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Skeletal edit swaps carbon for nitrogen 骨骼编辑把碳换成氮
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-scicon4
None Mark Peplow, special to C&EN
A team of researchers led by Mark Levin at the University of Chicago has unveiled a reaction that can perform a C-to-N swap in aromatic molecules that already contain a nitrogen atom, such as quinolines ( Nature 2023, DOI: 10.1038/s41586-023-06613-4 ). This approach, along with another that Levin’s lab unveiled in September, should enable medicinal chemists to make these single-atom substitutions in a swath of common molecules, easing efforts to generate analogs of drug candidates. “This is the problem that I started my lab to tackle,” Levin says. The method is the latest entrant to the growing field of skeletal editing , which aims to add, delete, or swap single atoms within a molecule’s backbone. Such alterations can have a profound effect on a molecule’s biological activity. Swapping out carbon in favor of nitrogen is a common tactic for boosting the potency of pharmaceuticals, but in practice these analogs often
由芝加哥大学Mark Levin领导的一个研究小组揭示了一种反应,可以在已经含有氮原子的芳香分子中进行C-to-N交换,例如喹啉(Nature 2023, DOI: 10.1038/s41586-023-06613-4)。这种方法,加上莱文的实验室在9月份公布的另一种方法,应该能让药物化学家在一大片普通分子中进行单原子取代,从而减轻产生候选药物类似物的努力。莱文说:“这就是我开始我的实验室要解决的问题。”这种方法是不断发展的骨架编辑领域的最新进入者,其目的是在分子的主链中添加、删除或交换单个原子。这样的改变会对分子的生物活性产生深远的影响。用氮取代碳是提高药物效力的常用策略,但在实践中,这些类似物经常
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引用次数: 0
Trillium Renewable Chemicals 可再生化学物质
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-cover11
None Craig Bettenhausen
At a 2013 workshop held in a hotel at the Detroit airport, representatives from the Clean Energy Manufacturing Initiative of the US Department of Energy (DOE) asked a group of industry leaders how to reduce emissions from manufacturing carbon fiber—a strong and lightweight material used to replace steel and aluminum in airplanes, automobiles, and wind turbines. They all had the same response. “We need sustainable acrylonitrile,” they said, according to Corey Tyree, CEO and cofounder of Trillium Renewable Chemicals. Acrylonitrile is the raw material used to make carbon fiber. It’s also used as a feedstock for polymers such as nitrile rubber and acrylonitrile-butadiene-styrene, the plastic in Lego blocks. Conventional acrylonitrile is normally made from propylene, a petrochemical with a heavy carbon footprint. After the workshop, the DOE funded a project at the nonprofit Southern Research Institute to make biobased acrylonitrile. The team found a way, and Southern Research spun out
2013年,在底特律机场一家酒店举行的研讨会上,来自美国能源部清洁能源制造倡议(DOE)的代表向一群行业领袖询问了如何减少制造碳纤维的排放。碳纤维是一种坚固而轻质的材料,用于取代飞机、汽车和风力涡轮机中的钢和铝。他们的反应都是一样的。“我们需要可持续的丙烯腈,”他们说,据Trillium Renewable Chemicals的首席执行官兼联合创始人科里·泰里(Corey Tyree)说。丙烯腈是用来制造碳纤维的原料。它还被用作丁腈橡胶和丙烯腈-丁二烯-苯乙烯等聚合物的原料,这些聚合物是乐高积木中的塑料。传统的丙烯腈通常由丙烯制成,丙烯是一种碳足迹很大的石化产品。研讨会结束后,美国能源部资助了非营利组织南方研究所的一个项目,以制造生物基丙烯腈。这个团队找到了一种方法,南方研究公司成立了
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引用次数: 0
Gate launches to stop bad proteins at their source Gate发射是为了从源头阻止有害蛋白质
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-buscon4
None Gina Vitale
