Category: Myeloma

dCBP-1 is a Selective PROTAC Degrader of p300/CBP

The paralogous chromatin regulators CREB-binding protein (CBP) and p300 are factors critical for establishing and activating enhancer-mediated transcription. The CREB-binding protein (CBP) and p300 are important factors for activating enhancer-mediated transcription. These proteins consist of at least 10 distinct functional domains. Most of them interact with over 400 other proteins,...

BMS-P5 is an Orally Active PAD4 Inhibitor

Multiple myeloma (MM), a kind of plasma cell malignancy, grows preferentially in the bone marrow (BM). Neutrophils serve as the first line of defense against a wide range of pathogens, by utilizing two major mechanisms: phagocytosis and degranulation. Recently, the formation of NETs represents another host defense mechanism of...

SC99 is an Orally Active and Selective STAT3 Inhibitor

STAT3 is a member of the STAT protein family. STAT3 mediates the expression of a variety of genes in response to cell stimulation. So it plays a key role in many cell processes, such as cell growth and apoptosis. Specifically, the oncogenic STAT3 signaling pathway is becoming a promising...

OTS514 is a Highly Potent TOPK Inhibitor with Anti-Myeloma Activity

Multiple myeloma represents a heterogeneous disease with various oncogenic mutations, chromosomal translocations, and copy number variations. The mitotic kinase T-LAK cell‐originated protein kinase/PDZ‐binding kinase ( TOPK/PBK) associates with the proliferation of tumor cells, maintenance of cancer stem cells, and poor patient prognosis in many cancers. In addition, TOPK plays...

LBW242 is a Potent and Orally Active Proapoptotic IAP Inhibitor

Acute myelogenous leukemia (AML) is a hematologic malignancy. The characteristics include a block in cellular differentiation and aberrant growth of myeloid precursor cells. Approximately 30% of AML patients and a portion of acute lymphoblastic leukemia (ALL) patients express a mutated form of the class III receptor tyrosine kinase, FLT3....

E64FC26 is a pan-Inhibitor of the Protein Disulfide Isomerase (PDI) Family

Multiple myeloma (MM) is an incurable hematological malignancy. MM results in the accumulation of clonal plasma cells within the bone marrow. The natural biology of the plasma cell makes MM uniquely sensitive to disruptions in protein homeostasis. Subsequently, it proposes targeting protein folding as a strategy for the treatment...

AZD4547 is a Potent FGFR Family Inhibitor

Fibroblast growth factors (FGF) and their receptors play important roles in multiple biologic processes, such as tissue repair, hematopoiesis, angiogenesis, and embryonic development. The FGFR family mainly comprises 4 main members (FGFR1–4). FGFRs and FGFRs FGF ligand binding can result in FGFR dimerization. In addition, receptor autophosphorylation and activation...