Paper Picks

Our paper pick for April 2024 discusses the reasons and strategies for replacing a carboxylic acid with a bioisostere. Of particular interest is the use of structural biology to identify neutral bioisosteres that rely on less commonly explored cation π-interactions.

Our highlighted paper for March 2024 looks at how chemists investigated and overcame anticoagulation mediated toxicity caused by an aldehyde oxidase metabolite.

Our choice for February comprises two papers looking at the impact of metabolism-mediated loss of radiolabel in human mass balance studies.

Our first paper pick for 2024 describes the discovery of IRAK4 inhibitors which benefited from inclusion of 2 hydroxyl groups at different positions in the structures.

Discover the recommendations made by the IQ Consortium Metabolite Bioanalysis Working Group around best practice in metabolite bioanalysis during drug development.

Find out why more focus should be placed on major metabolites of locally acting drugs such as the unusual gut metabolites of izencitinib.

Concerned about missing or unexplained metabolites? Checkout our paper pick for October 2023 for helpful case studies and advice.

Unusual biotransformation reactions uncovered at Genentech are featured in our paper pick for September 2023.

Our paper pick for August 23 describes an unexpected, slow-forming, and long half-life major metabolite of iclepertin

Our paper pick for July 2023 is an interesting and rare example of a discrete diglucuronide of GDC-0810 formed by glucuronidation on two different functional groups to a major circulating metabolite in humans.

Some super interesting biotransformations of navoximod were published by Shuai Wang and colleagues at Genentech in our paper pick for April 23

Who knew that this active hydroxylated metabolite discovered during clinical trials would help unearth some previously unknown structure-activity relationships?