Targeted protein degradation: expanding the toolbox.
Schapira, M., Calabrese, M., Bullock, A., & Crews, C. (2019). Targeted protein degradation: expanding the toolbox. Nature Reviews Drug Discovery, 18(12), 949-963.
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Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation.
Yu, X., Plotnikova, O., Bonin, P. D., Subashi, T. A., McLellan, T. J., Dumlao, D., … Han, S. (2019). Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation. eLife, 8, e48120.
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Taylor, A., Swewczyk, M., Kennedy, S., Trush, V., Wu, H., Zeng, H., ... Owen, D. (2019). Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase. Journal Of Medicinal Chemistry, 62(17), 7669-7683.
Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism.
Fox, N. G., Yu, X., Feng, X., Bailey, H. J., Martelli, A., Nabhan, J. F., … Han, S. (2019). Structure of the human frataxin-bound iron-sulfur cluster assembly complex provides insight into its activation mechanism. Nature communications, 10(1), 2210.
The promise and peril of chemical probes.
Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., … Zuercher, W. J. (2015). The promise and peril of chemical probes. Nature chemical biology, 11(8), 536–541.
Donated Chemical Probes for Open Science
Müller, S., Ackloo, S., Arrowsmith, C. H., Bauser, M., Baryza, J. L., Blagg, J., … Mueller-Fahrnow, A. (2018). Donated chemical probes for open science. eLife, 7, e34311.
Progress towards a public chemogenomic set for protein kinases and a call for contributions
Drewry, D. H., Wells, C. I., Andrews, D. M., Angell, R., Al-Ali, H., Axtman, A. D., … Willson, T. M. (2017). Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS ONE, 12(8), e0181585.
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain
Denny, R., Flick, A., Coe, J., Langille, J., Basak, A., Liu, S., ... Chekler, E. L. P. (2017). Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain. Journal Of Medicinal Chemistry, 60(13), 5349-5363.
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies
Igoe, N., Bayle, E. D., Fedorov, O., Tallant, C., Savitsky, P., Rogers, C., … Fish, P. V. (2017). Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. Journal of Medicinal Chemistry, 60(2), 668-680.
Advances and challenges in understanding histone demethylase biology
Nowak, R., Tumber, A., Johansson, C., Che, K., Brennan, P., Owen, D., Oppermann, U. (2016). Advances and challenges in understanding histone demethylase biology. Current Opinion In Chemical Biology, 33, 151-159.