Drug designers try many different tricks to degrade badly behaving proteins. Much of the action in that space comes from companies developing small molecules like proteolysis targeting chimeras (PROTACs) , which degrade proteins that operate inside the cell. Gate Bioscience , a start-up backed by Versant Ventures that launched Nov. 1 with $60 million in series A funding, has set its sights on disease-causing proteins that are destined to end up outside the cell. The company’s name hints at the mechanism behind its small molecules, which work within a channel in a cell’s rough endoplasmic reticulum. For many extracellular proteins, getting through this channel is an important step on their path to exit the cell. Gate’s molecules bind in the channel, which prevents disease-causing proteins from escaping and allows good proteins to move freely through. Unable to leave, the stymied proteins are then degraded, according to Gate cofounder and CEO
药物设计者尝试了许多不同的方法来降解行为不良的蛋白质。该领域的大部分活动来自开发小分子的公司,比如靶向嵌合体(PROTACs)的蛋白水解,它可以降解细胞内的蛋白质。Gate Bioscience是一家由Versant Ventures支持的初创公司,于11月1日以6000万美元的a轮融资成立,该公司已将目光投向了注定要在细胞外结束生命的致病蛋白质。该公司的名字暗示了其小分子背后的机制,这些小分子在细胞粗糙的内质网的通道内工作。对于许多细胞外蛋白来说,通过这个通道是它们离开细胞的重要一步。Gate的分子结合在通道中,防止致病蛋白质逃逸,并允许有益蛋白质自由通过。Gate的联合创始人兼首席执行官表示,由于无法离开,受阻的蛋白质就会被降解
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引用次数: 0
BASF invests in collagen therapy 巴斯夫投资胶原蛋白疗法
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-buscon12
None Craig Bettenhausen
BASF has invested an undisclosed sum in the molecular biology start-up 3Helix. The firm makes specialized peptides that bind to damaged collagen molecules. 3Helix has so far commercialized its technology for medical imaging and diagnostic applications. BASF will gain exclusive rights to commercialize 3Helix’s platform for personal care applications, where a wide range of firms are building antiaging products around supporting or supplementing collagen in skin.
巴斯夫(BASF)向分子生物学初创企业3Helix投资了一笔数额不详的资金。该公司生产与受损胶原蛋白分子结合的特殊肽。到目前为止,3Helix已经将其技术商业化,用于医学成像和诊断应用。巴斯夫将获得3Helix个人护理应用平台的独家商业化权利,许多公司正在围绕支持或补充皮肤中的胶原蛋白构建抗衰老产品。
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引用次数: 0
H2Pro H2Pro
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-cover6
None Alex Scott
Most of the world’s hydrogen is made unsustainably from methane or coal, and today most of it is used to produce petroleum-based fuels and chemicals. But the start-up H2Pro says hydrogen could also be key to slowing climate change if it is made without fossil fuels. This can be done by taking hydrogen out of water using renewable electricity. Scientists have long known how to extract hydrogen from water. But existing electrolyzers, the machines used to split water molecules , convert only about 70% of the electric energy they use into chemical energy, which is stored as hydrogen. H2Pro has devised a two-step process that generates hydrogen and oxygen in separate steps, ensuring they don’t mix. Hen Dotan, H2Pro’s cofounder and chief technology officer, says his company’s technology converts about 95% of the electricity it uses into chemical energy, a rate that would yield substantial financial savings at commercial scale.
