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Aug. 5, 2026
2026年8月5日
/PRNewswire/ -- Blacksmith Medicines, Inc. (Blacksmith), a leading biopharmaceutical company dedicated to discovering and developing therapeutics that target metalloenzymes, today announced the publication of research in the Journal of Medicinal Chemistry titled 'Discovery and Optimization of Novel Non-Hydroxamate LpxC Inhibitors for the Treatment of Multidrug-Resistant Gram-Negative Infections.'.
/美通社/ -- 专注于发现和开发靶向金属酶疗法的领先生物制药公司Blacksmith Medicines, Inc.(Blacksmith)今日宣布,其研究成果已在《药物化学杂志》上发表,题为“用于治疗的新型非羟肟酸LpxC抑制剂的发现与优化”。
'This peer-reviewed data demonstrates the capability of Blacksmith's chemistry platform to advance novel small-molecule inhibitors against challenging metalloenzyme targets,' said Zachary Zimmerman, Ph.D., CEO and co-founder of Blacksmith. 'LpxC has been studied for decades across the biopharmaceutical industry, with an overwhelming reliance on problematic hydroxamic acid to bind and inhibit the catalytic metal in the enzyme active site.
“这项经过同行评审的数据证明了Blacksmith的化学平台在推进针对具有挑战性的金属酶靶点的新型小分子抑制剂方面的能力,”Blacksmith首席执行官兼联合创始人Zachary Zimmerman博士表示。“LpxC在生物制药行业已被研究数十年,但长期以来严重依赖存在问题的羟肟酸来结合并抑制酶活性位点中的催化金属。”
The Blacksmith platform offers a differentiated solution by leveraging a proprietary metal-binding pharmacophore library to identify novel non-hydroxamate starting points for elaboration through rational drug design.'.
Blacksmith平台通过利用其专有的金属结合药效团库,为通过理性药物设计进行深化开发提供新颖的非羟肟酸类起始点,从而提供差异化的解决方案。
Blacksmith's lead antibacterial candidate targeting LpxC, FG-2101, is being advanced for both intravenous and oral administration for the treatment of susceptible and multidrug-resistant Gram-negative pathogens.
Blacksmith公司针对LpxC的领先抗菌候选药物FG-2101,正在推进用于静脉注射和口服给药,以治疗易感及多重耐药的革兰氏阴性病原体。
The FG-2101 program is currently supported under a contract with NIAID and was previously supported by CARB-X (see below for contract details).
FG-2101 项目目前在美国国家过敏和传染病研究所(NIAID)的合同支持下进行,此前曾获得 CARB-X 的支持(合同详情见下文)。
About LpxC
关于 LpxC
LpxC is a zinc-dependent hydrolase and an attractive antibiotic target that is conserved across Gram-negative bacteria but absent from Gram-positive species and human cells. Inhibition of LpxC results in potent, selective killing of Gram-negative bacteria. Previous LpxC inhibitors, primarily based on hydroxamic acid chemistry, have exhibited poor drug-like properties, and no LpxC-targeted therapies have been approved to date.
LpxC是一种锌依赖性水解酶,也是一个具有吸引力的抗生素靶点,它在革兰氏阴性菌中保守存在,但在革兰氏阳性菌和人类细胞中缺失。抑制LpxC会导致对革兰氏阴性菌的强效、选择性杀伤。以往的LpxC抑制剂主要基于羟肟酸化学结构,表现出较差的药物特性,迄今为止尚无针对LpxC的疗法获得批准。
Leveraging its proprietary chemistry platform, Blacksmith has developed novel non-hydroxamate LpxC inhibitors that demonstrate differentiated safety profiles and are efficacious in animal models against multidrug-resistant Gram-negative pathogens..
凭借自有的化学平台,Blacksmith 开发了新型非羟肟酸类 LpxC 抑制剂,这些抑制剂展现出差异化的安全性特征,并在针对多重耐药革兰氏阴性病原体的动物模型中显示出疗效。
About Metalloenzymes and the Blacksmith Platform
关于金属酶与Blacksmith平台
Metalloenzymes use metal ion cofactors in their active sites to carry out essential biological functions. Historically, these targets have been difficult to drug because conventional small-molecule chemistry has had limited ability to engage metal-dependent active sites with the precision needed for safe and effective therapeutics.
金属酶在其活性位点利用金属离子辅因子来执行关键的生物学功能。历史上,这些靶点一直难以进行药物开发,因为传统的小分子化学在精准作用于金属依赖性活性位点方面能力有限,难以满足开发安全有效疗法的需求。
The Blacksmith platform is designed to overcome these challenges through:.
Blacksmith 平台旨在通过以下方式克服这些挑战:
A proprietary fragment library of metal-binding pharmacophores;
一种专有的金属结合药效团片段库;
A comprehensive database that maps metalloenzyme functions, metal cofactors, and disease associations;
一个全面映射金属酶功能、金属辅因子和疾病关联的数据库;
A proprietary metallo-CRISPR library of custom single-guide RNAs;
一种专有的金属CRISPR库,包含定制的单引导RNA;
An advanced computational toolkit for docking, modeling, and structure-based drug design; and
用于分子对接、建模和基于结构的药物设计的先进计算工具包;以及
A robust intellectual property portfolio spanning bioinorganic, medicinal, and computational chemistry for metalloenzyme-targeted therapeutics.
