This section contains case studies, industry highlights, minireviews, and other articles for drug discovery professionals. Check out the resources page for posters, educational content, lists of drug approvals, and more.
The Genentech PI3Kα isoform-selective kinase inhibitor and mutant PI3Kα degrader inavolisib selectively depletes the oncogenic mutant p110α catalytic subunit of…
molecule
1 year ago ●
2 mins read
The Revolution Medicines KRASG12C inhibitor, RM-018, “glues” KRASG12C to the highly abundant chaperone protein, cyclophilin A, in a tri-complex (KRAS-…
molecule
1 year ago ●
2 mins read
The Lilly glucagon-like peptide-1 receptor (GLP-1R) agonist (LSN3318839) is a positive allosteric modulator intended to treat type 2 diabetes. This…
molecule
1 year ago ●
1 min read
The ARIAD/Takeda EGFR exon 20 insertion mutant (EGFRex20ins) inhibitor TAK-788 is a Breakthrough Therapy for patients with advanced non-small cell lung cancer (NSCLC) whose…
molecule
1 year ago ●
1 min read
MRTX1133 was nominated as December 2021’s cover molecule by reviewers Joachim Rudolph and Julien Lefranc. MRTX1133 is a non-covalent inhibitor…
molecule
1 year ago ●
2 mins read
MK-0616 is a macrocyclic PCSK9 inhibitor with demonstrated once-daily PCSK9-lowering and LDL-cholesterol-lowering activities in a human clinical trial (<300 mg…
molecule
1 year ago ●
2 mins read
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