世界上大部分的氢都是不可持续地从甲烷或煤中获得的,而今天大部分的氢都被用来生产石油基燃料和化学品。但初创公司H2Pro表示,如果不使用化石燃料,氢也可能是减缓气候变化的关键。这可以通过使用可再生电力从水中提取氢来实现。科学家们早就知道如何从水中提取氢。但是现有的用于分解水分子的电解槽只能将大约70%的电能转化为化学能,这些化学能以氢气的形式储存起来。H2Pro设计了一种两步制程,分别生成氢气和氧气,以确保它们不会混合。H2Pro的联合创始人兼首席技术长Hen Dotan说,他的公司的技术将大约95%的电力转化为化学能,这一比率将在商业规模上节省大量资金。
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引用次数: 0
Single-catalyst stereoenrichment 单个因素stereoenrichment
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-scicon2
None Brianna Barbu
Sometimes, conformity is a good thing. Particularly when it comes to stereochemistry. While stereocenters arise in mirror-image enantiomer pairs when left to their own devices, enantiomers can have very different biological activity. So synthetic and medicinal chemists would prefer to make only one of them at a time. Researchers from the Shanghai Institute of Organic Chemistry, led by Zhiwei Zuo , have now added a new reaction to the stereoselective toolbox. They have devised a clever method for turning mixtures of alcohol isomers into an enantiomerically pure product using a single catalyst ( Science 2023, DOI: 10.1126/science.adj0040 ). Once a mixture of stereoisomers is created, it’s very difficult to amend it without separating the isomers from each other and throwing out the unwanted one. Mixtures have higher entropy, which the universe prefers. And something called the principle of microscopic reversibility says that any mechanistic step that flips an unwanted enantiomer
有时候,从众是一件好事。尤其是在立体化学方面。虽然立体中心在镜像对映体对中产生,但对映体可以具有非常不同的生物活性。所以合成化学家和药物化学家宁愿一次只制造一种。由左志伟领导的上海有机化学研究所的研究人员现在在立体选择工具箱中增加了一种新的反应。他们发明了一种聪明的方法,用一种催化剂将酒精异构体混合物转化为对映体纯产物(《科学》2023,DOI: 10.1126/ Science)。adj0040)。一旦形成了立体异构体的混合物,就很难在不分离异构体和不需要的异构体的情况下对其进行修饰。混合物具有更高的熵,这是宇宙所喜欢的。微观可逆性原理说任何翻转不需要的对映体的机械步骤
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引用次数: 0
Cypris Materials 托材料
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-cover3
None Vanessa Zainzinger, special to C&EN
The multicolored feathers of a peacock, the brilliant blue wings of a morpho butterfly, and the metallic golden shell of a Chrysina beetle have one thing in common: they get their stunning color from biological nanostructures that have exactly the right spacing to reflect certain wavelengths of light. Scientists have long been interested in using this phenomenon to lend color to manufactured goods because traditional dyes and pigments require lots of water, energy, and harmful substances, such as heavy metals, aromatic amines, volatile organic compounds, and phthalates. In 2016, Ryan Pearson, then a materials chemistry PhD student at the University of Colorado Boulder, heard the apparel giant Nike present its dye problem at an industry workshop he attended. “Color was this huge environmental footprint for them,” he says. “And that’s kind of when it all clicked for me.” Structure-based colorants could offer an environmentally friendly option, but they have so
孔雀的多彩羽毛,大闪蝶的亮蓝色翅膀,金龟子的金属金色外壳都有一个共同点:它们令人惊叹的颜色来自生物纳米结构,这些纳米结构具有精确的间隔来反射特定波长的光。长期以来,科学家们一直对利用这种现象给制成品增添颜色很感兴趣,因为传统的染料和颜料需要大量的水、能量和有害物质,如重金属、芳香胺、挥发性有机化合物和邻苯二甲酸盐。2016年,时任科罗拉多大学博尔德分校材料化学博士生的瑞安·皮尔森(Ryan Pearson)在他参加的一个行业研讨会上听到了服装巨头耐克(Nike)提出的染料问题。“色彩对他们来说是巨大的环境足迹,”他说。“就在那时,我豁然开朗了。”基于结构的着色剂可以提供一个环保的选择,但他们没有
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引用次数: 0
Newscripts’ Holiday Gift Guide Newscripts的节日礼物指南
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-newscripts
None Bethany Halford