针对金属酶靶向治疗药物,拥有涵盖生物无机化学、药物化学和计算化学的坚实知识产权组合。
About Blacksmith Medicines
关于黑smith药品
Blacksmith Medicines is pioneering the development of therapeutics that target metal-dependent enzymes, a large and important class representing more than 30% of all known enzymes across major categories, including oxidoreductases, transferases, hydrolases, lyases, isomerases, and ligases. These enzymes rely on essential metal ions—such as magnesium, zinc, iron, manganese, and copper—for catalytic activity.
Blacksmith Medicines 正在开创性地开发靶向金属依赖性酶的治疗药物。这是一类庞大且重要的酶,占已知主要类别酶(包括氧化还原酶、转移酶、水解酶、裂解酶、异构酶和连接酶)的30%以上。这些酶的催化活性依赖于必需的金属离子,如镁、锌、铁、锰和铜。
Blacksmith's purpose-built platform integrates a proprietary library of metal-binding pharmacophores with advanced computational modeling to design small-molecule inhibitors that precisely engage metal ions within enzyme active sites. This approach enables the rapid and predictable development of potent, selective inhibitors..
Blacksmith 的专用平台将专有的金属结合药效团库与先进的计算建模相结合,旨在设计能够精准作用于酶活性位点内金属离子的小分子抑制剂。这种方法能够实现强效、高选择性抑制剂的快速且可预测的开发。
The company has established strategic collaborations with Basilea Pharmaceutica International Ltd., Cyteir Therapeutics Inc., Eli Lilly and Company, Hoffmann-La Roche Ltd., and Zoetis LLC, and has secured non-dilutive funding from CARB-X and NIH/NIAID. Blacksmith's investors include Eli Lilly, Evotec A.G., MP Healthcare Partners, MagnaSci Ventures, and Alexandria Venture Investments..
该公司已与巴塞尔国际制药有限公司(Basilea Pharmaceutica International Ltd.)、Cyteir Therapeutics Inc.、礼来公司(Eli Lilly and Company)、霍夫曼-拉罗氏有限公司(Hoffmann-La Roche Ltd.)以及硕腾有限责任公司(Zoetis LLC)建立战略合作关系,并获得了来自CARB-X和美国国立卫生研究院/国家过敏和传染病研究所(NIH/NIAID)的非稀释性资金。Blacksmith的投资者包括礼来公司、Evotec A.G.、MP Healthcare Partners、MagnaSci Ventures以及Alexandria Venture Investments。
For more information, visit
更多信息,请访问
www.BlacksmithMedicines.com
www.BlacksmithMedicines.com
or follow Blacksmith Medicines on LinkedIn.
或在 LinkedIn 上关注 Blacksmith Medicines。
Media Contact:
媒体联系人:
Amy Conrad
艾米·康拉德
Juniper Point
杜松角
[email protected]
[email protected]
858-366-3243
858-366-3243
This program has been supported by CARB-X (4500002736) and is currently supported under a contract with NIAID (75N93022C00060).
本项目曾获得CARB-X(编号4500002736)的支持,目前正根据与美国国家过敏和传染病研究所(NIAID)签订的合同(编号75N93022C00060)获得支持。
Funding for CARB-X has been provided by federal funds from the U.S. Department of Health and Human Services (HHS); Administration for Strategic Preparedness and Response; Biomedical Advanced Research and Development Authority (BARDA) under agreement number 75A50122C00028 and by awards from Wellcome (WT224842), the UK Department of Health and Social Care's Global Antimicrobial Resistance Innovation Fund (GAMRIF), the Gates Foundation, Germany's Federal Ministry of Research, Technology and Space (BMFTR), the Novo Nordisk Foundation, The Public Health Agency of Canada, Italy's Ministry of Economy and Finance (MEF), Japan's Ministry of Health, the European Commission's DG Health Emergency Preparedness and Response Authority (DG HERA), and KfW Development Bank.
CARB-X 的资金由以下机构提供:美国卫生与公众服务部(HHS)下属的战略准备与响应管理局(ASPR)及生物医学高级研究与开发局(BARDA)提供的联邦资金(协议号 75A50122C00028);以及来自惠康基金会(WT224842)、英国卫生与社会保健部全球抗微生物药物耐药性创新基金(GAMRIF)、盖茨基金会、德国联邦研究与技术空间部(BMFTR)、诺和诺德基金会、加拿大公共卫生局、意大利经济与财政部(MEF)、日本厚生劳动省、欧盟委员会健康紧急准备与响应总局(DG HERA)和德国复兴信贷银行(KfW Development Bank)的资助。
The U.S. National Institute of Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health (NIH) in HHS, provides support in the form of in-kind services through access to a suite of preclinical services for product development. The content of this publication is solely the responsibility of the authors and does not necessarily represent the official views of any CARB-X funders..
美国卫生与公众服务部(HHS)下属国立卫生研究院(NIH)的国家过敏和传染病研究所(NIAID)通过提供一系列用于产品开发的临床前服务,以实物服务的形式给予支持。本出版物的内容完全由作者负责,并不一定代表任何 CARB-X 资助方的官方观点。
SOURCE Blacksmith Medicines
来源:铁匠药品
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