
Click chemistry reactions may boost cancer-fighting drug potency LA JOLLA, CA Feb. 16, 2018 Researchers at The Scripps Research Institute (TSRI) have developed a quick and easy way to simultaneously modify dozens of drugs or molecules to improve their disease-fighting properties. Using the approach, scientists exchanged one chemical group for another in 39 cancer drugs and discovered under lab conditions that the chemically altered versions of three of the drugs had more potent anti-cancer activity.
The results, published today in the Journal of the American Chemical Society, reveal a powerful application of so-called click chemistry to drug discovery.
Usually you have to make thousands or millions of molecules and go through a big screening process to find one or two molecules that are interesting and might work, says Peng Wu, PhD, a TSRI associate professor and one of the study's lead authors. With this new approach, you can save time and money by starting with drugs and molecules you know are already active and asking whether a quick modification makes any of them any better.
Our results suggest we will be able take a drug and make it more potent, faster acting, and hopefully with better bioavailability, adds Nobel laureate K. Barry Sharpless, PhD, who co-led the study.
Sharpless, the TSRI W.M. Keck Professor of Chemistry, first conceived of click chemistry in the 1990s. Click chemistry is the term for simple molecular reactions that can each be carried out in one container, undisturbed by water, and generate just one stable product at high yield. Sharpless compares the method to decorating molecules like Christmas trees, adding a new functional ornament to one of a molecule's branches, which he calls clickable hubs.
Instead of pursuing leads, which is the traditional method, SuFEx click chemistry is about connecting promising drug candidates directly with targets, says Sharpless.
One of the latest click chemistry reactions developed by Sharpless' group was Sulfur (VI) Fluoride Exchange (SuFEx), which transforms any phenol chemical group into a fluorosulfate. Because fluorosulfates have some benefits over phenols including tighter binding to proteins, and less ability to be modified in the cell the SuFEx reaction offers a way to potentially improve phenol drugs.
However, the transformation typically relies on sulfuryl fluoride gas, which makes it hard to perform on many different molecules at the same time; each reaction must be carried out in its own flask.
In the new paper, Sharpless and Wu show that sulfuryl fluoride gas can be dissolved in an organic solvent to make a liquid form of the reagent needed for SuFEx. Now, suddenly, we can use this in high-throughput experiments, says Wu.
To test the reaction's utility in drug discovery, Sharpless, Wu and their colleagues put 39 existing cancer drugs containing phenols into plates, added the liquid version of sulfuryl fluoride to each well, and exposed cancer cells to both the original compounds and the resulting fluorosulfate versions. In three instances, the new fluorosulfate drug killed more cancer cells than the original version. When modified with SuFEx, the breast cancer drug Fulvestrant had a great effect on estrogen receptors in breast cancer cells, and the cancer drug Combretastatin A4 was 70 times more potent against colon cancer cells.
Upon further examination, the researchers discovered that the new molecules bound to their molecular targets better and were less apt to be metabolized by the cells.
We think our approach is generally applicable to drug modification outside of just cancer drugs, says Wu. The team is already using the new high-throughput SuFEx to modify drugs targeting the immune system's T cells, he adds.
In addition to Wu and Sharpless, authors of the study, SuFEx click chemistry enabled late-stage drug functionalization, are Zilei Liu, Jie Li, Suhua Li and Gencheng Li of The Scripps Research Institute.
This work was supported by the National Institutes of Health (grants R01 GM117145, R01 GM111938 and R01GM113046).
