and Drug Discovery
Dr. Al-awar, Head of Therapeutic Innovation and Drug Discovery, discovers and develops new drugs in collaboration with academic and industry partners. Since joining OICR in 2008, Dr. Rima Al-awar’s focus has been to build a drug discovery program that can efficiently help translate cancer-related academic discoveries from Ontario’s scientific community into novel oncology therapies that will benefit cancer patients.
She has endeavoured to build a team that complements the requirements of Ontario’s academic community and the team is now comprised of researchers whose collective expertise spans the entire drug discovery process from target identification and validation to clinical candidate selection. The group has extensive experience within pharma and biotech environments and combines the biology, ADME/PK, analytical, medicinal and computational chemistry expertise with the state of the art infrastructure necessary to successfully advance drug discovery projects.
The major goal of the Drug Discovery group is to help translate the most promising ideas coming from Ontario’s academic community into therapeutic benefits to cancer patients by identifying hits and lead molecules and optimizing them to potential drug candidates.
- Head, Route Selection Group, Chemical Process Research and Development at Eli Lilly and Company, Indianapolis, IN, U.S.
- Head, Discovery Chemistry Research and Technologies at Eli Lilly and Company, Indianapolis, IN, U.S.
- Post-doctoral Fellow, University of North Carolina at Chapel Hill, NC, U.S.
- PhD, North Carolina State University, Raleigh, NC, U.S.
- Head, Therapeutic Innovation and Drug Discovery, OICR
- Professor, University of Toronto, Department of Chemistry
- Professor, University of Toronto, Department of Pharmacology and Toxicology
- Associate Graduate Faculty Member, University of Toronto, Department of Pharmacology and Toxicology
- Ackloo S, Al-awar R, Amaro R, Arrowsmith C, Azevedo H, Batey R, Bengio Y, Betz U, Bologa C, Chodera J, Cornell W, Dunham I, Ecker G, Edfeldt K, Edwards A, Gilson M, Gordijo C, Hessler G, Hillisch A, Hogner A, Irwin J, Johanna Jansen J, Kuhn D, Leach A, Lee A, Lessel U, Morgan M, Moult J, Muegge I, Oprea T, Perry B, Riley P, Rousseaux S, Saikatendu K, Santhakumar V, Schapira M, Scholten C, Todd M, Vedadi M, Volkamer A, Willson T. “CACHE:A public-private partnership benchmarking initiative to enable the development of computational methods for hit-finding” Nat Rev Chem 6, 287–295 (2022).
- Saraon P, Snider J, Schormann W, Rai A, Radulovich N, Sánchez-Osuna M, Coulombe-Huntington J, Huard C, Mohammed M, Lima-Fernandes E, Thériault B, Halabelian L, Chan M, Joshi D, Drecun L, Yao Z, Pathmanathan S, Wong V, Lyakisheva A, Aboualizadeh F, Niu L, Li F, Kiyota T, Subramanian R, Joseph B, Aman A, Prakesch M, Isaac M, Mamai A, Poda G, Vedadi M, Marcellus R, Uehling D, Leighl N, Sacher A, Samaržija M, Jakopović M, Arrowsmith C, Tyers M, Tsao MS, Andrews D, Al-Awar R, Stagljar I. “Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation in Lung Cancer Cells.” J Mol Biol. 2021 Nov 19;433(23):167294.
- Barghout SH, Aman A, Nouri K, Blatman Z, Arevalo K, Thomas GE, MacLean N, Hurren R, Ketela T, Saini M, Abohawya M, Kiyota T, Al-awar R, Schimmer AD. A genome-wide CRISPR/Cas9 screen in acute myeloid leukemia cells identifies regulators of TAK-243 sensitivity. JCI Insight. 2021 Mar 8;6(5):e141518.
- Smil D, Wong JF, Williams E, Adamson R, Howarth A, McLeod D, Mamai A, Kim S, Wilson B, Kiyota T, Aman A, Owen J, Poda G, Horiuchi K, Kuznetsova E, Ma H, Hamblin JN, Cramp S, Roberts O, Edwards A, Uehling D, Al-awar R, Bullock A, O’Meara Jeff, Isaac M. “Leveraging an Open Science Drug Discovery Model to Develop CNS Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.” J. Med. Chem. 2020 63 (17), 10061-10085.
- Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D. “Pharmacological Inhibition Of PRMT7 Links Arginine Monomethylation To The Cellular Stress Response.” Nat Commun 14 May 2020 11:2396.
- Ensan D, Smil D, Zepeda-Velázquez CA, Panagopoulos D, Wong JF, Williams EP, Adamson R, Bullock AN, Kiyota T, Aman A, Roberts OG, Edwards AM, O’Meara JA, Isaac MB, Al-awar R. “Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.” J. Med. Chem. 2020, 63, 9, 4978–4996.
