FOR IMMEDIATE RELEASE
ACS News Service Weekly PressPac: November 03, 2021
A quick, high-yield synthesis of molnupiravir, an investigational COVID antiviral pill
"Engineered Ribosyl-1-Kinase Enables Concise Synthesis of Molnupiravir, an Antiviral for COVID-19"
ACS Central Science
As SARS-CoV-2 continues to spread and mutate, it’s important to identify new treatment options. Molnupiravir is an investigational oral antiviral being developed for the treatment of COVID-19, and has been submitted for review by the U.S. Food and Drug Administration. Researchers now report in ACS Central Science that they have engineered enzymes to help manufacture the pill, resulting in a much shorter and higher-yielding synthesis than current methods.
Originally developed to treat influenza, molnupiravir works by causing viruses to make errors when copying their own RNA, introducing mutations that inhibit replication. Recently, interim phase 3 clinical trial findings indicated that molnupiravir reduced the risk of hospitalization and death from COVID-19 for newly diagnosed, at-risk patients, and that it worked equally well against different SARS-CoV-2 variants. John McIntosh, Patrick Fier and colleagues at Merck and Codexis set out to develop a shorter, higher-yielding and sustainable way to synthesize the molecule.
The researchers developed a three-step synthesis of molnupiravir from a sugar molecule called ribose. They identified enzymes or chemical treatments to sequentially add the appropriate chemical groups to ribose to generate the molecule. For the second step of the synthesis, the team identified bacterial enzymes that weakly catalyzed the desired reactions. Using in vitro evolution, they greatly enhanced these enzymes’ activities. The new synthetic route, which also included a phosphate recycling strategy, was 70% shorter and had a seven-fold higher overall yield than the original route.
The authors acknowledge funding from Merck Sharp & Dohme Corp.
###
The American Chemical Society (ACS) is a nonprofit organization founded in 1876 and chartered by the U.S. Congress. ACS is committed to improving all lives through the transforming power of chemistry. Its mission is to advance scientific knowledge, empower a global community and champion scientific integrity, and its vision is a world built on science. The Society is a global leader in promoting excellence in science education and providing access to chemistry-related information and research through its multiple research solutions, peer-reviewed journals, scientific conferences, e-books and weekly news periodical Chemical & Engineering News. ACS journals are among the most cited, most trusted and most read within the scientific literature; however, ACS itself does not conduct chemical research. As a leader in scientific information solutions, its CAS division partners with global innovators to accelerate breakthroughs by curating, connecting and analyzing the world’s scientific knowledge. ACS’ main offices are in Washington, D.C., and Columbus, Ohio.
Registered journalists can subscribe to the ACS journalist news portal on EurekAlert! to access embargoed and public science press releases. For media inquiries, contact newsroom@acs.org.
Note: ACS does not conduct research but publishes and publicizes peer-reviewed scientific studies.
Media Contact
ACS Newsroom
newsroom@acs.org
###
La sociedad American Chemical Society (ACS) es una organización sin fines de lucro fundada en 1876 y aprobada por el Congreso de los Estados Unidos. La ACS se ha comprometido a mejorar la vida de todas las personas mediante la transformación del poder de la química. Su misión es promover el conocimiento científico, empoderar a la comunidad global y defender la integridad científica, y su visión es un mundo construido basándose en la ciencia. La Sociedad es líder mundial en la promoción de la excelencia en la educación científica y en el acceso a información e investigación relacionadas con la química a través de sus múltiples soluciones de investigación, publicaciones revisadas por expertos, conferencias científicas, libros electrónicos y noticias semanales periódicas de Chemical & Engineering News. Las revistas de la ACS se encuentran entre las más citadas, las más fiables y las más leídas en la literatura científica; sin embargo, la propia ACS no realiza investigación química. Como líder en soluciones de información científica, su división CAS se asocia con innovadores internacionales para acelerar los avances mediante la preservación, la conexión y el análisis de los conocimientos científicos del mundo. Las sedes principales de la ACS se encuentran en Washington, D.C., y Columbus, Ohio.
Los periodistas registrados pueden suscribirse al portal de noticias para periodistas de ACS en EurekAlert! para acceder a comunicados de prensa públicos y retenidos. Para consultas de los medios, comuníquese con newsroom@acs.org.
Nota: ACS no realiza investigaciones, pero publica y divulga estudios científicos revisados por expertos.
View larger image