Simulation- and AI-directed optimization of 4,6-substituted 1,3,5-triazin-2(1H)-ones as inhibitors of human DNA topoisomerase IIα. [PDF]
Herlah B +5 more
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DNA topoisomerase II inhibition potentiates osimertinib's therapeutic efficacy in EGFR-mutant non-small cell lung cancer models. [PDF]
Chen Z +8 more
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Targeted repression of topA by CRISPRi reveals a critical function for balanced DNA topoisomerase I activity in the Chlamydia trachomatis developmental cycle. [PDF]
Shen L, Gao L, Swoboda AR, Ouellette SP.
europepmc +1 more source
Raludotatug Deruxtecan, a CDH6-Targeting Antibody-Drug Conjugate with a DNA Topoisomerase I Inhibitor DXd, Is Efficacious in Human Ovarian and Kidney Cancer Models. [PDF]
Suzuki H +13 more
europepmc +1 more source
DB-1314, a novel DLL3-targeting ADC with DNA topoisomerase I inhibitor, exhibits promising safety profile and therapeutic efficacy in preclinical small cell lung cancer models. [PDF]
Lin S +6 more
europepmc +1 more source
DNA topoisomerase I acts as supercoiling sensor for transcription elongation inE. coli
Vidmar V +9 more
europepmc +1 more source
DB-1310, an ADC comprised of a novel anti-HER3 antibody conjugated to a DNA topoisomerase I inhibitor, is highly effective for the treatment of HER3-positive solid tumors. [PDF]
Li X +8 more
europepmc +1 more source
Correction to 'Using energy to go downhill-a genoprotective role for ATPase activity in DNA topoisomerase II'. [PDF]
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DNA topoisomerases are enzymes that control the topological state of DNA in all cells; they have central roles in DNA replication and transcription. They are classified into two types, I and II, depending on whether they catalyze reactions involving the breakage of one or both strands of DNA.
Katherine, Evans-Roberts +1 more
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In the past year, the atomic structures of three fragments of type I DNA topoisomerases were elucidated. Together with the atomic structure of a fragment of bacterial gyrase, this wealth of structural information is helping to further our understanding of the mechanism of action of topoisomerases.
A, Sharma, A, Mondragón
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