Drug discovery encompasses processes ranging from target selection and validation to the selection of a development candidate. While comprehensive drug discovery work flows are implemented predominantly in the big pharma domain, early discovery focus in academia serves to identify probe molecules that can serve as tools to study targets or pathways. Despite differences in the ultimate goals of ...

Inosine monophosphate (IMP) dehydrogenase (IMPDH) is a significant enzyme in the purine nucleotide biosynthetic pathway. IMPDH is viewed as an important biological target in the quest for drugs in the antiviral therapeutic area. This review article is focused on the chemistry and biology of IMPDH inhibitors and the use of IMPDH inhibition data as a probe in antiviral drug discovery. Examples of...

Histone acetyltransferases (HATs) are a class of epigenetic enzymes involved in critical cellular processes like nucleosome assembly, DNA damage repair, and transcriptional regulation. HATs are implicated in many human pathologies including cancers. This chapter describes essential experimental considerations for performing high-throughput screening assays, and offers practical strategies for a...

Elevated systemic levels of glucocorticoids are causally related to peripheral insulin resistance. The pharmacological use of synthetic glucocorticoids (corticosteroids) often results in insulin resistance/type II diabetes. Skeletal muscle is responsible for close to 80% of the insulin-induced systemic disposal of glucose and is a major target for glucocorticoid-induced insulin resistance. We u...

Introduction The UV fiber optics system has emerged in dissolution testing of solid dosage forms as a useful alternative to conventional dissolution tests in both research & development and quality control. The system allows continuous in situ analysis of the drug concentration without the need for sample withdrawal and preparation. Therefore, this technique not only facilitates automation, but...

conclusions we can conclude that treatment of af using a right-sided minithoracotomy approach and rf energy in patients undergoing cardiac surgery for various valve diseases is feasible, safe, and reproducible. objectives our aim is to evaluate the feasibility, safety, and immediate plus medium-term results of concomitant af ablation therapy in patients undergoing minimally invasive valve surge...

The potentially pathogenic Non-Tuberculosis Mycobacteria (NTM) are emerging nowadays which result in pulmonary and non-pulmonary infections in human. This group of bacteria consists of at least 200 different species. While the pulmonary disease is the most common form of NTM infections, NTM can cause diffused infections as well as extrapulmonary infections in every organ, such as bone marrow, s...

Kidney is a major target for adverse effects associated with corticosteroids. A microarray dataset was generated to examine changes in gene expression in rat kidney in response to methylprednisolone. Four control and 48 drug-treated animals were killed at 16 times after drug administration. Kidney RNA was used to query 52 individual Affymetrix chips, generating data for 15,967 different probe s...