Dr. Rima Al-awar
Dr. Rima Al-awar
Contact
Dr. Rima Al-awar
Head, Therapeutic Innovation
and Drug Discovery

ralawar@oicr.on.ca

Ashif Kachra
Senior Executive Assistant, Drug Discovery
akachra@oicr.on.ca

Head, Therapeutic Innovation
and Drug Discovery

In 2008, Dr. Al-awar founded the OICR Drug Discovery Program. The Drug Discovery group, is comprised of dozens of researchers with deep industry expertise, focuses on translating the most promising ideas coming from Ontario’s academic community into therapeutic benefits for cancer patients by identifying hit and lead molecules and optimizing them as potential drug candidates.

Dr. Al-awar earned her PhD in synthetic organic chemistry from North Carolina State University and did a post-doctoral fellowship at the University of North Carolina at Chapel Hill prior to joining Eli Lilly and Company in 1995. During her time at Eli Lilly, she served as Head in Discovery Chemistry Research and Technologies, and later as Head in Route Selection in Chemical Product Research and Development.

Dr Al-awar is a full Professor in the Departments of Pharmacology & Toxicology as well as Chemistry, at the University of Toronto.

Experience & Education
  • 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.
Current Affiliations
  • 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
Select Publications
  • 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.

Research Areas
Treatment
Disease Areas
All
Opportunities to Collaborate

To inquire about our medicinal chemistry expertise and resources please visit: OICR’s Collaborative Research Resources directory.

Selected Patents
  • 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.
In the News
OICR-affiliated researchers awarded $6.6 million in funding from CIHR
OICR-affiliated researchers awarded $6.6 million in funding from CIHR
Mar 09, 2021
Two OICR innovations bolstered by investments from FACIT
Two OICR innovations bolstered by investments from FACIT
Apr 28, 2022
Previously overlooked proteins are a potential source for a new class of cancer killing drugs
Previously overlooked proteins are a potential source for a new class of cancer killing drugs
Aug 29, 2022