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Small Molecule Antagonists Of The Pro-Survival Protein Mcl-1


Technology Benefits

Direct inhibition of the MCL-1 proteinSmall molecule inhibitor


Technology Application

Therapeutic approach to activate the apoptosis pathway, potentially leading to cancer cell deathPotentially used as a combination therapy, or as a monotherapy


Detailed Technology Description

UCLA Researchers in the Department Chemistry & Biochemistry have developed novel small molecules that bind MCL-1, which in turn promotes the activation of the apoptosis pathway, resulting in cancer cell death.


Application No.

2017066747


Others

State Of Development

Successful demonstration in vitro binding of recombinant protein


Background

Multiple cancer types, including chronic lymphocytic leukemia (CML) have been shown to overexpress signaling proteins involved the inhibition of apoptosis, including BCL-2 and MCL-1.This feature makes these proteins ideal targets for cancer therapeutics.Currently, there is one small molecule that has been FDA approved that targets this signaling pathway, binding to BCL-2.However, 60% of patients each year are resistant to this treatment, highlighting the necessity of targeting other proteins within this pathway, such as MCL-1.


Related Materials

Bracken, JD, Carlson, AD, Frederich, JH, Nguyen, M, Shore, GC, Harran, PG. “Tailored fragments of roseophilin selectively anatagonize Mcl-1 in vitro”. Tetrahedron Letters 2015 Jun 3; 56(23): 3612-3616.


Tech ID/UC Case

27303/2014-387-0


Related Cases

2014-387-0


Country/Region

USA

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