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9 papers
Recent·Most cited
P. D. Okoro, R. Jaberi, S. Blackburn, D. Patel, N. Halasah, J. Mapa, M. Shih, R. Botzbach, J. Tan, V. I. Vullev, H. Liu, V. Santhakumar, Iman Noshadi
This paper develops a conductive hydrogel that reduces glial and vascular damage in traumatic brain injury models.
bioRxiv · Nov 9, 2026 · PreprintNeuroscience
C. H. Arrowsmith, S. Ackloo, F. Li, M. Szewczyk, A. Seitova, P. Loppnau, H. Zeng, S. Ahmad, S. Beldar, A. Bolotokova, I. Chau, S. Dehghani-Tafti, A. Dong, P. Ghiabi, E. Gibson, , Arnautova
The paper develops a resource for discovering ligands for WDR proteins using experimental and computational methods, leading to the identification of drug-like ligands for 9 out of 20 targets.
bioRxiv · Mar 3, 2024Biochemistry
A. K. Yazdi, S. Perveen, X. Song, A. Dong, M. Szewczyk, M. Calabrese, A. Casimiro-Garcia, C. Subramanyam, M. S. Dowling, E. Ficici, J. Lee, J. I. Montgomery, T. N. O'Connell, G. J. Skrzypek, T. P. Tran, , D. R. Owen
The paper develops chemical tools and probes for the Gid4 subunit of the human CTLH E3 ligase complex, achieving sub-100 nM binding affinity for further study.
bioRxiv · Nov 13, 2023Biophysics
G. L. Righetto, Y. Yin, V. Vu, D. Duda, M. Szewczyk, H. Zeng, Y. Li, P. Loppnau, T. Mei, Y.-Y. Li, A. Seitova, J.-F. Brazeau, D. Barsyte-Lovejoy, V. Santhakumar, C. Chaudhry, L. Halabelian
This study characterizes DCAF12 interactions with MAGEA3 and CCT5 degrons using biophysical assays and cryo-EM, revealing key residues for degron recognition and informing PROTAC design.
bioRxiv · Aug 15, 2023 · PreprintBiochemistry
S. Kimani, S. Perveen, M. Szewczyk, H. Zeng, A. Dong, F. Li, P. Ghiabi, Y. Li, I. Chau, C. Arrowsmith, D. Barsyte-Lovejoy, V. Santhakumar, M. Vedadi, L. Halabelian
The paper investigates how a small-molecule inhibitor binds to and inactivates Cbl-b, revealing a structural mechanism that locks the protein in an inactive conformation.
bioRxiv · May 5, 2023 · PreprintImmunology
R. J. Harding, I. Franzoni, M. K. Mann, M. Szewczyk, B. Mirabi, D. D. Owens, S. Ackloo, A. Scheremetjew, K. A. Juarez-Ornelas, R. Sanichar, R. J. Baker, C. Dank, P. J. Brown, D. Barsyte-Lovejoy, V. Santhakumar, , C. H. Arrowsmith
The paper identifies and characterizes a chemical probe, SGC-UBD253, that targets the HDAC6 UBD with selectivity, and a less active derivative as a negative control.
bioRxiv · Feb 21, 2023Pharmacology & Toxicology
M. Sutherland, A. Li, A. Kaghad, D. Panagopoulos, F. Li, M. Szewczyk, D. Smil, C. Scholten, L. Bouche, T. Stellfeld, C. Arrowsmith, D. Barsyte, M. Vedadi, I. V. Hartung, H. Steuber, , V. Santhakumar
This study designs and synthesizes a new class of selective PRMT4 inhibitors with improved selectivity over other PRMT family members.
bioRxiv · Nov 17, 2020Pharmacology & Toxicology
P. Mader, R. Mendoza-Sanchez, A. Iqbal, A. Dong, E. Dobrovetsky, V. Corless, S. Liew, S. Houliston, R. Ferreira De Freitas, D. Smil, C. Dela Sena, S. Kennedy, D. Diaz, H. Wu, L. Dombrovski, , C. Arrowsmith
The paper identifies small molecule fragments that bind to the tudor domain of SETDB1 and describes their binding modes and biophysical properties.
Bioorganic & Medicinal Chemistry · Sep 1, 2019Peer-reviewedPharmacology & Toxicology
R. Ferreira de Freitas, R. Harding, I. Franzoni, M. Ravichandran, M. K. Mann, H. Ouyang, M. Lautens, V. Santhakumar, C. Arrowsmith, M. Schapira
The paper identifies HDAC6 ZnF-UBD inhibitors and describes their structure-activity relationships, revealing key binding features and potential for further optimization.
bioRxiv · Feb 20, 2018Biophysics