Structure–Affinity and Structure–Kinetic Relationship Studies of Benzodiazepine Derivatives for the Development of Efficacious Vasopressin V2 Receptor Antagonists

Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease

(2022) Xudong Cao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Long Residence Time at the Vasopressin V2 Receptor Translates into Superior Inhibitory Effects in Ex Vivo and In Vivo Models of Autosomal Dominant Polycystic Kidney Disease

(2022) Haoran Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of mPGES ‐2 ameliorates NASH by activating NR1D1 via heme

(2022) Dandan Zhong et al.   HEPATOLOGY

PF ‐06409577 inhibits renal cyst progression by concurrently inhibiting the mTOR pathway and CFTR channel activity

(2022) Limin Su et al.   FEBS Open Bio

Revisit ligand-receptor interaction at the human vasopressin V2 receptor: A kinetic perspective

(2020) Chunji Liu et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A tolvaptan skeptic repents

(2020) Brad H. Rovin   KIDNEY INTERNATIONAL

Autosomal dominant polycystic kidney disease: Disrupted pathways and potential therapeutic interventions

(2019) Talieh Malekshahabi et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Autosomal dominant polycystic kidney disease

(2019) Emilie Cornec-Le Gall et al.   LANCET

Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes

(2019) Yi Yun et al.   BIOCHEMICAL PHARMACOLOGY

Quercetin inhibits renal cyst growth in vitro and via parenteral injection in a polycystic kidney disease mouse model

(2018) Yangyang Zhu et al.   Food & Function

OUP accepted manuscript

(2018)   NEPHROLOGY DIALYSIS TRANSPLANTATION

The Role of Binding Kinetics in GPCR Drug Discovery

(2015) David Swinney et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Translating slow-binding inhibition kinetics into cellular and in vivo effects

(2015) Grant K Walkup et al.   Nature Chemical Biology

The drug–target residence time model: a 10-year retrospective

(2015) Robert A. Copeland   NATURE REVIEWS DRUG DISCOVERY

Inhibition of Human Hepatic Bile Acid Transporters by Tolvaptan and Metabolites: Contributing Factors to Drug-Induced Liver Injury?

(2015) Jason R. Slizgi et al.   TOXICOLOGICAL SCIENCES

Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action

(2010) Georges Vauquelin et al.   BRITISH JOURNAL OF PHARMACOLOGY

Drug–target residence time: critical information for lead optimization

(2010) Hao Lu et al.   CURRENT OPINION IN CHEMICAL BIOLOGY