About The Scripps Research Institute
The Scripps Research Institute (TSRI) is one of the worlds largest independent, not-for-profit organizations focusing on research in the biomedical sciences. TSRI is internationally recognized for its contributions to science and health, including its role in laying the foundation for new treatments for cancer, rheumatoid arthritis, hemophilia, and other diseases. An institution that evolved from the Scripps Metabolic Clinic founded by philanthropist Ellen Browning Scripps in 1924, the institute now employs more than 2,500 people on its campuses in La Jolla, CA, and Jupiter, FL, where its renowned scientists including two Nobel laureates and 20 members of the National Academies of Science, Engineering or Medicine work toward their next discoveries. The institutes graduate program, which awards PhD degrees in biology and chemistry, ranks among the top ten of its kind in the nation. In October 2016, TSRI announced a strategic affiliation with the California Institute for Biomedical Research (Calibr), representing a renewed commitment to the discovery and development of new medicines to address unmet medical needs. For more information, see www.scripps.edu.
# # #
For information:
Office of Communications
Tel: 858-784-2666
Fax: 858-784-8118
press@scripps.edu
Most recent headlines
05/01/2027
Worlds first 802.15.4ab-UWB chip verified by Calterah and Rohde & Schwarz to be ...
01/06/2026
January 6 2026, 05:30 (PST) Dolby Sets the New Standard for Premium Entertainment at CES 2026
Throughout the week, Dolby brings to life the latest innovatio...
01/05/2026
January 5 2026, 18:30 (PST) NBCUniversal's Peacock to Be First Streamer to ...
01/04/2026
January 4 2026, 18:00 (PST) DOLBY AND DOUYIN EMPOWER THE NEXT GENERATON OF CREATORS WITH DOLBY VISION
Douyin Users Can Now Create And Share Videos With Stun...
03/02/2026
9905MPx Card features unprecedented level of density with four independent signa...
03/02/2026
Champaign, IL - November 15, 2021 - Cobalt Digital, announced today that three of its products have received 2021 NAB Show Product of the Year Awards. Cobalt, ...
03/02/2026
Cobalt is pleased to confirm that Log4j vulnerability does NOT affect ANY Cobalt products including the HPF-9000 frame.
Given the recent concerns regarding wi...
03/02/2026
Software-based embedding and de-embedding solution will be highlighted at NAB 20...
03/02/2026
Series developed to fill an industry need.
Champaign, IL April 13, 2022 Cobalt Digital will introduce a new series of BlueBox Group (BBG) EO/OE 12G mini...
03/02/2026
Company receives Best in Shows from Next TV and TVB Europe, and two Product of the Year awards from NAB
Champaign, IL - May 6, 2022 - Cobalt Digital Inc. head...
03/02/2026
IBC Preview - IBC Stand 10.B44Journalists: Click to visit Cobalt
Cobalt will al...
03/02/2026
IBC Stand 10.B44Journalists: Click to visit Cobalt
Dr. Ciro Noronha, CTO, tapped as a panelist and speaker by many - and then there's the party!
Amsterda...
03/02/2026
IBC Stand 10.B44Journalists: Click to visit Cobalt
Growth Drives Cobalt Digital to Promote Dr. Ciro Noronha to CTO, and Appoint Anthony Tan as Director of Sale...
03/02/2026
IBC Stand 10.B44Journalists: Click to visit Cobalt
Dr. Ciro Noronha, CTO, tappe...
03/02/2026
Manufacturer plans also include solutions that provide a path to the cloud and redundancy updatesCABSAT Stand S1-I42Journalists: Click to visit Cobalt
Dubai - ...
03/02/2026
Award-Winning Product Portfolio is Being Presented on Smart Video Group Stand, and Company's Berend Blokzijl is Scheduled to Share RIST Insight on Innovatio...
03/02/2026
NEW Location IBC Stand 10.F42 Same Hall, NEW StandJournalists: Click to visi...
03/02/2026
TVBEurope spoke with our very own Dr. Ciro Noronha about RIST and more.Reliable Internet Stream Transport (RIST) is growing in popularity for contribution and d...
03/02/2026
NEW Location IBC Stand 10.F42 Same Hall, NEW StandJournalists: Click to visi...
