Galith Karoutchi

TL;DR: The pharmacologic evidence showed that AZD9496 is an oral, nonsteroidal, selective estrogen receptor antagonist and downregulator in ER(+ breast cells that could provide meaningful benefit to ER(+) breast cancer patients.

TL;DR: The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described.

TL;DR: A series of potentCathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.

TL;DR: A piperazine series of cyclin-dependent kinase (CDK) inhibitors have been identified that exhibit excellent physiochemical properties and a novel binding mode, whereby a bridging interaction via a water molecule with Asp 86 of CDK2, leads to selectivity for the CDK family of enzymes over other kinases.

TL;DR: A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors.