Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

Akt kinase, a member of AGC kinases, is important in many cellular functions including
proliferation, migration, cell growth and metabolism. There are three known Akt isoforms …

The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …

Tapinarof (GSK2894512) is a naturally derived topical treatment with demonstrated efficacy
for patients with psoriasis and atopic dermatitis, although the biologic target and mechanism …

Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

As part of the global effort toward malaria eradication, phenotypic whole-cell screening
revealed the 2-aminopyridine class of small molecules as a good starting point to develop …

Highlights•Preclinical studies support us of PI3K inhibitors in autoimmunity and
inflammation.•First in class PI3K inhibitor has been approved for treatment of B cell …

The biochemical role of the PI3K/PKB/mTOR signalling pathway in cell-cycle regulation is
now well known. During the onset and development of different forms of cancer it becomes …

Concomitant inhibition of multiple cancer-driving kinases is an established strategy to
improve the durability of clinical responses to targeted therapies. The difficulty of discovering …

Abstract Next-Generation Risk Assessment is defined as an exposure-led, hypothesis-driven
risk assessment approach that integrates new approach methodologies (NAMs) to assure …