Here comes a new post in our series inspired by Drug Hunter’s “Molecules of the Month”!
Below are two molecules that were recently highlighted by Drug Hunter!
1. GLPG 2534 is a potent and selective inhibitor of interleukin-1 receptor-associated kinase (IRAK4), which is a part of the TLR signaling pathway. The IRAK4 integrates downstream signals of receptors playing a role in innate and adaptive immune responses. The modulators of immune responses display great therapeutic potential in treating immune-mediated inflammatory diseases (IMIDs). Various tests showed the activity of GLPG 2534 in models of inflammatory skin diseases (ISD). Also, substantial inhibition of TLR and IL-1 responses in primary keratinocytes, granulocytes, and T cells was observed in vitro. Skin inflammation of psoriasis and atopic dermatitis (AD) in mouse models was evidently damped down with the inhibition of IRAK4. Thus, the use of GLPG 2534 as an IRAK4 inhibitor is a promising trend in ISD treatment.
You can find the analogs to this molecule here!
2. Pociredir (FTX-6058) is an oral and potent inhibitor of polycomb repressive complex 2 (PRC2). It binds to the embryonic ectoderm development (EED) protein which is a part of this complex. EED inhibiting leads to the downregulation of main fetal globin repressors in a potent way that causes an increase in fetal hemoglobin (HbF) protein expression in cell and rodent models. FTX-6058 was developed as a promising drug candidate for treating various hemoglobinopathies, including sickle cell disease (SCD) and β-thalassemia. It was in Phase 2 clinical trial in people with SCD and granted FDA Fast Track designation and Orphan Drug designation, but now the investigations are on hold.
You can find the analogs to this molecule here!
Use chem-space.com/search to find off-the-shelf and Make-on-Demand molecules of your interest!