Category: Multiple Myeloma

Urabrelimab (SRF231) is a Fully Human Anti-CD47 Monoclonal Antibody

CD47 (Cluster of Differentiation 47) is a transmembrane protein, belonging to the immunoglobulin superfamily. It can interact with signal-regulatory protein alpha (SIRPα) which is an inhibitory transmembrane receptor present on myeloid cells. The interaction leads to different cell-to-cell responses, such as phagocytosis inhibition, cell-cell fusion stimulation, and T-cell activation....

Nanrilkefusp alfa is a Selective and Potent Agonist Fusion Protein of IL-15.

IL-15 is a cytokine involved in the regulation of the innate immune system. It stimulates the proliferation and activation of natural killer (NK) cells and memory CD8+ T cells. And also it promotes the secretion of a variety of cytokines. Moreover, IL-15 enhances the antibody-dependent cytotoxicity (ADCC) of antibodies. Specifically,...

MS159 is a First-In-class NSD2 PROTAC degrader for Multiple Myeloma Research

Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule, including two active domains, and a linker. Importantly, it can remove specific unwanted proteins. PROTAC is a technology based on the ligand binding of TAP and then the degradation of TAP. PROTAC provides an alternative approach to those so-called non-druggable...

Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor

HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because acetylation and de-acetylation can regulate DNA expression. Acetylation is controlled by two antagonistic enzyme families:...

Oprozomib (PR-047) is an Orally Active Peptide Epoxyketone Proteasome Inhibitor

Proteasome inhibition has been validated as a modality in the research of multiple myeloma and Non-Hodgkin’s lymphoma. The proteasome is a multicatalytic protease complex that is responsible for the ubiquitin-dependent turnover of cellular proteins. Proteasome substrates include misfolded or misassembled proteins as well as short-lived components of signaling cascades...

Iberdomide (CC-220) is an Orally Active Cereblon (CRBN) E3 Ligase Modulator (CELMoD)

Cereblon (CRBN) is a key protein in autosomal recessive nonsyndromic mental retardation. Specifically, it plays an intermediary role in helping immunomodulatory drugs play their immunomodulatory and tumor-killing roles. Besides, CRBN is highly conserved from plants to mammals, and mRNA expression in humans, rats, and mice is common. CRBN interacts...

M3258 is an Orally Active and Highly Selective LMP7 (β5i) Inhibitor

The ubiquitin-proteasome system (UPS) plays an essential role in maintaining cellular homeostasis by degrading ubiquitinated proteins. The immunoproteasome and constitutive proteasome are multisubunit cylindrical complexes each containing three proteolytic subunits; large multifunctional peptidase 2 (LMP2/β1i/PSMB9), MECL-1 (LMP10/β2i/PSMB10), and LMP7 (β5i/PSMB8) in the immunoproteasome, replaced, respectively, by β1 (β1c/PSMB6), β2...