merck p53 peptide patent Merck - collagen-peptides-serum-anti-wrinkle peptides Merck's Pioneering Work in p53 Peptide Patents: Advancing Cancer Therapeutics

sj-peptides-reviews The intricate world of cancer research is continuously evolving, with a significant focus on understanding and manipulating the p53 tumor suppressor gene. Patents related to p53 and its associated peptides are at the forefront of developing novel therapeutic strategies. Merck, a global leader in biopharmaceuticals, has been actively involved in this domain, as evidenced by numerous patent filings and research collaborations. This article delves into the merck p53 peptide patent landscape, exploring key innovations, scientific underpinnings, and the broader implications for cancer treatment作者：AL Czarna·2009—Upon binding to Mdm2, thep53 peptideforms an amphipathic helix highly complementary to the hydrophobic pocket at the Mdm2 surface. Main contacts for the ....

At the core of this research is the p53 protein, often referred to as the "guardian of the genome," which plays a crucial role in preventing tumor formation. Mutations in the p53 gene are among the most frequent genetic alterations in human cancers, leading to the loss of its tumor-suppressive functions. Consequently, a significant research effort is directed towards developing therapeutic agents that can either restore the function of mutated p53 or exploit its specific vulnerabilities.

Several patent applications highlight efforts to create stabilized alpha-helix of p53 (SAH-p53) peptides作者：MH Reutershan·2021·被引用次数：26—An updatepatentreview of MDM2–p53interaction inhibitors (2019–2023). Expert Opinion on TherapeuticPatents2024, 34 (12) , 1177-1198.. These peptides are designed to exhibit high affinity for proteins that interact with p53, such as HDM2Biopharmaceuticals: The Patent Implications of Peptide Therapeutics. By stabilizing the alpha-helical structure of p53, these peptides can effectively modulate the p53-HDM2 interaction, a key regulatory axis in cancer. For instance, UPhase 2a study of a novel stapled peptide ALRN-6924 ....S. Patent US9527896B2 describes such stabilized alpha-helix of p53 (SAH-p53) peptides and their therapeutic applications. The ability to create more stable peptide formats is crucial for their efficacy as drug candidates, addressing challenges like rapid degradation in the body.

Furthermore, research has focused on developing peptides that can reactivate p53 mutants.US8343760B2 - p53 activator peptides Many cancer-associated p53 mutations result in misfolded or inactive proteins. The development of novel polypeptides that activate p53 aims to restore the function of these mutated forms. This includes strategies to refold misfolded p53 or to enhance the activity of partially functional mutants.Here in TABLE 1 we highlight selectedpatentapplications published in the past year related top53. Data were researched using the Espacenet database. NEWS & ... The goal is to leverage the inherent tumor-suppressive capabilities of p53, even in its mutated state.Described herein arestabilized alpha-helix of p53 (SAH-p53) peptidesthat exhibit high affinity for HDM2, and, in contrast to the corresponding unmodified p53 ...

Merck's involvement is evident in various patent assignments and collaborations. For example, MERCK PATENT GmbH is listed as an assignee in patents related to therapeutic agents.(PDF) Tumor-Targeted Delivery of the p53-Activating ... The company has also been involved in collaborations, such as the one with Astex Pharmaceuticals to discover small molecule candidates for cancer treatment, indicating a broad approach to targeting cancer pathways, including those involving p53. Moreover, research has explored the use of p53-activating peptides in targeted delivery systems. For instance, studies have investigated using epidermal growth factor receptor (EGFR)-targeted lipodisks to deliver p53-activating stapled peptide VIP116 to EGFR-expressing tumors.

The concept of "stapled peptides" represents a significant advancement in peptide therapeutics. These peptides, like ALRN-6924, the first-in-class clinical stage stapled peptide, are structurally modified to enhance their stability and cell permeability. ALRN-6924 is a cell-penetrating stapled alpha-helical peptide designed to disrupt the interaction between the p53 tumor suppressor protein and its inhibitors, such as MDM2 and MDMX. This approach aims to restore p53 function in cancer cells. The patent landscape includes filings like EP3256484A1, which may be related to Merck's work on macrocyclic peptides and potentially stapled peptides.

Beyond directly targeting p53 or its interactions, patents also cover p53 biomarkers.2025年10月17日—Here, we utilized epidermal growth factor receptor (EGFR)-targeted lipodisks to deliverp53-activating stapledpeptideVIP116 to EGFR-expressing ... U.S.European Patent O Patent EP3159696A1 relates to the identification of p53 biomarker profiles that can predict patient response to therapies, particularly in hyperproliferative diseases. This highlights the importance of companion diagnostics in the development of p53-targeted therapies.

The scientific rationale behind these merck p53 peptide patent endeavors is rooted in a deep understanding of molecular biology and cancer genetics. Upon binding to Mdm2, the p53 peptide typically forms an amphipathic helix that is complementary to a hydrophobic pocket on the Mdm2 surface. Disrupting this interaction can stabilize p53 and allow it to perform its tumor-suppressive functions. Research into p53 mutations, such as the p53 Y220C mutation, has led to the development of specific reactivators like Rezatapopt (PC14586), which is being evaluated in clinical trials. Similarly, compounds are being designed to target specific p53 mutant forms, such as the p53 R175H peptide, with agents like CLSP-1025 being developed for this purposeUS9527896B2 - Stabilized p53 peptides and uses thereof.

The broader field of peptide therapeutics is also reflected in the patent literature. Patents related to peptide synthesis, modification, and delivery are essential for advancing these technologies.2023年8月9日—Astex Pharmaceuticals andMerck(MSD) have expanded their collaboration to identify small molecule candidates for cancer treatment. For example, patents assigned to Merck Patent cover processes for selective enzymatic hydrolysis of peptide esters, underscoring the company's interest in optimizing peptide manufacturing. The development of peptide mimetics, such as dimeric benzodiazepines, also represents an innovative approach to targeting p53-dependent drug resistance in cancers.

In summary, the merck p53 peptide patent domain is characterized by a multi-faceted approach to harnessing the power of the p53 tumor suppressor.The disordered p53 transactivation domain is the target of ... From stabilized alpha-helical peptides to mutant p53 reactivators and p53 biomarker identification, Merck and its collaborators are making significant contributions to the field. The ongoing research and patenting activities underscore the immense therapeutic potential of targeting the p53 pathway in the fight against cancer, offering hope for more effective and personalized treatment strategies. The continuous innovation in peptide design and delivery, coupled with a growing understanding of p53 biology, promises to yield groundbreaking advancements in oncology.