Myc targeting by omo 103 in solid tumors a phase 1 trial pubmed The omomyc peptide represents a significant advancement in cancer therapy, emerging as a direct inhibitor of the MYC oncoprotein. This innovative peptide, also referred to as omoMYC or OMO-103 in its therapeutic form, is engineered to specifically target and disrupt the function of MYC, a transcription factor critically involved in the development and progression of numerous cancers. As the first MYC-targeted therapy to successfully complete early-stage clinical trials, the omomyc peptide holds substantial promise for treating a wide range of solid tumors by offering a novel therapeutic approach to a previously undruggable target.2016年10月26日—Expression of a dominant-negative allele of MYC, termed OmoMYC,can induce rapid tumor regression in mouse modelswith little toxicity for ...
MYC is a family of oncogenic transcription factors that play a fundamental role in regulating cell growth, proliferation, and differentiation. In many cancers, MYC is aberrantly overexpressed, driving uncontrolled cell division and tumor formation. Its involvement in such a broad spectrum of malignancies has made it a highly sought-after target for drug development, but its complex structure and function have historically posed significant challenges. The development of the omomyc peptide marks a breakthrough in overcoming these obstacles.Intrinsic cell-penetrating activity propels Omomyc from ...
The omomyc peptide functions as a dominant-negative inhibitor.Blocking Myc to Treat Cancer: Reflecting on Two Decades ... It is designed to mimic MYC's structure, specifically its DNA-binding domain and coiled-coil region. By binding to the same E-box sequences in DNA that MYC normally targets, omomyc effectively blocks MYC from initiating the transcription of genes essential for cancer cell survival and proliferation. This interference leads to reduced MYC transcriptional activity, ultimately causing tumor regression and inhibiting cancer growth.
Research has demonstrated that the purified omomyc mini-protein exhibits intrinsic cell-penetrating properties, allowing it to efficiently enter cancer cells without the need for specialized delivery systems. This characteristic is crucial for its therapeutic efficacy.作者：ZZ Brown·2019·被引用次数：22—An abbreviated form of the c-Myc protein, called Omomyc,consists of the Myc DNA-binding domain and a coiled-coil regionto facilitate ... Studies have shown that omomyc can induce rapid tumor regression in preclinical models with minimal toxicity to healthy cells.作者：CP Cerrato·2025·被引用次数：6—We demonstrate the efficient delivery ofomoMYC, the first MYC inhibitor in clinical trials, using HBpep-SP, an engineeredpeptideforming liquid–liquid phase- ... Furthermore, omomyc has been observed to cause significant decreases in MYC promoter occupancy and alter the expression of genes that are heavily influenced by oncogenic MYC levels2025年8月21日—The outcomes of this study suggest that the inhibition of c-Myc exerted byOmomyc peptidereduces significantly cell growth and migration..
Omomyc has progressed into clinical trials, notably as OMO-103, a therapeutic agent developed by Peptomyc SL. Phase 1 trials have focused on evaluating the safety and efficacy of OMO-103 in patients with advanced solid tumors作者：E Wang·2018·被引用次数：94—Herein, we describe the engineering of thedominant-negative MYC peptide (OmoMYC) linked to a functional penetrating 'Phylomer' peptide (FPPa) as a therapeutic .... The results from these early studies are encouraging, with reports of patients responding positively to the treatmentBlocking Myc to Treat Cancer: Reflecting on Two Decades ....
Beyond its direct application, the omomyc peptide is also being explored in combination therapies and as a basis for developing improved variants.作者：MJ Demma·2019·被引用次数：111—The MYC inhibitorOmomyccan reduce the ability of MYC to bind specific box sequences in promoters of MYC target genes by binding directly to E box sequences. For instance, research is investigating the combination of omomyc with other cancer treatments, such as PARP inhibitors in breast cancer, to enhance therapeutic outcomesBlocking Myc to Treat Cancer: Reflecting on Two Decades .... Efforts are also underway to engineer omomyc-based cell-penetrating peptides and conjugates, like EV20/Omomyc, which links omomyc to an anti-HER3 antibody, to further refine its targeting and delivery capabilities.
The omomyc peptide represents a groundbreaking development in the fight against cancer. By directly targeting the MYC oncoprotein, a key driver of tumor development, omomyc offers a novel and potentially highly effective therapeutic strategy. Its inherent cell-penetrating ability and demonstrated efficacy in preclinical and early clinical studies underscore its promise2016年10月26日—Expression of a dominant-negative allele of MYC, termed OmoMYC,can induce rapid tumor regression in mouse modelswith little toxicity for .... As research and clinical trials continue, the omomyc peptide and its derivatives are poised to become vital tools in the oncologist's arsenal, offering new hope for patients battling a wide range of MYC-driven cancers.
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