XRS Project Summary β Progress and Upcoming PlansΒ #39
Description
π΅ In Progress/ π’ Completed/ π΄ Pending
vs. Plasmodium falciparum:
| # | Collaborator | Purpose | Compounds / Notes | Status |
|---|---|---|---|---|
| 1. | David Fidock (Columbia) | Resistance generation | OSM-S-106 and Pro (no inactive enantiomer) | π΅ Processing results |
| 2. | TCGLS (MMV) | Pf3D7, Dd2, HepG2, ADME Tier 1 | The 6 compounds: 106-Pro, 106-Pro-D, 106-ILeu, 106-Phe, 106-Lys, 106-Ser | π’ Data available |
| 3. | TCGLS (MMV) | PRR | 106-Pro | π’ Data available |
| 4. | TCGLS (MMV) | CaCo-2 permeability | 106-Pro and 106-Phe | π΅ Shipped. Awaiting results |
| 5. | Andrew Plater & Beatriz Baragana (Dundee) | Enzymatic pECβ β inhibition | The 6 compounds: 106-Pro, 106-Pro-D, 106-ILeu, 106-Phe, 106-Lys, 106-Ser; And plus: 106, 106-Gly | π’ Data available |
| 6. | Jacquin Niles (MIT) | Testing against panel and cKD parasites | π΄ Follow-up made | |
| 7. | SSGCID | Diffraction (structural studies) | 106-Pro | π’ Data available |
| 8. | Yoga & Amit Sharma (ICGEB Delhi) | Biochemical potency assays | 106, 106-Pro, 106-Pro-D, 106-Phe, 106-Lys | π΅ Shipped. Awaiting results π’ Lys data available |
| 9. | Conner Payne & Ralph Mazitschek (HSPH) | TR-FRET assay | 106 and 106-Pro | π’ Data available |
| 10. | Amanda Lukens & Dyann Wirth (HSPH) | Cellular profiling against ProRS mutants | 106, 106-Pro and 106-Pro-D | π’ 106 and 106-Pro data available. π΅ Awaiting 106-Pro-D result |
| 11. | Stanley Xie & Leann Tilley (UoM) | eIF2Ξ± phosphorylation | 106-Pro and 106-Pro-D | π’ Data available |
| 12. | Rebecka (Barcelona) | Solubility testing | 106, 106-Pro, 106-ala, 106-ILeu, 106-Leu, 106-Val, 106-Phe, 106-Asp | π’ Data available; contact Rebecka |
| 13. | UKHSA | Biochemical potency assays against M. avium | 106, 106-Pro, 106-ala, 106-ILeu, 106-Leu, 106-Val, 106-Phe, 106-Asp | π’ Data available |
| 14. | London Metropolitan University | Elemental analysis | 106-Pro (Bot, Salt and neutralised) | π΄ coordinating |
Others:
| # | Collaborator | Purpose | Compounds / Notes | Status |
|---|---|---|---|---|
| 1. | David Sibley & Taher Uddin (WUSTL) | Toxoplasma gondii testing | 106 + The 6 adducts | π’ Data available, further collaboration |
| 2. | Jim Janetka & Makedonka Mitva (WUSTL) | Nematode testing (hookworm, whipworm) | 106 + The 6 adducts | π’ Data available |