R&D Programs

Oncology

Inhibitors of BCL2 proteins (ref ID: ASNX-BCL)

The ability of cells to evade apoptosis or programmed cell death is a hallmark of cancer. Many cancer cells overexpress multiple anti-apoptotic proteins which are closely associated  with the onset of disease, the maintenance of the disease state, and chemo-resistance.

The role of the BCL-2 family of anti-apoptotic proteins as high-priority targets in oncology is well established. Preclinical and clinical data strongly support the value of BCL-2 family subtype-selective inhibitors as well as inhibitors with efficacy against various combinations of subtypes in the treatment of solid and hematologic tumors.

ASINEX has developed a unique and exceptionally efficient Compound-to-Target™ platform and via this platform ASINEX has identified several compounds that inhibit the activity of anti-apoptotic BCL-2 family proteins: Bcl-2, Mcl-1 and Bcl-xL. The optimization of primary hits has led to the development of several lead series demonstrating significant on-target potency and selectivity supported by efficacy in cellular models.

The program is avalable for partnering or research collaboration. For more information, please contact us

CDK9 Small Molecule Inhibitors (ref ID: ASNX-CDK)

Cyclin-dependent kinases (CDKs) are members of a subfamily of serine/threonine kinases which are responsible for cell cycle regulation and transcription. CDKs are universally deregulated in various types of cancer, viral infections, neurodegenerative diseases, ischemia and some proliferative disorders.

Several small-molecule multi-CDK inhibitors have been discovered and these inhibitors show promising activity in anticancer and antiviral models. However, the discovery of inhibitors that are selective to a particular isoform of the CDK family remains a significant challenge.

Utilizing our Compound-to-Target™ platform ASINEX has identified a series of small molecule CDK-9 selective inhibitors demonstrating low nM binding affinity to CDK9/cyclin T and high selectivity over other kinases and other CDK isoforms. Our compounds exert high cytotoxic activity in AML, colon, breast and ovarian cancer cell lines (EC50 < 100 nM) but not in normal epithelial or fibroblast cells. Optimization of ADME/PK profiles has led to the identification of highly potent and orally available lead compounds that exhibit promising efficacy in LLC and melanoma models.

The program is avalable for partnering or research collaboration. For more information, please contact us

Inhibitors of Wnt/β-catenin pathway (ref ID: ASNX-WNT)

The Wnt/β-catenin signaling pathway plays a critical role in a broad range of biological systems including stem cell biology, developmental biology, and adult organ systems. Deregulation of the functional components of the pathway has been implicated in a wide spectrum of diseases including cancer, neurological, skin, and cardiovascular disorders.

Several components of the Wnt/β-catenin signaling pathway represent valuable targets for drug discovery efforts.

Utilizing our Compound-to-Target™ platform ASINEX has identified a series of small molecule Wnt-pathway regulators that act through the inhibition of transcription of β-catenin-dependent oncogenes.

The program is avalable for partnering or research collaboration. For more information, please contact us

Infectious diseases

Novel antibacterial agents

Antimicrobial resistance represents a major threat to public health worldwide. To address this challenge Asinex has applied its Compound-to-Target™ platform to discover novel antibacterial agents. This effort has resulted in the identification of small molecule and macrocyclic compounds that can effectively kill several hostile pathogens including Mycobacterium tuberculosis and Staphylococcus aureus. The Compound-to-Target™ platform has also allowed us to identify new compounds that synergize with existing antimicrobials.

The program is avalable for partnering or research collaboration. For more information, please contact us