Holiday gift ideas Chemistry-themed goodies for the scientists in your life Playing cards Who needs the queen of hearts when you’ve got the queen of benzene? This chemistry-themed deck of cards features prominent chemists and molecular suits, $17.50 from the OneCreativeAcademic shop on Etsy. Pins These chemistry cat-themed pins are purrfect for decorating backpacks and book bags, $12.99 per 3 cm tall pin at the ItsKindaCatchyShoppe on Etsy. Magnets Stick important memos and papers to fridges and filing cabinets with these colorful flask-shaped tags backed with neodymium magnets, $9.75 for a set of 6 of the 1.75 cm tall magnets in rainbow colors from the yakitori store on Etsy. Embroidered cap Add molecular flair to your headwear with these embroidered caps from the embroideredchem shop on Etsy. Customize the molecule for $25 or choose from favorites like caffeine for $22. Whiskey glass Toast the evolution of the molecular model with
节日礼物创意给你生命中的科学家的化学主题的糖果打牌当你有了苯皇后谁还需要红心皇后?这副以化学为主题的卡片以著名化学家和分子套装为特色,Etsy上的OneCreativeAcademic商店售价17.50美元。这些以化学猫为主题的别针非常适合装饰背包和书包,Etsy上ItsKindaCatchyShoppe上每3厘米高的别针售价12.99美元。把重要的备忘录和文件贴在冰箱和文件柜上,贴上这些彩色的瓶子形状的标签,背面是钕磁铁,一套6块,高1.75厘米,彩虹色,从Etsy上的烤鸡肉店买到,售价9.75美元。从Etsy上的绣花化学商店为你的头饰添加分子的天赋。自定义分子的价格为25美元,或者选择喜欢的咖啡因,价格为22美元。威士忌酒杯的演变与分子模型的搭配
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引用次数: 0
Business Roundup 业务综述
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-buscon18
BUSINESS Business Roundup ShareShare onFacebookTwitterWechatLinked InRedditEmail C&EN, 2023, 101 (37), p 13November 13, 2023Cite this:C&EN 101, 37, 13Abstract Braskem will supply Indorama subsidiary Oxiteno with ethylene made from renewable sources. Braskem says its biobased ethylene, which is derived from sugar cane and corn ethanol, has been certified under the International Sustainability and Carbon Certification scheme. Montinutra has raised $2.1 million for a demonstration plant in Vilppula, Finland, that will convert forestry waste products into biobased chemicals for binders, coatings, and other products. The firm says it can make chemicals from cellulose, hemicellulose, and lignin. OMV has formed a joint venture with the plastics recycler Interzero that plans to build a plant in Walldürn, Germany, capable of sorting up to 260,000 metric tons per year of mixed waste plastic. OMV will use sorted plastic waste from the plant as feedstock for making pyrolysis oil for new plastic production.  Aclarity has raised $15.9 million in series A funding led by the water-focused venture capital fund Aqualateral. Aclarity isView: PDF | Full Text HTMLDownload PDF
商业商业综合报道共享于facebook twitter微信链接于reddite电子邮件C&EN, 2023,101 (37), p 13 11月13日引用此:C&EN 101,37,13摘要布拉斯科姆将向Indorama子公司Oxiteno提供由可再生能源制成的乙烯。布拉斯科公司说,它的生物基乙烯是从甘蔗和玉米乙醇中提取的,已经通过了国际可持续发展和碳认证计划的认证。Montinutra已经为芬兰Vilppula的一家示范工厂筹集了210万美元,该工厂将把林业废弃物转化为生物基化学品,用于粘合剂、涂料和其他产品。该公司表示,它可以从纤维素、半纤维素和木质素中制造化学物质。OMV与塑料回收商Interzero成立了一家合资企业,计划在德国walld建立一家工厂,每年能够分拣多达26万吨的混合废塑料。OMV将使用从工厂中分类的塑料废物作为原料,生产用于新塑料生产的热解油。clarity在A轮融资中获得1590万美元,领投方是专注于水资源的风险投资基金Aqualateral。清晰度isView: PDF |全文html下载PDF
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引用次数: 0
BMS buys Orum’s cancer drug BMS买下了Orum的抗癌药物
Pub Date : 2023-11-13 DOI: 10.1021/cen-10137-buscon14
None Laura Howes
Bristol Myers Squibb has purchased Orum Therapeutics’ protein degrader for treating acute myeloid leukemia or high-risk myelodyplastic syndromes. For an up-front payment of $100 million, BMS gets ORM-6151, a molecular-glue drug that is coupled to an antibody. The antibody helps the drug be delivered to cancer cells. There, the glue portion of ORM-6151 is released and marks the target protein GSPT1 for degradation, which ultimately kills the cancer cell.
百时美施贵宝(Bristol Myers Squibb)收购了Orum Therapeutics的蛋白质降解剂,用于治疗急性髓性白血病或高风险骨髓增生综合征。BMS先支付1亿美元,就可以获得ORM-6151,这是一种与抗体偶联的分子胶药物。这种抗体有助于药物被运送到癌细胞中。在那里,ORM-6151的粘合部分被释放,并标记目标蛋白GSPT1进行降解,最终杀死癌细胞。
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引用次数: 0
期刊
C&EN Global Enterprise
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