- Saraon P, Snider J, Kalaidzidis Y, Wybenga-Groot LE, Weiss K, Rai A, Radulovich N, Drecun L, Vučković N, Vučetić A, Wong V, Thériault B, Pham NA, Park JH, Datti A, Wang J, Pathmanathan S, Aboualizadeh F, Lyakisheva A, Yao Z, Wang Y, Joseph B, Aman A, Moran MF, Prakesch M, Poda G, Marcellus R, Uehling D, Samaržija M, Jakopović M, Tsao MS, Shepherd FA, Sacher A, Leighl N, Akhmanova A, Al-awar R, Zerial M, Stagljar I. “A Drug Discovery Platform To Identify Compounds That Inhibit EGFR Triple Mutants.” Nat. Chem. Biol. 16, 577–586 (2020).
- Seneviratne AK, Xu M, Henao JJA, Fajardo VA, Hao Z, Voisin V, Xu GW, Hurren R, Kim S, MacLean N, Wang X, Gronda M, Jeyaraju D, Jitkova Y, Ketela T, Mullokandov M, Sharon D, Thomas G, Chouinard-Watkins R, Hawley JR, Schafer C, Yau HL, Khuchua Z, Aman A, Al-Awar R, Gross A, Claypool SM, Bazinet RP, Lupien M, Chan S, De Carvalho DD, Minden MD, Bader GD, Stark KD, LeBlanc P, Schimmer AD. “The Mitochondrial Transacylase, Tafazzin, Regulates for AML Stemness by Modulating Intracellular Levels of Phospholipids.” Cell Stem Cell 2019 Apr 4;24(4):621-636.
- Christott T, Bennett J, Coxon C, Monteiro O, Giroud C, Beke V, Felce SL, Gamble V, Gileadi C, Poda G, Al-awar R, Farnie G, Fedorov O. “Discovery Of A Selective Inhibitor For The YEATS Domains Of ENL/AF9.” SLAS Discov. 2019 Feb;24(2):133-141.
- Medrano M, Communal L, Brown KR, Iwanicki M, Normand J, Paterson J, Sircoulomb F, Krzyzanowski P, Novak M, Doodnauth SA, Suarez Saiz F, Cullis J, Al-awar R, Neel BG, McPherson J, Drapkin R, Ailles L, Mes-Massons AM, Rottapel R. “Interrogation of Functional Cell-Surface Markers Identifies CD151 Dependency in High-Grade Serous Ovarian Cancer.” Cell Reports. 2017 March 7; 18(10): 2343-58.
- Logie J, Ganesh AN, Aman AM, Al-awar RS, Shoichet MS. “Preclinical Evaluation of Taxane-binding Peptide-modified Polymeric Micelles Loaded with Docetaxel in an Orthotopic Breast Cancer Mouse Model.” Biomaterials. 123:39-47. April 2017.
- Getlik M, Smil D, Zepeda-Velázquez C, Bolshan Y, Poda G, Wu H, Dong A, Kuznetsova E, Marcellus R, Senisterra G, Dombrovski L, Hajian T, Kiyota T, Schapira M, Arrowsmith CH, Brown PJ, Vedadi M, Al-awar R. “Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1). J. Med. Chem. 2016, 59(6): 2478-96.
- Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G,Schönegger A, Bilban M, Bock C, Brown PJ, Zuber J, Bennet KL, Al-awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G. “Pharmacological Targeting of the WDR5-MLL Interaction in C/EBPα N-terminal Leukemia.” Nat Chem Biol, 2015, 11(8): 571-8.
See Dr. Al-awar’s recent publications on PubMed.
To inquire about our medicinal chemistry expertise and resources please visit: OICR’s Collaborative Research Resources directory.
- Al-Awar, Rima; Isaac, Methvin; Chau, Anh My; Mamai, Ahmed; Watson, Iain; Poda, Gennady; Subramanian, Pandiaraju; Wilson, Brian; Uehling, David; Prakesch, Michael. “Preparation of substituted pyrrolopyrimidinylacetamides as inhibitors of the BCL6 BTB domain protein-protein interaction and uses thereof.” PCT Int. Appl. (2019), WO 2019153080 A1 20190815
- Al-Awar, Rima; Isaac, Methvin; Chau, Anh My; Mamai, Ahmed; Watson, Iain; Poda, Gennady; Subramanian, Pandiaraju; Wilson, Brian; Uehling, David. Preparation of tricyclic as inhibitors of interaction between the BCL6 BTB with its SMRT, NcoR and BCOR corepressors and/or as BCL6 degraders. United States. WO 2019119145 A1. 2019/06/27.
- Al-Awar, Rima; Mamai, Ahmed; Zhang, Andrew. “Preparation of piperazinylaryl dihydropyridine carboxamides and uses thereof” PCT Int. Appl. WO 2019119141 A1 2019/06/13.
- Al-Awar, Rima; Isaac, Methvin; Joseph, Babu; Liu, Yong; Mamai, Ahmed; Poda, Gennady; Subramanian, Pandiaraju; Uehling, David; Wilson, Brian; Zepeda-Velazquez, Carlos Armando. “Preparation of piperazinylaryl dihydropyridine carboxamides and related compounds as inhibitors of WDR5 protein-protein binding useful in treatment of WDR5-mediated disorders” PCT Int. Appl. (2019) WO 2019046944 A1. 2019/03/14.