In a groundbreaking development, Blacksmith Medicines, Inc., a renowned biopharmaceutical company dedicated to the discovery and development of medicines targeting metalloenzymes, unveiled preclinical findings on its oncology program focusing on flap endonuclease 1 (FEN1). This structure-specific metallonuclease plays a crucial role in cleaving 5′ DNA flaps during replication and repair processes.
The announcement was made by Dr. Zachary Zimmerman, CEO of Blacksmith, at the prestigious American Association for Cancer Research (AACR) Annual Meeting 2024 held at the San Diego Convention Center in San Diego, California. Dr. Zimmerman highlighted the significance of FEN1 as a therapeutic metalloenzyme and the challenges faced in previous drug discovery efforts due to limitations in chemistry.
Utilizing their innovative metalloenzyme fragment-based drug discovery approach, Blacksmith identified a potent and selective inhibitor of FEN1, named BSM-1516. This inhibitor demonstrated remarkable efficacy, being approximately 65-fold more potent against FEN1 compared to its related enzyme Exonuclease 1 (Exo1). The selective targeting of FEN1 was validated through various assays, including cellular thermal shift assay and clonogenic assays.
Moreover, the study revealed that BRCA2-deficient cells exhibited increased sensitivity to FEN1 inhibition, highlighting the potential of this inhibitor in treating HR deficient cancer cells. In addition, synergistic interactions were observed between BSM-1516 and various DDR inhibitors, opening up new possibilities for combination therapies in cancer treatment.
The promising results from the preclinical data paved the way for further investigations, including in vivo testing of BSM-1516 as a single agent or in combination with other synergistic DDR inhibitors. The company’s commitment to advancing the field of metalloenzyme-targeted medicines was underscored by their comprehensive approach, combining a proprietary fragment library, metallo-CRISPR technology, and advanced computational tools.
Blacksmith Medicines has established strategic collaborations with leading pharmaceutical companies and received funding from prominent organizations like CARB-X and NIH/NIAID. With a focus on developing innovative treatments targeting metal-dependent enzymes, Blacksmith is poised to make significant contributions to the field of oncology and beyond.
For more information about Blacksmith Medicines and their groundbreaking research, visit their website at www.BlacksmithMedicines.com or connect with them on LinkedIn. For media inquiries, please contact Amy Conrad at Juniper Point.
This news article was sourced from Blacksmith Medicines and was disseminated through PRNewswire. the recent spike in COVID-19 cases in the UK.
In recent weeks, the United Kingdom has experienced a significant surge in COVID-19 cases, raising concerns among health officials and the general public. The rise in infections has been attributed to the highly transmissible Delta variant, which has become the dominant strain in the country.
According to the latest data from Public Health England, the number of daily new cases has more than doubled in the past month, with the majority of infections occurring in younger, unvaccinated individuals. This worrying trend has prompted the government to take action to curb the spread of the virus.
In response to the surge in cases, Prime Minister Boris Johnson has announced a delay to the final stage of reopening, originally scheduled for June 21st. This decision has been met with mixed reactions, with some welcoming the cautious approach and others expressing frustration at the continued restrictions.
Health Secretary Matt Hancock has urged the public to remain vigilant and follow the guidelines to prevent further spread of the virus. He stressed the importance of getting vaccinated, especially as the Delta variant has shown to be more resistant to the available vaccines.
In light of the rising cases, testing and contact tracing efforts have been ramped up across the country. Mobile testing units have been deployed to hotspot areas, and additional resources have been allocated to track and isolate positive cases.
The surge in cases has also put pressure on the healthcare system, with hospitals reporting an increase in COVID-19 admissions. Health officials have warned that if the current trend continues, there could be a strain on hospital capacity, potentially leading to a rise in serious illnesses and deaths.
In an effort to address the situation, the government has launched a campaign to encourage vaccination uptake, particularly among younger age groups. Pop-up vaccination clinics have been set up in communities with lower vaccine coverage, and efforts are being made to reach out to those who may be hesitant or unsure about getting vaccinated.
As the UK grapples with this latest wave of infections, experts are emphasising the importance of continued vigilance and adherence to public health measures. While the vaccination programme has been successful in reducing severe illness and death, it is crucial that the public remains cautious and follows the guidelines to prevent further spread of the virus.
In conclusion, the recent spike in COVID-19 cases in the UK is a cause for concern, and efforts are being made to control the spread of the virus. With the Delta variant posing a significant threat, it is imperative that the public remains vigilant and takes the necessary precautions to protect themselves and others..
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