Zobrazeno 1 - 9 of 9 pro vyhledávání: '"Afshin, Mahmoudi"'
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Akademický článek
Crystal structures of PRK1 in complex with the clinical compounds lestaurtinib and tofacitinib reveal ligand induced conformational changes.
Autor: Philip Chamberlain, Silvia Delker, Barbra Pagarigan, Afshin Mahmoudi, Pilgrim Jackson, Mahan Abbasian, Jeff Muir, Neil Raheja, Brian Cathers
Publikováno v: PLoS ONE, Vol 9, Iss 8, p e103638 (2014)
Protein kinase C related kinase 1 (PRK1) is a component of Rho-GTPase, androgen receptor, histone demethylase and histone deacetylase signaling pathways implicated in prostate and ovarian cancer. Herein we describe the crystal structure of PRK1 in ap
Externí odkaz: https://doaj.org/article/c526a3195de743a1bd4e5704485209b9
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2
Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1
Autor: Kevin Ronald Condroski, Matt Hickman, Wei Liu, Laurie LeBrun, Gilles Carmel, Joshua Hansen, Gang Lu, Afshin Mahmoudi, Frans Baculi, Correa Matthew D, Tim Crea, Hon-Wah Man, George W. Muller, Chin-Chun Lu, Alexander L. Ruchelman, Fan Vocanson, Weihong Zhang
Publikováno v: Journal of Medicinal Chemistry. 61:492-503
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure–activity relationships for analogs of 3 with exploration of the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::82b447b68c060eec6fd08bffe825f2a7
https://doi.org/10.1021/acs.jmedchem.6b01911
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3
Protein Degradation via CRL4
Autor: Joshua D, Hansen, Kevin, Condroski, Matthew, Correa, George, Muller, Hon-Wah, Man, Alexander, Ruchelman, Weihong, Zhang, Fan, Vocanson, Tim, Crea, Wei, Liu, Gang, Lu, Frans, Baculi, Laurie, LeBrun, Afshin, Mahmoudi, Gilles, Carmel, Matt, Hickman, Chin-Chun, Lu
Publikováno v: Journal of medicinal chemistry. 61(2)
We previously disclosed the identification of cereblon modulator 3 (CC-885), with potent antitumor activity mediated through the degradation of GSPT1. We describe herein the structure-activity relationships for analogs of 3 with exploration of the st
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f8916d455404142030cbeb1a6662660c
https://pubmed.ncbi.nlm.nih.gov/28358507
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6
Crystal Structures of PRK1 in Complex with the Clinical Compounds Lestaurtinib and Tofacitinib Reveal Ligand Induced Conformational Changes
Autor: Afshin Mahmoudi, Barbra Pagarigan, Philip P Chamberlain, Neil Raheja, Mahan Abbasian, Jeff Muir, Brian E. Cathers, Silvia L. Delker, Pilgrim Jackson
Publikováno v: PLoS ONE, Vol 9, Iss 8, p e103638 (2014)
PLoS ONE
Protein kinase C related kinase 1 (PRK1) is a component of Rho-GTPase, androgen receptor, histone demethylase and histone deacetylase signaling pathways implicated in prostate and ovarian cancer. Herein we describe the crystal structure of PRK1 in ap
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::800a3fdeb62b9d7b6b1d97d0c28941e9
https://doi.org/10.1371/journal.pone.0103638
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7
Inhibitor Binding Mode Differences Within the AGC Subfamily
Autor: Philip P Chamberlain, Brian E. Cathers, Daniel Cashion, Sami Bahmanyar, Wei Fang, Silvia L. Delker, Mahan Abbasian, Barbra Pagarigan, Afshin Mahmoudi, Dale Robinson
Publikováno v: Acta Crystallographica Section A Foundations and Advances. 70:C1640-C1640
Designing potent selective kinase inhibitors is an ongoing challenge due to the high level of homology within the protein kinome. The AGC family comprises ~12% of the kinome and includes many important drug targets. We compared the binding mode of tw
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::616f2e11808b80af6ce1e6d035e66019
https://doi.org/10.1107/s2053273314083594
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8
Direct Binding with Cereblon Mediates the Antiproliferative and Immunomodulatory Action of Lenalidomide and Pomalidomide
Autor: Anita Gandhi, Helen Brady, Antonia Lopez-Girona, Normand Richard, Emily Rychak, Brian E. Cathers, Jilly F. Evans, Jian Kang, Afshin Mahmoudi, Derek Mendy, Pilgrim Jackson, Gilles Carmel, Peter H. Schafer, Thomas O. Daniel, Karen Miller, Mahan Abbasian, Rajesh Chopra
Publikováno v: Blood. 118:738-738
Abstract 738 Thalidomide, lenalidomide and pomalidomide are therapeutically active in a number of hematological malignant and premalignant conditions including myelodysplastic syndromes, multiple myeloma, and lymphomas. Clinical efficacy is ascribed
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cd49be72743b4398c05427f7b14eb908
https://doi.org/10.1182/blood.v118.21.738.738
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9
Potent triazolopyridine and pyrazolopyrimidine inhibitors of PLK1 and the structural basis for divergent SAR between the series
Autor: Barbra Pagarigan, S. Bahmanyar, J.R. Riggs, Philip P Chamberlain, Afshin Mahmoudi, D. Zhu, J. Muir, P. Patel, Mahan Abbasian
Publikováno v: Acta Crystallographica Section A Foundations of Crystallography. 67:C816-C816
Polo-like kinase 1 (PLK1) is a serine/threonine kinase which functions in mitosis and cytokinesis and as such is a target for anticancer therapeutics. Here we describe the discovery of 2 classes of potent PLK1 inhibitors: namely, the [1,2,4]triazolo[
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::00308ba1761b57186c2366794251c914
https://doi.org/10.1107/s0108767311079323
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