Cullgen Announces Publication of Small Molecule BRAF Protein Degraders in Journal of Medicinal Chemistry

SAN DIEGO--(BUSINESS WIRE)-- Cullgen Inc., a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE™ platform of targeted protein degradation technology, today announced that the company’s internal program to develop selective degraders that target key BRAF mutant proteins has been accepted for publication by the Journal of Medicinal Chemistry. BRAF protein, which is necessary for normal cell signaling and cell growth function, is also one of the most frequently mutated genes in human cancers, including melanoma, colorectal, and thyroid cancers. The first-in-class degraders developed by Cullgen efficiently degrade mutated, disease causing forms of the BRAF protein and subsequently inhibit cancer cell growth.

According to the National Cancer Institute, over 96,000 new cases of melanoma were reported in the USA in 2019. Colorectal cancer is the fourth most common type of cancer diagnosed each year in the USA, with over 145,000 new cases and 51,000 deaths reported in 2019. Patients with BRAF-driven mutations of these cancers represent an important unmet clinical need and underscore the opportunity for promising new therapeutics.

“This seminal publication exemplifies the strength of our uSMITE™ technology to identify and develop novel and highly selective degraders for the treatment of important and debilitating diseases such as cancer,” stated Dr. Ying Luo, Chairman and President of Cullgen. “In addition to our multiple oncology degrader programs which are advancing smoothly through pre-clinical studies, we have also utilized our uSMITE™ platform to discover novel E3 ligands which we will use to develop completely new classes of targeted protein degraders.”

Journal of Medicinal Chemistry is a peer-reviewed science and medical journal published by a division of the American Chemical Society (ACS). The journal publishes innovative studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action.

About Cullgen Inc.

Cullgen is a privately held biopharmaceutical company dedicated to the development of first-in-class new chemical entities (NCEs) for the treatment of diseases lacking effective therapeutic approaches. We are developing our proprietary technology platform, ubiquitin-mediated, small molecule-induced target elimination technology, (uSMITE™), based on recent advances in the science of protein degradation. Typically, drugs are designed to interact with the functional sites of proteins and block their activities. We are developing uSMITE™ to expand the drug design paradigm beyond functional site inhibition, to make it possible to eliminate previously “undruggable” enzymes and proteins by targeted destruction. We also intend to use the uSMITE™ technology to harness the ubiquitin proteasome system, a multi-step biochemical process that controls protein degradation in all cells. From years of research on the proteasome system and key discoveries about its assembly, Cullgen’s founders have already demonstrated that the underlying technology can rapidly generate a large number of highly potent, selective, and bioavailable compounds. Furthermore, this process is significantly more cost effective compared with traditional drug discovery approaches. For more information, visit www.cullgen.com.

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