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 …

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, …

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 …

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-…

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 …

[PDF][PDF] Microcephaly proteins Wdr62 and Aspm define a mother centriole complex regulating centriole biogenesis, apical complex, and cell fate

…, N Krogan, JW Harper, JF Reiter, WY Timothy… - Neuron, 2016 - cell.com
Mutations in several genes encoding centrosomal proteins dramatically decrease the size
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 …

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 …

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 …

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 …