XRS Project Summary — Progress and Upcoming Plans

[yinuowang0812]

🔵 In Progress/ 🟢 Completed/ 🔴 Pending

vs. Plasmodium falciparum:

#	Collaborator	Purpose	Compounds / Notes	Status
1.	David Fidock (Columbia)	Resistance generation	OSM-S-106 and Pro (no inactive enantiomer)	🔵 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	🟢 Data available
3.	TCGLS (MMV)	PRR	106-Pro	🟢 Data available
4.	TCGLS (MMV)	CaCo-2 permeability	106-Pro and 106-Phe	🔵 Shipped. Awaiting results
5.	Andrew Plater & Beatriz Baragana (Dundee)	Enzymatic pEC₅₀ inhibition	The 6 compounds: 106-Pro, 106-Pro-D, 106-ILeu, 106-Phe, 106-Lys, 106-Ser; And plus: 106, 106-Gly	🟢 Data available
6.	Jacquin Niles (MIT)	Testing against panel and cKD parasites		🔴 Follow-up made
7.	SSGCID	Diffraction (structural studies)	106-Pro	🟢 Data available
8.	Yoga & Amit Sharma (ICGEB Delhi)	Biochemical potency assays	106, 106-Pro, 106-Pro-D, 106-Phe, 106-Lys	🔵 Shipped. Awaiting results 🟢 Lys data available
9.	Conner Payne & Ralph Mazitschek (HSPH)	TR-FRET assay	106 and 106-Pro	🟢 Data available
10.	Amanda Lukens & Dyann Wirth (HSPH)	Cellular profiling against ProRS mutants	106, 106-Pro and 106-Pro-D	🟢 106 and 106-Pro data available. 🔵 Awaiting 106-Pro-D result
11.	Stanley Xie & Leann Tilley (UoM)	eIF2α phosphorylation	106-Pro and 106-Pro-D	🟢 Data available
12.	Rebecka (Barcelona)	Solubility testing	106, 106-Pro, 106-ala, 106-ILeu, 106-Leu, 106-Val, 106-Phe, 106-Asp	🟢 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	🟢 Data available
14.	London Metropolitan University	Elemental analysis	106-Pro (Bot, Salt and neutralised)	🔴 coordinating

---

Others:

#	Collaborator	Purpose	Compounds / Notes	Status
1.	David Sibley & Taher Uddin (WUSTL)	Toxoplasma gondii testing	106 + The 6 adducts	🟢 Data available, further collaboration
2.	Jim Janetka & Makedonka Mitva (WUSTL)	Nematode testing (hookworm, whipworm)	106 + The 6 adducts	🟢 Data available

---

XRSProject_Summary_May2025.docx