Xiaorong Liang
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View article: Discovery of GuaB inhibitors with efficacy against <i>Acinetobacter baumannii</i> infection
Discovery of GuaB inhibitors with efficacy against <i>Acinetobacter baumannii</i> infection Open
Guanine nucleotides are required for growth and viability of cells due to their structural role in DNA and RNA, and their regulatory roles in translation, signal transduction, and cell division. The natural antibiotic mycophenolic acid (MP…
View article: Meeting Report on the 3rd Chinese American Society for Mass Spectrometry Conference—Advancing Biological and Pharmaceutical Mass Spectrometry
Meeting Report on the 3rd Chinese American Society for Mass Spectrometry Conference—Advancing Biological and Pharmaceutical Mass Spectrometry Open
Following the highly successful Chinese American Society for Mass Spectrometry (CASMS) conferences in the previous 2 years, the 3rd CASMS Conference was held virtually on August 28–31, 2023, using the Gather.Town platform to bring together…
View article: Meeting Report on the 2nd Chinese American Society for Mass Spectrometry Conference: Advancing Biological and Pharmaceutical Mass Spectrometry
Meeting Report on the 2nd Chinese American Society for Mass Spectrometry Conference: Advancing Biological and Pharmaceutical Mass Spectrometry Open
View article: Supplementary Figure 1 from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Supplementary Figure 1 from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
PDF file 122K, A) Chemical structure of GNE-617, B) cellular NAD and ATP levels in H522 cells after exposure to 4nM GNE-617, C) correlation of NAPRT1 mRNA and protein (n=32, spearman r= 0.88, p,0.0001)
View article: Supplementary Figure 1 from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Supplementary Figure 1 from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
PDF file 122K, A) Chemical structure of GNE-617, B) cellular NAD and ATP levels in H522 cells after exposure to 4nM GNE-617, C) correlation of NAPRT1 mRNA and protein (n=32, spearman r= 0.88, p,0.0001)
View article: Data from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Data from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
Purpose: We sought to identify predictive biomarkers for a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor.Experimental Design: We use a NAMPT inhibitor, GNE-617, to evaluate nicotinic acid rescue status in a p…
View article: Supplementary Methods and Tables from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Supplementary Methods and Tables from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
PDF file 141K, Supplementary methods for NAD quantification and the QMSP assay. Table S1 GNE-617 IC50 and mRNA Levels of NAMPT and NAPRT1, Table S2 Cell Lines Not Rescued with 10uM NA, Table S3 Cell Lines with Low NAPRT1 Expression
View article: Supplementary Methods and Tables from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Supplementary Methods and Tables from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
PDF file 141K, Supplementary methods for NAD quantification and the QMSP assay. Table S1 GNE-617 IC50 and mRNA Levels of NAMPT and NAPRT1, Table S2 Cell Lines Not Rescued with 10uM NA, Table S3 Cell Lines with Low NAPRT1 Expression
View article: Data from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors
Data from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors Open
Purpose: We sought to identify predictive biomarkers for a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor.Experimental Design: We use a NAMPT inhibitor, GNE-617, to evaluate nicotinic acid rescue status in a p…
View article: Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947
Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947 Open
View article: An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma
An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma Open
View article: Changes in Organic Anion Transporting Polypeptide Uptake in HEK293 Overexpressing Cells in the Presence and Absence of Human Plasma
Changes in Organic Anion Transporting Polypeptide Uptake in HEK293 Overexpressing Cells in the Presence and Absence of Human Plasma Open
View article: An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma
An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma Open
View article: Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor
Investigation of the absolute bioavailability and human mass balance of navoximod, a novel IDO1 inhibitor Open
Aims Navoximod (GDC‐0919, NLG‐919) is a small molecule inhibitor of indoleamine‐2,3‐dioxygenase 1 (IDO1), developed to treat the acquired immune tolerance associated with cancer. The primary objectives of this study were to assess navoximo…
View article: Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study
Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study Open
Background: Mass balance studies conducted using radiolabeled material (14C or 3H) definitively characterize the Absorption, Metabolism, and Excretion (AME) of a drug. A critical aspect of these studies is that the radiotracer maintains it…
View article: Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors
Phase Ia study of the indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor navoximod (GDC-0919) in patients with recurrent advanced solid tumors Open
ClinicalTrials.gov identifier: NCT02048709 .
View article: Correction to: Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency
Correction to: Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency Open
View article: A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors Open
The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region an…
View article: GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Open
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderate…
View article: Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency
Strategies of Drug Transporter Quantitation by LC-MS: Importance of Peptide Selection and Digestion Efficiency Open
View article: Rosuvastatin Pharmacokinetics in Asian and White Subjects Wild Type for Both OATP1B1 and BCRP Under Control and Inhibited Conditions
Rosuvastatin Pharmacokinetics in Asian and White Subjects Wild Type for Both OATP1B1 and BCRP Under Control and Inhibited Conditions Open
View article: Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats
Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats Open
Improved small molecule bioanalytical sensitivity and concomitant decreased sample volume requirements provide an opportunity to reconsider how toxicokinetic (TK) data are collected in rat toxicity studies. Often, satellite groups of rats …
View article: Metabolic Response to NAD Depletion across Cell Lines Is Highly Variable
Metabolic Response to NAD Depletion across Cell Lines Is Highly Variable Open
Nicotinamide adenine dinucleotide (NAD) is a cofactor involved in a wide range of cellular metabolic processes and is a key metabolite required for tumor growth. NAMPT, nicotinamide phosphoribosyltransferase, which converts nicotinamide (N…