Category: Myeloma

PTC-209 is a Specific BMI-1 Inhibitor and Impairs the Tumor Microenvironment

Glioblastoma multiforme (GBM) is the most common and aggressive brain tumor and refractory to existing therapies. BMI-1 is part of the polycomb repressive complex 1 (PRC1). There is a statistically significant correlation between the high frequency of BMI-1-positive tumor cells and poor prognosis of patients according to the data...

Lenalidomide, a Ligand of CRBN, is an Orally Active Immunomodulator

Immunomodulatory imide drugs (IMiDs) are a class of immunomodulatory drugs containing an imide group. The discovery of anti-angiogenic and anti-inflammatory properties promoted the development of Thalidomide analogs. These compounds bind Cereblon (CRBN), the substrate adaptor for the CRBN-CRL4 E3 ubiquitin ligase, and modulate the substrate specificity of the enzyme....

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....