Výsledky vyhledávání - "John A. Gilleran"

Benzothiazolyl and Benzoxazolyl Hydrazones Function as Zinc Metallochaperones to Reactivate Mutant p53

Autor: John A. Gilleran, S. David Kimball, Jacques Roberge, Alan J. Blayney, Stewart N. Loh, Adam R. Blanden, David Augeri, Darren R. Carpizo, Anthony F. Bencivenga, Xin Yu, Bing Na

Publikováno v: J Med Chem

We identified a set of thiosemicarbazone (TSC) metal ion chelators that reactivate specific zinc-deficient p53 mutants using a mechanism called zinc metallochaperones (ZMCs) that restore zinc binding by shuttling zinc into cells. We defined biophysic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37960bf2b8c996bc4b1a6bffd407a5ac
https://doi.org/10.1021/acs.jmedchem.0c01360

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Identification of Dihydromyricetin and Metabolites in Serum and Brain Associated with Acute Anti-Ethanol Intoxicating Effects in Mice

Autor: Qingli Wu, John A. Gilleran, Harna Patel, Nicholas T. Bello, Lihong Hao, Eileen Carry, James E. Simon, Bo Yuan, Jacques Roberge, Daryl L. Davies, Dushyant Kshatriya, Elizabeth R. Park, Joshua Silva

Publikováno v: International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 22, Iss 7460, p 7460 (2021)
Volume 22
Issue 14

Dihydromyricetin is a natural bioactive flavonoid with unique GABAA receptor activity with a putative mechanism of action to reduce the intoxication effects of ethanol. Although dihydromyricetin’s poor oral bioavailability limits clinical utility,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae38dac29769dc357e7a43417b363d5f
http://europepmc.org/articles/PMC8307506

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Combinatorial Therapy of Zinc Metallochaperones with Mutant p53 Reactivation and Diminished Copper Binding

Autor: Stewart N. Loh, Adam R. Blanden, Yue Liu, S. David Kimball, Bing Na, Tracy Withers, Anthony F. Bencivenga, Alan J. Blayney, Saif Zaman, Xin Yu, Darren R. Carpizo, David A. Boothman, John A. Gilleran

Publikováno v: Molecular Cancer Therapeutics. 18:1355-1365

Chemotherapy and radiation are more effective in wild-type (WT) p53 tumors due to p53 activation. This is one rationale for developing drugs that reactivate mutant p53 to synergize with chemotherapy and radiation. Zinc metallochaperones (ZMC) are a n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8918faaad9539fd65e5cb4d867c088d8
https://doi.org/10.1158/1535-7163.mct-18-1080

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Abstract P6-20-05: Therapeutic targeting of BRCA1 and TP53 mutant breast cancer through mutant p53 reactivation

Autor: John A. Gilleran, Shridar Ganesan, Darren R. Carpizo, Bing Xia, Ming Yao, Dirk F. Moore, D Kimball, T Wither, Xin Yu, Chunxia Chen, B Na, Yong Lin, Tzeh Keong Foo

Publikováno v: Cancer Research. 79:P6-20

Triple negative breast cancer (TNBC) is an aggressive subset for which novel therapeutic approaches are needed. A significant proportion of TNBC patients harbor either germline or somatic mutations in BRCA1, or epigenetic silencing of BRCA1, which re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::479dbf6680c67f499f0160c21c55c3ec
https://doi.org/10.1158/1538-7445.sabcs18-p6-20-05

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Bone morphogenetic protein receptor 2 inhibition destabilizes microtubules promoting the activation of lysosomes and cell death of lung cancer cells

Autor: Salma K. Jabbour, John Langenfeld, Elaine Langenfeld, Logan Napoli, Jacques Roberge, Arindam Mondal, Youyi Peng, Dongxuan Jia, John A. Gilleran, Christopher Rongo, Zoya Syed, Rachel NeMoyer, Mehul Vora

Publikováno v: Cell Communication and Signaling : CCS
Cell Communication and Signaling, Vol 19, Iss 1, Pp 1-15 (2021)

BackgroundRecent studies have shown that bone morphogenetic protein receptor 2 (BMPR2) regulates cell survival signaling events in cancer cells independent of the BMP type 1 receptor (BMPR1) or the Smad-1/5 transcription factor. Mutations in BMPR2 tr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2aeb4478bc0be2fd7b129abd3e46cfdc
https://pubmed.ncbi.nlm.nih.gov/34563224

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Bone morphogenetic protein (BMP) receptor inhibitor JL5 synergizes with Ym155 to induce Apoptosis-Inducing Factor (AIF) caspase independent cell death

Autor: John A. Gilleran, Arindam Mondal, Jacques Roberge, Michael Scott, Elaine Langenfeld, Andrew Zloza, David J. Augeri, John Langenfeld, Danea Glover, Rachel NeMoyer, Lauren Lairson, Youyi Peng

Background: Bone morphogenetic protein (BMP) is an evolutionarily conserved morphogen that is reactivated in lung carcinomas. BMP receptor inhibitors promote cell death of lung carcinomas by mechanisms not fully elucidated. The studies here reveal no

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d26fa0d1896b8ebc32cee2bc3155473e
https://doi.org/10.21203/rs.3.rs-20532/v2

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Bone morphogenetic protein (BMP) receptor inhibitor JL5 synergizes with Ym155 to induce AIF-caspase independent cell death

Autor: Arindam Mondal, Jacques Roberge, Michael Scott, John A. Gilleran, Elaine Langenfeld, Andrew Zloza, Rachel NeMoyer, John Langenfeld, Lauren Lairson, Danea Glover, Youyi Peng, David J. Augeri

Background: BMP is an evolutionary conserved morphogen that is reactivated in lung carcinomas. BMP receptor inhibitors promote cell death of lung carcinomas by mechanisms not fully elucidated. The studies here reveal novel mechanisms by which the “

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8bed356959bff67a225add4661a03339
https://doi.org/10.21203/rs.3.rs-20532/v1

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Thiosemicarbazones Functioning as Zinc Metallochaperones to Reactivate Mutant p53

Autor: Ashley T. Tsang, John A. Gilleran, Xin Yu, Adam R. Blanden, Anthony F. Bencivenga, S. David Kimball, Saif Zaman, Darren R. Carpizo, Stewart N. Loh, Yue Liu

Publikováno v: Molecular Pharmacology. 91:567-575

Small-molecule restoration of wild-type structure and function to mutant p53 (so-called mutant reactivation) is a highly sought-after goal in cancer drug development. We previously discovered that small-molecule zinc chelators called zinc metallochap

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ee576c9bcff6cff399a7d714943d9c9
https://doi.org/10.1124/mol.116.107409

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Therapeutic targeting of BRCA1 and TP53 mutant breast cancer through mutant p53 reactivation

Autor: Ming Yao, Tracy Withers, Xin Yu, John A. Gilleran, S. David Kimball, Dirk F. Moore, Bing Xia, Shridar Ganesan, Chunxia Chen, Yong Lin, Darren R. Carpizo, Tzeh Keong Foo, Bing Na

Publikováno v: NPJ Breast Cancer
npj Breast Cancer, Vol 5, Iss 1, Pp 1-10 (2019)

Triple negative breast cancer (TNBC) is an aggressive subset for which effective therapeutic approaches are needed. A significant proportion of TNBC patients harbor either germline or somatic mutations in BRCA1, or epigenetic silencing of BRCA1, whic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6043e92f228aeb4d5643845cbe626a0
https://doi.org/10.1038/s41523-019-0110-1

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