Degrasyn-like symmetrical compounds: possible therapeutic agents for multiple myeloma (MM-I).
A series of degrasyn-like symmetrical compounds have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against these tumor cells in comparison to degrasyn and inhibited Usp9x activity in vitro and in intact cells. These observations suggest that this new class of compounds holds promise as cancer therapeutic agents.
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Zhenghong
Z
Peng
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
David S
DS
Maxwell
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Duoli
D
Sun
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Basvoju A
BA
Bhanu Prasad
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Paul T
PT
Schuber
Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Ashutosh
A
Pal
Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Yunming
Y
Ying
Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Dongmei
D
Han
Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Liwei
L
Gao
Department of Experimental Diagnostic Imaging, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States.
Shimei
S
Wang
Unit of Cellular Signaling, Department of Biological Chemistry, The Hebrew University of Jerusalem, Jerusalem, Israel.
Alexander
A
Levitzki
Department of Internal Medicine/Division of Hematology/Oncology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
Vaibhav
V
Kapuria
Department of Internal Medicine/Division of Hematology/Oncology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
Moshe
M
Talpaz
Department of Pharmacology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
Matthew
M
Young
Department of Medicinal Chemistry, University of Michigan College of Pharmacy, Ann Arbor, MI 48109, United States.
Hollis D
HD
Showalter
Department of Internal Medicine/Division of Hematology/Oncology, University of Michigan School of Medicine, Comprehensive Cancer Center, United States.
Nicholas J
NJ
Donato
Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, United States. Electronic address: wbornmann@mdanderson.org.
William G
WG
Bornmann
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003487:Cyanoacrylates; D019281:Dimerization; D006801:Humans; D008958:Models, Molecular; D009101:Multiple Myeloma / Q000188:drug therapy; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D043222:Ubiquitin Thiolesterase / Q000037:antagonists & inhibitors / Q000378:metabolism
D000970:Antineoplastic Agents; D003487:Cyanoacrylates; D009570:Nitriles; D011725:Pyridines; C506234:USP9X protein, human; C519751:degrasyn; D043222:Ubiquitin Thiolesterase
Degrasyn; Inhibitors; Jak2/Stat3; Multiple myeloma; Small molecules; Synthesis