Shapeshifting cyclic peptides as single molecule polypharmacological drugs
Active Project Grant Awarded Last action
- Award ID
- R21GM154148
- Recipient
-
The Regents Of The University Of Colorado UEI SPVKK1RC2MZ3
- Awarding agency
-
National Institute of General Medical Sciences
National Institutes of Health, Department of Health and Human Services
- Obligated
- $373,876
Award facts
- Assistance listing
- 93.859 Biomedical Research and Research Training
- Completion date 74% complete
- Originally
- Funding agency
- Assistant Secretary for Financial Resources Department of Health and Human Services
- Place of performance
- Boulder, CO 80309, USA
Award details come from USAspending.gov.
Description
- Abstract
- For many years, scientists have been trying to find new therapeutic drugs. However, small molecules are still imperfect tools for influencing human physiology. The chemical space that our known drugs occupy is extremely small, representing a tiny sliver of the estimated 10^63 possible drug-like molecules. What's more, the targets of these drugs make up just about 3.5% of the roughly 20,000 proteins in the human proteome. This means almost 97% of the proteome is still untouched for drug intervention. These two factors suggest there's immense potential for discovering novel chemical structures to combat disease. However, systematically exploring such enormous chemical spaces is physically unachievable. To synthesize even milligram scale representations of this chemical space would result in a mass surpassing that of the known universe. This practical obstacle partly explains why only a small portion of the proteins in the proteome have been pharmacologically targeted. To overcome this diversity enumeration hurdle, we aim to introduce a completely new class of molecules capable of spontaneously "shape shifting" at physiological temperature. This unique ability will allow them to assume a wide array of rapidly interchanging structural isomers, essentially behaving like many molecules in one. We plan to demonstrate this technology through the development of synthetic bullvalene amino acids that can be seamlessly incorporated into existing methodologies for combinatorial solid phase peptide synthesis to create shape shifting cyclic peptides (SSCP). Our ultimate goal is to create a dynamic and adaptable library that far outpaces any known library in terms of diversity. We aim to utilize this technology to identify single molecular entities that display multi- target pharmacological properties.
Transactions
| Action | Obligated | Date |
|---|---|---|
| Amendment | $0 | |
| Amendment | $160,313 | |
| Original award | $213,563 |
Subawards
| Subrecipient | Amount | Awarded |
|---|---|---|
| The University Of Adelaide | $66,710 |
Quick answers
Who received award R21GM154148?
R21GM154148 was awarded to The Regents Of The University Of Colorado by National Institute of General Medical Sciences (National Institutes of Health) on August 28, 2024.
How much is award R21GM154148 worth?
$373,876 has been obligated on R21GM154148.
Which agency awarded R21GM154148?
National Institute of General Medical Sciences (National Institutes of Health) awarded R21GM154148, with funding from Assistant Secretary for Financial Resources (Department of Health and Human Services).
On GovTribe
See this award's full record
- Every transaction and subaward
- The recipient's other awards and teaming partners
- Similar grant awards
- Ask GovTribe AI about this award