Ganetespib (STA-9090) is a HSP90 Inhibitor
Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...
Ruxolitinib (INCB018424) is an Orally Active JAK1 and JAK2 Inhibitor
The myeloproliferative neoplasms (MPNs) are a group of related clonal diseases probably arising from hematopoietic progenitor or stem cells. Patients with MPNs have an increased risk of thrombotic and bleeding complications and disease progression to acute myeloid leukemia. JAK2 is a member of the JAK family of cytoplasmic tyrosine...
MRTX9768 is an Orally Active PRMT5 Inhibitor
PRMT5 is the main type II enzyme. It catalyzes symmetric dimethylarginine of histone proteins to induce gene silencing by generating repressive histone marks. PRMT5 can also methylate nonhistone proteins such as the transcription factors p53 and p65. Modifications of these proteins by PRMT5 have relations with diverse cellular processes....
UK122 is a Selective Urokinase-Type Plasminogen Activator (uPA) Inhibitor
Urokinase, also known as urokinase-type plasminogen activator (uPA), is a serine protease found in humans and other animals. Specifically, UPA is relevant to tissue remodeling and cell migration. The active form of uPA binds to its high-affinity receptor on the cell surface, and specific inhibitors can regulate its enzyme...
DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP
Proteolysis targeting chimera (PROTAC) is a bifunctional small molecule. Interestingly, dual PROPACs are dual-targeted degradation molecules that combine the concepts of PROTAC and dual-targeting. Dual PROPACs degrade two completely different pathway targets while simultaneously taking advantage of both PROTAC and dual-target drugs. Thus, dual PROPACs not only achieve the...
Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor
PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...
Sitravatinib (MGCD516) is an Orally Bioavailable RTK Inhibitor with PD-1 Blockade Activity
Sarcomas are rare but highly aggressive mesenchymal tumors. Mutation and overexpression of many receptor tyrosine kinases (RTKs) including c-Met, PDGFR, c-Kit and IGF1-R drive defective signaling pathways in sarcomas. Sitravatinib is a small molecule inhibitor targeting multiple receptor tyrosine kinases involved in driving sarcoma cell growth. Moreover, Sitravatinib significantly...