Overview of Critical Parameters for the Design and Execution of a High-Throughput Screen for Allosteric Ligands [0.03%]
高通量别构配体筛选的设计及实施要点综述
Andrew Alt
Andrew Alt
Allosteric ligands modulate the activity of receptor targets by binding to sites that are distinct from the orthosteric (native agonist) binding site. Allosteric modulators have potential therapeutic advantages over orthosteric agonists and...
Kathleen M Knights,David M Stresser,John O Miners et al.
Kathleen M Knights et al.
Knowledge of the metabolic stability of newly discovered drug candidates eliminated by metabolism is essential for predicting the pharmacokinetic (PK) parameters that underpin dosing and dosage frequency. Further, characterization of the en...
Michael S Saporito,Eva Zuvich,Amy DiCamillo
Michael S Saporito
Detailed in this unit is a mouse model of overactive bladder and urinary incontinence based on diuretic stress-induced urination. The procedure involves the use of a unique, highly sensitive, and automated urine capturing method to measure ...
Terry Kenakin
Terry Kenakin
G protein-coupled receptors (GPCRs) are often pleiotropically linked to numerous cellular signaling mechanisms in cells, and it is now known that many agonists differentially activate some signaling pathways at the expense of others. The me...
Bradley J S C Olson
Bradley J S C Olson
Biochemical analysis of proteins relies on accurate quantification of protein concentration. Detailed in this appendix are some commonly used methods for protein analysis, e.g., Lowry, Bradford, bicinchoninic acid (BCA), UV spectroscopic, a...
Genetically Engineered Mouse Models of Pancreatic Cancer: The KPC Model (LSL-Kras(G12D/+) ;LSL-Trp53(R172H/+) ;Pdx-1-Cre), Its Variants, and Their Application in Immuno-oncology Drug Discovery [0.03%]
胰腺癌转基因小鼠模型KPC及其亚型在免疫药物研发中的应用
Jae W Lee,Chad A Komar,Fee Bengsch et al.
Jae W Lee et al.
Pancreatic ductal adenocarcinoma (PDAC) ranks fourth among cancer-related deaths in the United States. For patients with unresectable disease, treatment options are limited and lack curative potential. Preclinical mouse models of PDAC that ...
Katy Phelan,Kristin M May
Katy Phelan
Cultured tissues and cells are used extensively in physiological and pharmacological studies. In vitro cultures provide a means of examining cells and tissues without the complex interactions that would be present if the whole organism were...
Ronald J Tallarida
Ronald J Tallarida
Described in this unit are experimental and computational methods to detect and classify drug interactions. In most cases, this relates to two drugs or compounds with overtly similar effects, e.g., two analgesics or two anti-hypertensives. ...
Djane B Duarte,Michael R Vasko,Jill C Fehrenbacher
Djane B Duarte
The subcutaneous air pouch is an in vivo model that can be used to study the components of acute and chronic inflammation, the resolution of the inflammatory response, the oxidative stress response, and potential therapeutic targets for tre...
Byoungwook Bang,Lenard M Lichtenberger
Byoungwook Bang
Animal models of experimentally induced inflammatory bowel disease (IBD) are useful for understanding more about the mechanistic basis of the disease, identifying new targets for therapeutic intervention, and testing novel therapeutics. Thi...