Zobrazeno 1 - 10 of 34 pro vyhledávání: '"Mehran, Jalaie"'
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Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
Autor: Marlena Walls, Tod Smeal, Suvi T. M. Orr, Zhengyu Liu, Cheng Hengmiao, Shuiwang Wang, Kephart Susan Elizabeth, Jean Joo Matthews, Rose Ann Ferre, Neal W. Sach, Scott L. Weinrich, Doug Behenna, Sherry Niessen, Sangita M. Baxi, Deepak Dalvie, Sujin Cho-Schultz, Dac M. Dinh, Kevin Ryan, Jim Solowiej, Elaine E. Tseng, Simon Paul Planken, Sajiv Krishnan Nair, Brion W. Murray, Jun Li Feng, Jennifer Lafontaine, Pairish Mason Alan, Shijian Ren, Michelle Hemkens, Shuibo Xin, Mehran Jalaie, Tran Khanh Tuan, Robert Steven Kania, Sutton Scott Channing, William F. Vernier, Kevin K.-C. Liu, Amy Jackson-Fisher, Beth Lunney, Min-Jean Yin, Ketan S. Gajiwala, Asako Nagata, Haiwei Xu, Michael Zientek, Ru Zhou, Daniel Tyler Richter, Simon Bailey, Martin Paul Edwards, Martha A. Ornelas, Chau Almaden, John Charles Kath, Hong Shen, Theodore O. Johnson
Publikováno v: Journal of Medicinal Chemistry. 59:2005-2024
First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients’ disease progresses, often driven by a second-site mutation in the EGFR kinas
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dcd650965ee5ecc3e2b378a7f2542e1b
https://doi.org/10.1021/acs.jmedchem.5b01633
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3
Reviving B-Factors: Activating ALK Mutations Increase Protein Dynamics of the Unphosphorylated Kinase
Autor: Dan Gehlhaar, Alexei Brooun, Mehran Jalaie, Michele McTigue, Sergei Timofeevski, Ben Bolaños, Gallego Rebecca Anne, Ted William Johnson
Publikováno v: ACS medicinal chemistry letters. 9(9)
[Image: see text] Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that can become oncogenic by activating mutations or overexpression. Full kinetic characterization of both phosphorylated and nonphosphorylated wildtype and mutant ALK k
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b39967fea24061049591a5a3172a007f
https://pubmed.ncbi.nlm.nih.gov/30258533
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4
Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ
Autor: Jo Ann Davis, Christopher F. Bigge, Mehran Jalaie, Seungil Han, Jeffrey F. Ohren, Jing Chen, Noel A. Powell, Fred A. Ciske, Agustin Casimiro-Garcia, Teresa Ellis, Ronald J. Heemstra, Declan Flynn, Nadia Esmaeil
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:767-772
Identification of a series of imidazo[4,5-c]pyridin-4-one derivatives that act as dual angiotensin II type 1 (AT1) receptor antagonists and peroxisome proliferator-activated receptor-γ (PPARγ) partial agonists is described. Starting from a known AT
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1d7100e721853331ca8766501b9c589
https://doi.org/10.1016/j.bmcl.2012.11.088
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5
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
Autor: Hengmiao, Cheng, Sajiv K, Nair, Brion W, Murray, Chau, Almaden, Simon, Bailey, Sangita, Baxi, Doug, Behenna, Sujin, Cho-Schultz, Deepak, Dalvie, Dac M, Dinh, Martin P, Edwards, Jun Li, Feng, Rose Ann, Ferre, Ketan S, Gajiwala, Michelle D, Hemkens, Amy, Jackson-Fisher, Mehran, Jalaie, Ted O, Johnson, Robert S, Kania, Susan, Kephart, Jennifer, Lafontaine, Beth, Lunney, Kevin K-C, Liu, Zhengyu, Liu, Jean, Matthews, Asako, Nagata, Sherry, Niessen, Martha A, Ornelas, Suvi T M, Orr, Mason, Pairish, Simon, Planken, Shijian, Ren, Daniel, Richter, Kevin, Ryan, Neal, Sach, Hong, Shen, Tod, Smeal, Jim, Solowiej, Scott, Sutton, Khanh, Tran, Elaine, Tseng, William, Vernier, Marlena, Walls, Shuiwang, Wang, Scott L, Weinrich, Shuibo, Xin, Haiwei, Xu, Min-Jean, Yin, Michael, Zientek, Ru, Zhou, John C, Kath
Publikováno v: Journal of medicinal chemistry. 59(5)
First generation EGFR TKIs (gefitinib, erlotinib) provide significant clinical benefit for NSCLC cancer patients with oncogenic EGFR mutations. Ultimately, these patients' disease progresses, often driven by a second-site mutation in the EGFR kinase
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f69cf3e766e492ce164cc24ad82b59de
https://pubmed.ncbi.nlm.nih.gov/26756222
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7
Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-γ
Autor: Chad L. Stoner, Teresa Ellis, Robert Ostroski, Ronald J. Heemstra, Jeffrey F. Ohren, Nadia Esmaeil, Christopher F. Bigge, Geyer Andrew George, Jo Ann Davis, Mehran Jalaie, Declan Flynn, Filzen Gary Frederick, Agustin Casimiro-Garcia, Danette Dudley, Jeremy J. Edmunds, Robert P. Schaum, Jing Chen
Publikováno v: Journal of Medicinal Chemistry. 54:4219-4233
Mining of an in-house collection of angiotensin II type 1 receptor antagonists to identify compounds with activity at the peroxisome proliferator-activated receptor-γ (PPARγ) revealed a new series of imidazo[4,5-b]pyridines 2 possessing activity at
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf9c977be8a5559862d6fef61c5de7bc
https://doi.org/10.1021/jm200409s
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8
The flexible alignment of molecular structures using simulated annealing with weighted Lagrangian multipliers
Autor: Mehran Jalaie, John W. Raymond, Daniel D. Holsworth
Publikováno v: Journal of Computational Chemistry. 32:210-217
A framework for superimposing small molecules is presented. The proposed method consists of a simple atom-based, flexible alignment. The optimization procedure used in the alignment is based on a recently published variant of the simulated annealing
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf8d38933e24dac3023dc5b7c75d2378
https://doi.org/10.1002/jcc.21586
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9
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors
Autor: Chad A. Van Huis, Wendy Collard, Cuiman Cai, Michelle Mastronardi, Roxane Collins, Michael J. Ryan, Jeremy J. Edmunds, Erli Zhang, Mehran Jalaie, Chungang Gu, Ken Mennen, John W. Bryant, Patrick I. McConnell, Fred L. Ciske, Suzie Ferreira, Jacqueline E. Day, Daniel D. Holsworth, Noel A. Powell, Igor Mochalkin
Publikováno v: Bioorganic & Medicinal Chemistry. 15:5912-5949
We report the design and synthesis of a series of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as orally bioavailable small molecule inhibitors of renin. Compounds with a 2-methyl-2-aryl substitution pattern exhibit potent renin inhibition and go
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5134728dfb02df8a38ff3f31d48c05e
https://doi.org/10.1016/j.bmc.2007.05.069
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10
Virtual Screening: Are We There Yet?
Autor: Shanmugasundaram, Mehran Jalaie
Publikováno v: Mini-Reviews in Medicinal Chemistry. 6:1159-1167
The cost of pharmaceutical development has increased dramatically in recent years, and many assorted approaches have been developed to decrease both the time and costs associated with bringing a drug to the market. Among these methods is the use of i
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3807d31659acb21c283616d00d9c120
https://doi.org/10.2174/138955706778560157
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