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Checkpoint inhibitor therapy is a form of cancer immunotherapy. The therapy targets immune checkpoints , key regulators of the immune system that when stimulated can dampen the immune response to an immunologic stimulus.
This checkpoint is the target of Merck & Co.'s melanoma drug Keytruda, which gained FDA approval in September 2014. The checkpoint is also the target of EMD Serono (Merck KGaA)'s drug Bavencio, which gained FDA approval in 2017. An advantage of targeting PD-1 is that it can restore immune function in the tumor microenvironment.
Positive immunostaining can predict response to the treatment. PD-1 inhibitors and PD-L1 inhibitors are a group of checkpoint inhibitor anticancer drugs that block the activity of PD-1 and PDL1 immune checkpoint proteins present on the surface of cells. Immune checkpoint inhibitors are emerging as a front-line treatment for several types of ...
CHEK2 (Checkpoint kinase 2) is a tumor suppressor gene that encodes the protein CHK2, a serine-threonine kinase. CHK2 is involved in DNA repair , cell cycle arrest or apoptosis in response to DNA damage.
Checkpoint kinase 1, commonly referred to as Chk1, is a serine/threonine-specific protein kinase that, in humans, is encoded by the CHEK1 gene. [ 5 ] [ 6 ] Chk1 coordinates the DNA damage response (DDR) and cell cycle checkpoint response. [ 7 ]
CTLA-4 is a member of the immunoglobulin superfamily that is expressed by activated T cells and transmits an inhibitory signal to T cells.CTLA-4 is homologous to the T-cell co-stimulatory protein, CD28, and both molecules bind to CD80 and CD86, also called B7-1 and B7-2 respectively, on antigen-presenting cells.
Eftilagimod alpha ("efti" in short) is a soluble LAG-3 fusion protein that activates antigen-presenting cells.It is a 160 kDa protein consisting of the four extracellular domains of LAG-3 fused to the Fc region of an IgG1(LAG-3Ig).
Amongst people treated with immune checkpoint inhibitors, those with Faecalibacterium genus and other Bacillota present in the colonic flora have longer progression-free survival and overall survival. In addition, a higher rate of checkpoint inhibitor induced colitis is associated with the presence of Faecalibacterium in the fecal microbiota. [5]