03/02/2026
NEW Location IBC Stand 10.F42 Same Hall, NEW StandJournalists: Click to visit CobaltCatch Cobalt's Blue WAVE of Innovation in a New LocationHighlights t...
03/02/2026
Cobalt Digital Scores Best of Show Awards at IBC 2023 from TVB Europe and TV Technology
Amsterdam, 2 October 2023 - Cobalt Digital has announced that it has w...
03/02/2026
NAB NY Booth: 1126Cobalt Digital to Present New PACIFIC Ultra-Low Latency 4K HEVC Encoder / Decoder Platform at NAB NY 2023Cobalt's NAB NY Plans Have Live P...
03/02/2026
Cobalt's Inter BEE Line-up Targets 4K 2110 Processing with INDIGO Option and Offers High-Density Routing Solutions with New WAVE SeriesNew Mini Converters a...
03/02/2026
Cobalt Digital's NAB 2024 Plans Include a Simplified Path to ATSC 3.0
Other Highlights include Enhanced IP Multiviewers, Expanded Router and Control Panel ...
03/02/2026
Featuring a Simplified Path to ATSC 3.0, Significant Support for ST 2110, and a New DANTE Embedder/De-Embedder with Frame SyncWAVE family of routers and expande...
03/02/2026
Company adds two 2024 NAB Show Product of the Year awards and one Best of Show from TV Tech to long list of accolades
Las Vegas, NV - April 24, 2024 - Cobalt ...
03/02/2026
Share
Copy link
Facebook
X
Linkedin
Bluesky
Email...
03/02/2026
BeckTV, a premier systems integrator for the broadcast media industry, and Ross Video, a global leader in live video production technology, have partnered once ...
03/02/2026
Audiovisual (AV) solutions provider MeyerPro has a long legacy of delivering exceptional live event productions. The Pacific Northwest-based outfit has served c...
03/02/2026
At the Vienna Interdisciplinary Symposium on Aortic Repair (VISAR), Riedel Communications' Managed Technology Division delivered a turnkey technical infrast...
03/02/2026
Limecraft today announced the release of Limecraft 2026.1, the first platform update of the year. Limecraft is an AI-powered production platform that enables co...
03/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
03/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
03/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
03/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
03/02/2026
Berklee Alumni Recognized at the 2026 Grammy Awards Winners took home trophies in nine categories, including Best Traditional Pop Vocal Album and Songwriter o...
02/02/2026
SBS's High-Flying Drama The Airport Chaplain casts Hugo Weaving alongside Th...
02/02/2026
The National Film and Video Foundation (NFVF), in partnership with the French Institute of South Africa (IFAS), is calling for applications from experienced Sou...
02/02/2026
Photo Credit: NASA. Space Launch System (SLS) rocket and Orion Spacecraft rollou...
02/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
02/02/2026
Hewshott, an industry leading global AV, IT, Theatre, and Acoustics consultancy firm has completed a global transition with current UK Managing Director, Daniel...
02/02/2026
Public Media Management (PMM) today announced LTN as the technology partner for PMM Cloud, its new managed, cloud-based master control solution purpose-built fo...
02/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
02/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
02/02/2026
Share Share by:
Copy link
Facebook
X
Linkedin
Bluesky
Email...
02/02/2026
XR, the leading platform powering advertising operations, today announced the acquisition of Telly Traffic, a UK-based business affairs specialist with nearly t...
02/02/2026
Big Blue Marble, a provider of broadcast-grade, cloud-native video solutions for broadcasters, service providers, and content owners, has become a launch partne...
02/02/2026
February 2 2026, 20:30 (PST) Mahindra launches XUV 7XO as Indias first vehicle ...
02/02/2026
Teaser available to view HERE
Damien Molony as Jim Bergerac
Ahead of the hotly anticipated return of Bergerac to U and U&DRAMA in the Spring, a teaser has bee...
02/02/2026
Rohde & Schwarz reshapes mid-range market with new 44 GHz FPL spectrum analyzer ...