Peptomyc’s Post

🚀 𝐄𝐱𝐜𝐢𝐭𝐢𝐧𝐠 𝐍𝐞𝐰𝐬 𝐢𝐧 𝐏𝐫𝐞𝐜𝐢𝐬𝐢𝐨𝐧 𝐎𝐧𝐜𝐨𝐥𝐨𝐠𝐲! 🚀 Revolutionary advancements in precision oncology have been achieved through innovative strategies like genomic sequencing and the development of small-molecule kinase inhibitors. However, adaptive resistance mechanisms pose challenges for long-term treatment efficacy, calling for novel combination therapies. A recent study introduces MTX-531, a dual inhibitor of EGFR and PI3K designed for high selectivity and potency. Preclinical studies demonstrate promising results in treating head and neck squamous cell carcinomas (HNSCC) and colorectal cancer (CRC), particularly in combination with RAS-MAPK pathway intervention. MTX-531 shows remarkable efficacy in preclinical models, offering a potential solution to treatment failures associated with previous PI3K inhibitors. Notably, MTX-531 exhibits low-nanomolar potency against EGFR and PI3Kα with minimal off-target effects, setting it apart from existing inhibitors. The study's findings suggest that MTX-531 may address the challenges of toxicity and resistance commonly encountered in precision oncology treatments. 🌟💊🔬 #PrecisionOncology #CancerResearch #BioPharmaResearch 🖇 Link to the study in the comment below. 🖼 Image by Peter H from Pixabay

We're delighted to announce our recent publication in the European Journal of Medicinal Chemistry Reports, which introduces a novel benzoazipinone derivative, compound 12a. This pioneering research highlights that 12a significantly inhibits MKLP2 activity and suppresses tumor growth in preclinical models. Representing a promising new scaffold, compound 12a offers potential for further development in targeting MKLP2, a previously underexploited target in cancer therapy. Read the full text here: https://lnkd.in/ed-Z7_Uf #publication #Cancer #MKLP2 #MedicinalChemistry

Gilead recently conducted a clinical trial for GS-3583, an FMS-like tyrosine kinase 3 (FLT3) agonist Fc fusion protein. Gilead collaborated with NuProbe to develop a qBDA panel that targeted multiple AML hotspot mutations. This qBDA panel significantly helped in the accurate and sensitive detection of drug-induced mutation emergence down to 0.06% variants allele frequency with minimal sequencing depth, offering more information for the trial’s efficacy evaluation. Gilead discovered that other NGS methods were unable to detect what NuProbe's innovative qBDA technology detected. NuProbe’s qBDA technology enhances the precision and effectiveness of cancer therapy research and development.   Learn more about Gilead’s clinical trial published in the AACR Editor’s Picks here: https://lnkd.in/gngWUVVX

Led by Alejandro Villagra, researchers from The George Washington University, co-authored a research paper, “Cell therapy using ex vivo reprogrammed macrophages enhances anti-tumor immune responses in melanoma,” published in the Journal of Experimental & Clinical Cancer Research. In this study, researchers demonstrate a new method to boost the effectiveness of macrophage-based cell therapy for treating melanoma. The innovative aspect of this study is treating macrophages with HDAC6 inhibitors (HDAC6i) before introducing them to tumors, which helps to maintain the M1 (tumor fighting) state and prevents them from turning to the M2 (tumor supporting) state. Read more about the research: https://lnkd.in/g8zsJYkD  Alejandro Villagra is also co-inventor of GW technology “Novel Combination Immunotherapy Targeting CD47-SIRPα Axis and HDAC6 Inhibition,” licensed by Avstera Therapeutics Corp., an oncology-focused biotech company. Avstera received approval from the US FDA to conduct a Phase I a/b trial for AVS100, a drug based on the same technology. Read more about the technology: https://lnkd.in/ewVPPEgh #GWU #TCO #CancerResearch #Melonoma #Research #TechTransfer 

