of Non-Cytochrome P450 Drug-Metabolizing Enzymes by Quantitative Proteomics between Humans and Laboratory Animal Species
Published in Drug metabolism and disposition (01-03-2022)“…The use of animal pharmacokinetic models as surrogates for humans relies on the assumption that the drug disposition mechanisms are similar between preclinical…”
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Going Beyond Common Drug Metabolizing Enzymes: Case Studies of Biotransformation Involving Aldehyde Oxidase, γ-Glutamyl Transpeptidase, Cathepsin B, Flavin-Containing Monooxygenase, and ADP-Ribosyltransferase
Published in Drug metabolism and disposition (01-08-2016)“…The significant roles that cytochrome P450 (P450) and UDP-glucuronosyl transferase (UGT) enzymes play in drug discovery cannot be ignored, and these enzyme…”
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Carboxylesterase catalyzed 18O-labeling of carboxylic acid and its potential application in LC-MS/MS based quantification of drug metabolites
Published in Drug metabolism and pharmacokinetics (01-10-2019)“…LC-MS quantification of drug metabolites is sometimes impeded by the availability of internal standards that often requires customized synthesis and/or…”
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Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design
Published in Bioorganic & medicinal chemistry letters (01-06-2023)“…[Display omitted] Inhibition of NF-κB inducing kinase (NIK) has been pursued as a promising therapeutic target for autoimmune disorders due to its highly…”
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Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors
Published in Journal of medicinal chemistry (25-06-2015)“…The p21-activated kinases (PAKs) play important roles in cytoskeletal organization, cellular morphogenesis, and survival and have generated significant…”
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Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology
Published in ACS medicinal chemistry letters (09-09-2021)“…Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for the treatment of a number of indications ranging from pulmonary and…”
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10
Insights from the reanalysis of high-throughput chemical genomics data for Escherichia coli K-12
Published in G3 : genes - genomes - genetics (01-01-2021)“…Despite the demonstrated success of genome-wide genetic screens and chemical genomics studies at predicting functions for genes of unknown function or…”
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Ileocolonic-Targeted JAK Inhibitor: A Safer and More Effective Treatment for Inflammatory Bowel Disease
Published in Pharmaceutics (01-11-2022)“…Janus kinase (JAK) inhibitors, such as tofacitinib (Xeljanz) and filgotinib (Jyseleca), have been approved for treatment of ulcerative colitis with several…”
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Characterization of Raloxifene Glucuronidation in Vitro: Contribution of Intestinal Metabolism to Presystemic Clearance
Published in Drug metabolism and disposition (01-06-2002)“…Raloxifene, a selective estrogen receptor modulator used for the treatment of osteoporosis, undergoes extensive conjugation to the 6-β- and…”
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Introduction and expression of PIK3CA E545K in a papillary thyroid cancer BRAF V600E cell line leads to a dedifferentiated aggressive phenotype
Published in Journal of otolaryngology-head and neck surgery (01-02-2022)“…Anaplastic thyroid cancer (ATC) is a rare, aggressive form of undifferentiated thyroid cancer, which exhibits rapid progression and is almost universally…”
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A10 - Characterization of differential tissue abundance of major non-cyp enzymes in human
Published in Drug metabolism and pharmacokinetics (2020)Get full text
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15
NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus
Published in Nature communications (12-01-2018)“…NF-κB-inducing kinase (NIK) mediates non-canonical NF-κB signaling downstream of multiple TNF family members, including BAFF, TWEAK, CD40, and OX40, which are…”
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Comparative Immunogenicity of the 2014-2015 Northern Hemisphere Trivalent IIV and LAIV against Influenza A Viruses in Children
Published in Vaccines (Basel) (12-08-2019)“…Both inactivated influenza vaccines (IIV) and live-attenuated influenza vaccines (LAIV) have been recommended for administration to children. Children are a…”
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Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat
Published in Drug metabolism letters (01-06-2016)“…Significant under-prediction of in vivo clearance in rat was observed for a potent p21-activated kinase (PAK1) inhibitor, GNE1. Rate-determining (rapid uptake)…”
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Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP
Published in Bioorganic & medicinal chemistry letters (01-07-2014)“…Based on their structural similarity to previously described compound AMG 009, indole-phenyl acetic acids were proposed to be potent dual inhibitors of…”
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Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System
Published in ACS medicinal chemistry letters (13-08-2015)“…Time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes may incur serious undesirable drug–drug interactions and in rare cases drug-induced…”
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Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery
Published in Future medicinal chemistry (01-01-2014)“…The use of liver microsomes and hepatocytes to predict total in vivo clearance is standard practice in the pharmaceutical industry; however, metabolic…”
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