Hot Targets

Antisolvent/cooling and quench crystallization methodologies stand as predominant techniques in the crystallization domain, widely employed for the purification of starting materials, intermediates, and active pharmaceutical ingredients (APIs), as well as for identifying suitable polymorphs for drug products in the pharmaceutical industry. Quench crystallization, compared to antisolvent/cooling crystallization, exhibits the capability to generate crystals in the […]

Extracellular signal-regulated kinase 1/2 (ERK1/2) occupies a pivotal position as the distal effector in the intricate RAS-RAF-MEK-ERK signaling pathway. Remarkably, ERK1/2 exhibits a substantially lower frequency of mutational events in comparison to its upstream counterparts, namely RAS, RAF, and MEK. This inherent genetic stability confers distinct advantages upon ERK1/2 as a therapeutic target. Although ERK1/2

MEK1/2, the third component within the RAS-RAF-MEK-ERK cascade known as the “classical” MAPK oncology pathway, acts as the intermediary in transmitting signals from RAS and RAF to ERK, thereby modulating critical cellular processes such as survival and proliferation. Consequently, MEK1/2 has emerged as a promising target for cancer therapy. Currently, four MEK inhibitors have received

The RAF family kinase plays a crucial role as a pivotal component within the RAS/RAF/MEK/ERK signaling pathway, which is a fundamental cellular pathway involved in various physiological processes. Deregulation in RAF kinases, with a particular emphasis on BRAF, are frequently observed in malignant conditions including melanomas and papillary thyroid cancers. Consequently, the targeted inhibition of

Although the rule of 5 has served as a guiding principle for medicinal discovery scientists over the course of decades, it does not confine their exploration to molecules within the physicochemical property space. Protein degraders known as PROTACs, for instance, often possess properties that deviate from Lipinski’s rule, which characterizes molecules considered suitable for drug

There are 790+ interventional and observational clinical trial records associated with either KRAS itself or the pathway that KRAS  is part of. The interventional studies are designed to evaluate the potential treatments including small vaccines, monoclonal antibodies and  small molecules. More than 22 small molecule inhibitors with varied specificity against distinct KRAS mutants.

Since Novartis published the first SHP2 allosteric inhibitor SHP099 in 2016, the discovery of other SHP2 inhibitors has ignited explosively. By May 2023, more than 14 SHP2 inhibitors are under clinical trials. The disclosed structures of several SHP2 inhibitors, besides Novartis’ clinical candidate TNO155, indicate that they have adopted SHP099 as the lead compound.