What is CSF 1R inhibitor?

An orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF-1R; CSF1R), with potential antineoplastic activity. CSF1R inhibitor BLZ945 selectively binds to CSF1R expressed on tumor-associated macrophages (TAMs), blocks the activity of CSF1R, and inhibits CSF1R-mediated signal transduction pathways.

What does macrophage colony stimulating factor do?

Macrophage-colony stimulating factor (CSF-1) signaling through its receptor (CSF-1R) promotes the differentiation of myeloid progenitors into heterogeneous populations of monocytes, macrophages, dendritic cells, and bone-resorbing osteoclasts.

What cells make csf1?

Colony-Stimulating Factor 1 CSF-1, also known as monocyte–macrophage–CSF or macrophage-CSF (M-CSF), is a hematopoietic growth factor that supports the survival and differentiation of monocytic cells. It is produced by a wide variety of cells, including monocytes, smooth muscle cells, endothelial cells, and fibroblasts.

Where is CSF1R expressed?

macrophages
The major site of CSF1R expression is in macrophages. In hematopoiesis, CSF1R is upregulated during monocytic differentiation, but is downregulated during granulopoiesis. CSF1R is expressed predominantly in committed macrophage precursors (CFU-Ms), monocytes, and tissue macrophages.

How does a colony stimulating factors work?

Colony-stimulating factors (CSFs) are secreted glycoproteins that bind to receptor proteins on the surfaces of hematopoietic stem cells, thereby activating intracellular signaling pathways that can cause the cells to proliferate and differentiate into a specific kind of blood cell, usually white blood cells.

Do all macrophages express CSF1R?

Lung macrophage populations are primarily controlled by CSF2 (also known as GM-CSF, encoded by Csf2), rather than CSF129, but lung macrophages do express Csf1r and bind CSF111.

What are interleukins and colony stimulating factors?

Colony-stimulating factors (CSFs) are a diverse group of glycoproteins that induce differentiation of white blood cells in bone marrow. The CSF family includes: Multiple-colony-stimulating factor, or interleukin 3 (IL-3) Granulocyte-macrophage–colony-stimulating factor (GM-CSF)

What is meant by colony-stimulating factor?

Listen to pronunciation. (KAH-luh-nee-STIM-yoo-LAY-ting FAK-ter) A substance that stimulates the production of blood cells. Colony-stimulating factors include granulocyte colony-stimulating factor (G-CSF), granulocyte-macrophage colony-stimulating factor (GM-CSF), and promegapoietin.

How does macrophage colony stimulating factor ( CSF ) 1R work?

Macrophage-colony stimulating factor (CSF-1) signaling through its receptor (CSF-1R) promotes the differentiation of myeloid progenitors into heterogeneous populations of monocytes, macrophages, dendritic cells, and bone-resorbing osteoclasts.

Are there any drugs that target the colony stimulating factor 1 receptor?

Another CSF1R inhibitor that targets/depletes TAMs is Cabiralizumab (cabira; FPA-008) which is a monoclonal antibody and is in early clinical trials for metastatic pancreatic cancer. Colony stimulating factor 1 receptor has been shown to interact with: Suppressor of cytokine signaling 1, This receptor is also linked with the cells of MPS.

How does colony stimulating factor 1 affect microglia?

The increased receptor expression causes microglia to become more active. Both CSF1R, and its ligand colony stimulating factor 1 play an important role in the development of the mammary gland and may be involved in the process of mammary gland carcinogenesis.

What kind of receptor is CSF1R in mouse?

View/Edit Mouse. Colony stimulating factor 1 receptor (CSF1R), also known as macrophage colony-stimulating factor receptor (M-CSFR), and CD115 (Cluster of Differentiation 115), is a cell-surface protein encoded, in humans, by the CSF1R gene (known also as c-FMS).