Advancing a first-in-class AI-enabled cancer drug. A new article from Diana Spencer in Drug Discovery World looks at our REC-1245 program, a potentially first-in-class small molecule that recently received FDA IND clearance for a Phase 1/2 clinical trial for biomarker-enriched solid tumors and lymphoma. ▪ She writes: “Recursion identified the novel regulatory role of RBM39 associated with CDK12 using its maps of biology and first reported this relationship in early 2023, and notes that “preclinical data support that RBM39 degradation induces splicing defects which downregulate DNA Damage Response (DDR) networks and cell cycle checkpoints.” ▪ Chris Gibson says: “REC-1245 is a prime example of using an expansive AI-enabled platform for drug discovery. After exploring many predicted biological and chemical relationships across our maps of biology, we identified RMB39 as a novel target that looks functionally similar to the well-known but hard to drug target CDK12. We also identified and optimized small molecules that target RBM39 without directly impacting CDK12 or CDK13 using these same AI-enabled maps.” 👉 Read more: https://lnkd.in/ePy9XY5S #ai #clinicaltrials #techbio #cancer #tumor #cdk12 #rbm39

We are delighted to announce the publication of our recent article. “The effects of metformin and PCL‐sorafenib nanoparticle co‐treatment on MCF‐7 cell culture model of breast cancer” "Naunyn-Schmiedeberg's Archives of Pharmacology" (Q=2, IF=3.6 (2022)). Breast cancer, which is known for its aggressive nature and resistance to conventional therapies, remains a significant challenge across diverse demographics. Recently, the combination of sorafenib with other drugs has been shown to increase the efficiency of breast cancer treatment and is considered a promising alternative or supplementary procedure. In this study, we combined Sorafenib/PCL-sorafenib with metformin to improve drug absorption and promote therapeutic efficiency. Notably, our observations showed that this combination increased sorafenib absorption at lower doses and led to apoptosis and increased oxidative stress in MCF-7 cells. #breastcancer #drugdelivery #nanoparticle

September 2024, Prostate Cancer Awareness Month. 🔎 Prostate cancer is a major leading cause of cancer-related deaths in men with an incidence rate that is foreseen as increasing*. Although recent therapeutic advances have brought some relief, such as, for example, PARP inhibitors, androgen biosynthesis inhibitors, androgen receptor antagonists of second generation, many efforts still need to be made to achieve sustained disease control and long-term survival of patients with prostate cancer. There is an urgent need to characterize the many pathways that are involved in prostate cancer diseases. 🔬 At NovAliX, we provide an integrated offer from medicinal chemistry, in vitro pharmacology, relevant rodent in vivo pharmacology models to DMPK, translational science and histology solutions to support your projects throughout the drug discovery process. ▶️ Contact us to learn how we can support your discovery projects on cancer disease: https://lnkd.in/e9WnGYyQ *Figure source: https://lnkd.in/ecDzVQWi #drugdiscovery #pharmacology #medicinalchemistry #Cancer #ProstateCancer

Prostate cancer is the second most common cancer in men globally, with over 1.4 million cases reported in 2020. Early-stage survival rates are high, but significantly decline in advanced stages, highlighting the need for more effective treatments. A recent study using our TRC research chemicals identified the enzyme 2,4-dienoyl CoA reductase 2 (DECR2) as a promising therapeutic target. When combined with standard androgen receptor inhibitors, depletion of the DECR2 enzyme showed potential in treating preclinical models of castration-resistant prostate cancer. If you want to know more, read the full study in the British Journal of Cancer: https://okt.to/n8CZNb #ProstateCancer #oncology #oncologyresearch #ResearchChemicals

In a study funded by our division, Meisam Bagheri, Ph.D., Todd Miller, PhD, Diwakar Pattabiraman, et al. found that eribulin (an FDA-approved chemotherapeutic drug) induces chromatin remodeling to reverse epithelial to mesenchymal transition and sensitizes cancer cells to other chemotherapies in preclinical models of triple-negative #BreastCancer. https://lnkd.in/erd5cpTu

Kronos Bio announces the first patient dosed in an expansion cohort with KB-0742 at a dose of 80mg given on a four-days-on, three-days-off schedule. This expansion cohort is enrolling platinum-resistant patients with high-grade serous ovarian cancer (HGSOC). Many cancers exhibit transcriptional deregulation, often characterized by gene amplifications of MYC family oncogene. Targeting the transcription elongation cofactor, cyclin-dependent kinase 9 (CDK9) has emerged as a therapeutic strategy to disrupt MYC oncogenic activity. KB-0742 is an oral highly selective CDK9 inhibitor designed for the treatment of patients with MYC-amplified and other transcriptionally addicted relapsed or refractory solid tumors, including ovarian, lung, and triple-negative breast cancers. Chemenu supports your scientific research and drug discovery. Check our product catalog: https://lnkd.in/gHzCZpGb #MYC #tumors #ovariancancer #OC #HGSOC #CDK9 #inhibitor #buildingblocks #chemenu