Publications by authors named "Georgette Castanedo"

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Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Marie-Gabrielle Braun, Avi Ashkenazi, Ramsay E Beveridge, Georgette Castanedo, Heidi Ackerly Wallweber

J Med Chem· June 2024

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Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte Formation.
Ruth Dorel, Dawei Sun, Nicholas Carruthers, Georgette M Castanedo, Peter M-U Ung

J Med Chem· March 2024

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Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design.
James J Crawford, Jianwen Feng, Hans D Brightbill, Adam R Johnson, Matthew Wright, Georgette M Castanedo

Bioorg Med Chem Lett· June 2023

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Optimization of globomycin analogs as novel gram-negative antibiotics.
Keira Garland, Homer Pantua, Marie-Gabrielle Braun, Daniel J Burdick, Georgette M Castanedo

Bioorg Med Chem Lett· October 2020

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Unstable Mechanisms of Resistance to Inhibitors of Escherichia coli Lipoprotein Signal Peptidase.
Homer Pantua, Elizabeth Skippington, Marie-Gabrielle Braun, Cameron L Noland, Jingyu Diao, Georgette M Castanedo

mBio· September 2020

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Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.
Brendan T Parr, Richard Pastor, Benjamin D Sellers, Zhonghua Pei, Firoz A Jaipuri, Georgette M Castanedo

ACS Med Chem Lett· April 2020

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Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).
Jianwen A Feng, Patrick Lee, Moulay Hicham Alaoui, Kathy Barrett, Georgette Castanedo

ACS Med Chem Lett· September 2019

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Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.
Nicole Blaquiere, Georgette M Castanedo, Jason D Burch, Leonid M Berezhkovskiy, Hans Brightbill

J Med Chem· August 2018

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Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
James J Crawford, Adam R Johnson, Dinah L Misner, Lisa D Belmont, Georgette Castanedo

J Med Chem· March 2018

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NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Hans D Brightbill, Eric Suto, Nicole Blaquiere, Nandhini Ramamoorthi, Swathi Sujatha-Bhaskar, Georgette M Castanedo

Nat Commun· January 2018

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Introduction of Trifluoroethylamine as Amide Isostere by C-H Functionalization of Heteroarenes.
Marie-Gabrielle Braun, Georgette Castanedo, Ling Qin, Patrick Salvo, Samir Z Zard

Org Lett· August 2017

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Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).
Georgette M Castanedo, Nicole Blaquiere, Maureen Beresini, Brandon Bravo, Hans Brightbill

J Med Chem· January 2017

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Synthesis of Fused Imidazole-Containing Ring Systems via Dual Oxidative Amination of C(sp(3))-H Bonds.
Georgette Castanedo, Yanzhou Liu, James J Crawford, Marie-Gabrielle Braun

J Org Chem· September 2016

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Investigations into the mechanisms of pyridine ring cleavage in vismodegib.
S Cyrus Khojasteh, Qin Yue, Shuguang Ma, Georgette Castanedo, Jacob Z Chen

Drug Metab Dispos· March 2014

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Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.
Brian S Safina, Zachary K Sweeney, Jun Li, Bryan K Chan, Angelina Bisconte, Georgette Castanedo

Bioorg Med Chem Lett· September 2013

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Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.
Jeremy M Murray, Zachary K Sweeney, Bryan K Chan, Mercedesz Balazs, Erin Bradley, Georgette Castanedo

J Med Chem· September 2012

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Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.
Daniel P Sutherlin, Stewart Baker, Angelina Bisconte, Paul M Blaney, Anthony Brown, Georgette Castanedo

Bioorg Med Chem Lett· July 2012

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Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.
Brian S Safina, Stewart Baker, Matt Baumgardner, Paul M Blaney, Bryan K Chan, Georgette Castanedo

J Med Chem· June 2012

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Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Daniel P Sutherlin, Linda Bao, Megan Berry, Georgette Castanedo, Irina Chuckowree

J Med Chem· November 2011

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Rapid synthesis of 1,3,5-substituted 1,2,4-triazoles from carboxylic acids, amidines, and hydrazines.
Georgette M Castanedo, Pamela S Seng, Nicole Blaquiere, Sean Trapp, Steven T Staben

J Org Chem· February 2011

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Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.
Georgette M Castanedo, Shumei Wang, Kirk D Robarge, Elizabeth Blackwood, Daniel Burdick

Bioorg Med Chem Lett· November 2010

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Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Steven T Staben, Timothy P Heffron, Daniel P Sutherlin, Seema R Bhat, Georgette M Castanedo

Bioorg Med Chem Lett· October 2010

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Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
Timothy P Heffron, Megan Berry, Georgette Castanedo, Christine Chang, Irina Chuckowree

Bioorg Med Chem Lett· April 2010

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Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
Daniel P Sutherlin, Deepak Sampath, Megan Berry, Georgette Castanedo, Zhigang Chang

J Med Chem· February 2010

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GDC-0449-a potent inhibitor of the hedgehog pathway.
Kirk D Robarge, Shirley A Brunton, Georgette M Castanedo, Yong Cui, Michael S Dina

Bioorg Med Chem Lett· October 2009

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