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Page 1
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity.
Mabanglo MF, Wilson B, Noureldin M, Kimani SW, Mamai A, Krausser C, González-Álvarez H, Srivastava S, Mohammed M, Hoffer L, Chan M, Avrumutsoae J, Li ASM, Hajian T, Tucker S, Green S, Szewczyk M, Barsyte-Lovejoy D, Santhakumar V, Ackloo S, Loppnau P, Li Y, Seitova A, Kiyota T, Wang JG, Privé GG, Kuntz DA, Patel B, Rathod V, Vala A, Rout B, Aman A, Poda G, Uehling D, Ramnauth J, Halabelian L, Marcellus R, Al-Awar R, Vedadi M. Mabanglo MF, et al. Among authors: al awar r. Nat Commun. 2024 Nov 23;15(1):10165. doi: 10.1038/s41467-024-54500-x. Nat Commun. 2024. PMID: 39580491 Free PMC article.
Molecular glues that inhibit deubiquitylase activity and inflammatory signalling.
Chandler F, Reddy PAN, Bhutda S, Ross RL, Datta A, Walden M, Walker K, Di Donato S, Cassel JA, Prakesch MA, Aman A, Datti A, Campbell LJ, Foglizzo M, Bell L, Stein DN, Ault JR, Al-Awar RS, Calabrese AN, Sicheri F, Del Galdo F, Salvino JM, Greenberg RA, Zeqiraj E. Chandler F, et al. Among authors: al awar rs. bioRxiv [Preprint]. 2024 Nov 15:2024.09.07.611787. doi: 10.1101/2024.09.07.611787. bioRxiv. 2024. PMID: 39282282 Free PMC article. Preprint.
High-throughput sensitive screening of small molecule modulators of microexon alternative splicing using dual Nano and Firefly luciferase reporters.
Best AJ, Braunschweig U, Wu M, Farhangmehr S, Pasculescu A, Lim JJ, Comsa LC, Jen M, Wang J, Datti A, Wrana JL, Cordes SP, Al-Awar R, Han H, Blencowe BJ. Best AJ, et al. Among authors: al awar r. Nat Commun. 2024 Jul 27;15(1):6328. doi: 10.1038/s41467-024-50399-6. Nat Commun. 2024. PMID: 39068192 Free PMC article.
Discovery of Two Highly Selective Structurally Orthogonal Chemical Probes for Activin Receptor-like Kinases 1 and 2.
Němec V, Remeš M, Beňovský P, Böck MC, Šranková E, Wong JF, Cros J, Williams E, Tse LH, Smil D, Ensan D, Isaac MB, Al-Awar R, Gomolková R, Ursachi VC, Fafílek B, Kahounová Z, Víchová R, Vacek O, Berger BT, Wells CI, Corona CR, Vasta JD, Robers MB, Krejci P, Souček K, Bullock AN, Knapp S, Paruch K. Němec V, et al. Among authors: al awar r. J Med Chem. 2024 Aug 8;67(15):12632-12659. doi: 10.1021/acs.jmedchem.4c00629. Epub 2024 Jul 18. J Med Chem. 2024. PMID: 39023313 Free PMC article.
Discovery of Conformationally Constrained ALK2 Inhibitors.
González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Sweeney MN, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R. González-Álvarez H, et al. Among authors: al awar r. J Med Chem. 2024 Mar 28;67(6):4707-4725. doi: 10.1021/acs.jmedchem.3c02308. Epub 2024 Mar 18. J Med Chem. 2024. PMID: 38498998 Free PMC article.
The Imipridone ONC213 Targets α-Ketoglutarate Dehydrogenase to Induce Mitochondrial Stress and Suppress Oxidative Phosphorylation in Acute Myeloid Leukemia.
Su Y, Carter JL, Li X, Fukuda Y, Gray A, Lynch J, Edwards H, Ma J, Schreiner P, Polin L, Kushner J, Dzinic SH, Buck SA, Pruett-Miller SM, Hege-Hurrish K, Robinson C, Qiao X, Liu S, Wu S, Wang G, Li J, Allen JE, Prabhu VV, Schimmer AD, Joshi D, Kalhor-Monfared S, Watson IDG, Marcellus R, Isaac MB, Al-Awar R, Taub JW, Lin H, Schuetz JD, Ge Y. Su Y, et al. Among authors: al awar r. Cancer Res. 2024 Apr 1;84(7):1084-1100. doi: 10.1158/0008-5472.CAN-23-2659. Cancer Res. 2024. PMID: 38266099 Free PMC article.
Targeting tumour-associated macrophages in hodgkin lymphoma using engineered extracellular matrix-mimicking cryogels.
Bahlmann LC, Xue C, Chin AA, Skirzynska A, Lu J, Thériault B, Uehling D, Yerofeyeva Y, Peters R, Liu K, Chen J, Martel AL, Yaffe M, Al-Awar R, Goswami RS, Ylanko J, Andrews DW, Kuruvilla J, Laister RC, Shoichet MS. Bahlmann LC, et al. Among authors: al awar r. Biomaterials. 2023 Jun;297:122121. doi: 10.1016/j.biomaterials.2023.122121. Epub 2023 Apr 9. Biomaterials. 2023. PMID: 37075613
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M. Li ASM, et al. Among authors: al awar r. J Med Chem. 2023 Apr 13;66(7):5041-5060. doi: 10.1021/acs.jmedchem.2c02132. Epub 2023 Mar 22. J Med Chem. 2023. PMID: 36948210 Free PMC article.
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Mamai A, Chau AM, Wilson BJ, Watson ID, Joseph BB, Subramanian PR, Morshed MM, Morin JA, Prakesch MA, Lu T, Connolly P, Kuntz DA, Pomroy NC, Poda G, Nguyen K, Marcellus R, Strathdee G, Theriault B, Subramaniam R, Mohammed M, Abibi A, Chan M, Winston J, Kiyota T, Undzys E, Aman A, Austin N, Du Jardin M, Packman K, Phillippar U, Attar R, Edwards J, O'Meara J, Uehling DE, Al-Awar R, Privé GG, Isaac MB. Mamai A, et al. Among authors: al awar r. ACS Med Chem Lett. 2023 Jan 12;14(2):199-210. doi: 10.1021/acsmedchemlett.2c00502. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793435 Free PMC article.
83 results