Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites
J Gan, TW Harper, MM Hsueh, Q Qu… - Chemical research in …, 2005 - ACS Publications
A sensitive and quantitative method was developed for the estimation of reactive metabolite
formation in vitro. The method utilizes reduced glutathione (GSH) labeled with a …
formation in vitro. The method utilizes reduced glutathione (GSH) labeled with a …
Shift in pH of biological fluids during storage and processing: effect on bioanalysis
A Fura, TW Harper, H Zhang, L Fung… - Journal of Pharmaceutical …, 2003 - Elsevier
The pH of ex vivo plasma, bile and urine was monitored at different times and temperatures
of storage, and following different sample processing methods such as ultrafiltration, …
of storage, and following different sample processing methods such as ultrafiltration, …
Discovery of a parenteral small molecule coagulation factor XIa inhibitor clinical candidate (BMS-962212)
…, EJ Crain, PC Wong, Z Lou, TW Harper… - Journal of Medicinal …, 2017 - ACS Publications
Factor XIa (FXIa) is a blood coagulation enzyme that is involved in the amplification of
thrombin generation. Mounting evidence suggests that direct inhibition of FXIa can block …
thrombin generation. Mounting evidence suggests that direct inhibition of FXIa can block …
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment
…, S Zhuang, C Chen, CS Madsen, TW Harper… - Bioorganic & medicinal …, 2007 - Elsevier
A series of 2,4,5-tri-substituted imidazoles has proven to be highly potent in inhibiting mammalian
15-lipoxygenase (15-LO) with excellent selectivity over human isozymes 5- and P-12-…
15-lipoxygenase (15-LO) with excellent selectivity over human isozymes 5- and P-12-…
Reaction phenotyping: current industry efforts to identify enzymes responsible for metabolizing drug candidates
TW Harper, PJ Brassil - The AAPS journal, 2008 - Springer
Reaction phenotyping studies to identify specific enzymes involved in the metabolism of drug
candidates are increasingly important in drug discovery efforts. Experimental approaches …
candidates are increasingly important in drug discovery efforts. Experimental approaches …
[PDF][PDF] Microcephaly proteins Wdr62 and Aspm define a mother centriole complex regulating centriole biogenesis, apical complex, and cell fate
Mutations in several genes encoding centrosomal proteins dramatically decrease the size
of the human brain. We show that Aspm (abnormal spindle-like, microcephaly-associated) …
of the human brain. We show that Aspm (abnormal spindle-like, microcephaly-associated) …
Cardioselective anti-ischemic ATP-sensitive potassium channel openers
…, SZ Ahmed, FN Ferrara, TW Harper… - Journal of medicinal …, 1993 - ACS Publications
Diazoxide (4) vasodilation. 1 The original excitement about the discovery of this class of
agents is somewhat dampened as no clear advantages of Katp openers over the existing …
agents is somewhat dampened as no clear advantages of Katp openers over the existing …
Structure-based design of macrocyclic factor XIa inhibitors: Discovery of the macrocyclic amide linker
…, S Sheriff, Z Lou, JJ Zheng, TW Harper… - Journal of Medicinal …, 2017 - ACS Publications
A novel series of macrocyclic FXIa inhibitors was designed based on our lead acyclic phenyl
imidazole chemotype. Our initial macrocycles, which were double-digit nanomolar FXIa …
imidazole chemotype. Our initial macrocycles, which were double-digit nanomolar FXIa …
1-Aminobenzotriazole, a known cytochrome P450 inhibitor, is a substrate and inhibitor of N-acetyltransferase
Q Sun, TW Harper, EA Dierks, L Zhang, S Chang… - Drug metabolism and …, 2011 - ASPET
1-Aminobenzotriazole (ABT) has been used widely as a nonselective in vitro and in vivo
inhibitor of cytochrome P450 enzymes. To date, however, it has not been evaluated as an …
inhibitor of cytochrome P450 enzymes. To date, however, it has not been evaluated as an …
Novel phenylalanine derived diamides as Factor XIa inhibitors
…, PC Wong, R Narayanan, TW Harper… - Bioorganic & Medicinal …, 2016 - Elsevier
The synthesis, structural activity relationships (SAR), and selectivity profile of a potent series
of phenylalanine diamide FXIa inhibitors will be discussed. Exploration of P1 prime and P2 …
of phenylalanine diamide FXIa inhibitors will be discussed. Exploration of P1 prime and P2 …