2020 Publications

Inhibition of USP7 activity selectively eliminates senescent cells in part via restoration of P53 activity.

He, Y.; Li, W.; Lv, D.; Zhang, X(in).; Zhang, X(uan).; Ortiz, Y. T.; Budamagunta, V.; Campisi, J.; Zheng, G.; Zhou, D.*
Aging Cell. 2020, 19, e13117. Doi: 10.1111/acel.13117


Synthesis and liver microsomal metabolic stability studies of a fluoro-substituted δ-tocotrienol derivative.

Liu, X.; Poddar, S.; Song, L.; Hendrickson, H.; Zhang, X.; Yuan, Y.; Zhou, D.; Zheng, G.*
ChemMedChem. 2020, 15, 506-516. Doi: 10.1002/cmdc.201900676


Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity.

Zhang, X.; Thummuri, D.; Liu, X.; Khan, S.; He, Y.; Zhang, P.; Hu, W.; Yuan, Y.; Zhou, D.;* Zheng, G.*
Eur. J. Med. Chem. 2020, 192, 112186. Doi: 10.1016/j.ejmech.2020.112186


Targeting anti-apoptotic BCL-2 family proteins for cancer treatment.

Zhang, X.; Liu, X.; Zhou, D.; Zheng, G.*
Future Med. Chem. 2020, 12, 563-565. Doi: 10.4155/fmc-2020-0004


Using proteolysis targeting chimera technology to overcome ABT263 on-target platelet toxicity and improve its senolytic activity.

He, Y.; Zhang, X(uan).; Chang, J.; Kim, H-N.; Zhang, P.; Wang, Y.; Khan, S.; Liu, X.; Zhang, X(in).; Lv, D.; Li, W.; Thummuri, D.; Yuan, Y.; Elisseeff, J. H.; Campisi, J.; Almeida, M.; Zheng, G.;* Zhou, D.*
Nat. Commun. 2020, 11, 1996. Doi: 10.1038/s41467-020-15838-0


Deuteration of the farnesyl terminal methyl groups of δ-tocotrienol and its effects on the metabolic stability and ability of inducing G-CSF production.

Liu, X.; Gao, Z.; Fu, Q.; Song, L.; Zhang, P.; Zhang, X.; Hendrickson, H.; Crooks, P. A.; Zhou, D.; Zheng, G.*
Bioorg. Med. Chem. 2020, 28, 115498. Doi: 10.1016/j.bmc.2020.115498


Assays and technologies for developing proteolysis targeting chimera degraders.

Liu, X.; Zhang, X.; Lv, D.; Yuan, Y.; Zheng, G.; Zhou, D.*
Future Med. Chem. 2020, 12, 1155-1179. Doi: 10.4155/fmc-2020-0073


Discovery of IAP-based BCL-XL PROTACs as potent degraders across multiple cancer cell lines.

Zhang, X.; He, Y.; Zhang, P.; Budamagunta, V.; Lv, D.; Thummuri, D.; Yang, Y.; Yuan, Y.; Zhou, D.;* Zheng, G.*
Eur. J. Med. Chem. 2020, 199, 112397. Doi: 10.1016/j.ejmech.2020.112397


Proteolysis targeting chimeras (PROTACs) as emerging anticancer therapeutics.

Khan, S.; He, Y.; Zhang, X.; Yuan, Y.; Pu, S.; Kong, Q.; Zheng, G.; Zhou, D.*
Oncogene. 2020, 39, 4909-4924. Doi: 10.1038/s41388-020-1336-y


Proteolysis targeting chimeras are emerging therapeutics for hematologic malignancies.

He, Y.; Khan, S.; Huo, Z.; Lv, D.; Zhang, X.; Liu, X.; Yuan, Y.; Hromas, R.; Xu, M.; Zheng, G.; Zhou, D.*
JHematol. Oncol. 2020, 13, 103. Doi: 10.1186/s13045-020-00924-z


DT2216 is highly active against T-cell lymphomas by degrading Bcl-xL without causing thrombocytopenia.

He, Y.; Koch, R.; Budamagunta, V.; Zhang, P.; Zhang, X(uan).; Khan, S.; Thummuri, D.; Ortiz, Y. T.; Zhang, X(in).; Lv, D.; Wiegand, J. S.; Li, W.; Palmer, A. C.; Zheng, G.; Weistock, D. M.;* Zhou, D.*
J. Hematol. Oncol. 2020, 13, 95. Doi: 10.1186/s13045-020-00928-9


Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs.

Xiao, Y.; Wang, J.; Zhao, L.; Chen, X.; Zheng, G.; Zhang, X.;* Liao, D.*
Chem. Comm. 2020, 56, 9866-9869. Doi: 10.1039/d0cc03243c


PROTAC is an effective approach to address the platelet toxicity associated with BCL-XL inhibitors.

Zhang, P.; Zhang, X.; Liu, X.; Khan, S.; Zhou, D.; Zheng, G.*
Explor. Target Antitumor Ther. 2020, 1, 259-272. Doi: 10.37349/etat.2020.00017


Facile semisynthesis and evaluation of garcinoic acid and its analogs for the inhibition of human DNA polymerase β.

Gujarathi, S.; Khan, M. Z.; Liu, X.; Eoff, R. L.; Zheng, G.*
Molecules. 2020, 25, 5847. Doi: 10.3390/molecules25245847