Publications by authors named "Mark Ultsch"

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Discovery and characterization of potent macrocycle inhibitors of ubiquitin-specific protease-7.
Rafael Miranda, Francesca Anson, Shannon T Smith, Mark Ultsch, Connie A Tenorio

Structure· April 2025

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Cystine-knot peptide inhibitors of HTRA1 bind to a cryptic pocket within the active site region.
Yanjie Li, Yuehua Wei, Mark Ultsch, Wei Li, Wanjian Tang

Nat Commun· May 2024

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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Emily J Hanan, Marie-Gabrielle Braun, Robert A Heald, Calum MacLeod, Connie Chan, Mark Ultsch

J Med Chem· December 2022

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Overcoming Preclinical Safety Obstacles to Discover ()--((1,2,3,5,6,7-Hexahydro--indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5-pyrazolo[5,1-][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
Christopher McBride, Lynnie Trzoss, Davide Povero, Milos Lazic, Geza Ambrus-Aikelin, Mark Ultsch

J Med Chem· November 2022

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Allosteric inhibition of HTRA1 activity by a conformational lock mechanism to treat age-related macular degeneration.
Stefan Gerhardy, Mark Ultsch, Wanjian Tang, Evan Green, Jeffrey K Holden

Nat Commun· September 2022

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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
BinQing Wei, Kirk Robarge, Sharada S Labadie, Jinhua Chen, Laura B Corson, Mark Ultsch

Bioorg Med Chem Lett· March 2022

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Structures of the ApoL1 and ApoL2 N-terminal domains reveal a non-classical four-helix bundle motif.
Mark Ultsch, Michael J Holliday, Stefan Gerhardy, Paul Moran, Suzie J Scales

Commun Biol· July 2021

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Regions of conformational flexibility in the proprotein convertase PCSK9 and design of antagonists for LDL cholesterol lowering.
Daniel Kirchhofer, Daniel J Burdick, Nicholas J Skelton, Yingnan Zhang, Mark Ultsch

Biochem Soc Trans· August 2020

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Design of Organo-Peptides As Bipartite PCSK9 Antagonists.
Daniel J Burdick, Nicholas J Skelton, Mark Ultsch, Maureen H Beresini, Charles Eigenbrot

ACS Chem Biol· February 2020

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Tetravalent biepitopic targeting enables intrinsic antibody agonism of tumor necrosis factor receptor superfamily members.
Yanli Yang, Sherry H Yeh, Shravan Madireddi, Wadim L Matochko, Chen Gu, Mark Ultsch

MAbs· January 2020

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Development, Optimization, and Structural Characterization of an Efficient Peptide-Based Photoaffinity Cross-Linking Reaction for Generation of Homogeneous Conjugates from Wild-Type Antibodies.
Nicholas Vance, Neelie Zacharias, Mark Ultsch, Guangmin Li, Aimee Fourie

Bioconjug Chem· January 2019

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Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.
Yingnan Zhang, Mark Ultsch, Nicholas J Skelton, Daniel J Burdick, Maureen H Beresini

Nat Struct Mol Biol· October 2017

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Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Jun Liang, Anne Van Abbema, Mercedesz Balazs, Kathy Barrett, Leo Berezhkovsky, Mark Ultsch

Bioorg Med Chem Lett· September 2017

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Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.
Brian S Safina, Richard L Elliott, Andrew K Forrest, Robert A Heald, Jeremy M Murray, Mark Ultsch

ACS Med Chem Lett· September 2017

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Structure of Crenezumab Complex with Aβ Shows Loss of β-Hairpin.
Mark Ultsch, Bing Li, Till Maurer, Mary Mathieu, Oskar Adolfsson

Sci Rep· December 2016

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Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity.
Calliope A Dendrou, Adrian Cortes, Lydia Shipman, Hayley G Evans, Kathrine E Attfield, Mark Ultsch

Sci Transl Med· November 2016

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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
Hans E Purkey, Kirk Robarge, Jinhua Chen, Zhongguo Chen, Laura B Corson, Mark Ultsch

ACS Med Chem Lett· October 2016

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Developments in the Implementation of Acoustic Droplet Ejection for Protein Crystallography.
Ping Wu, Cameron Noland, Mark Ultsch, Bonnie Edwards, David Harris

J Lab Autom· February 2016

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Generation of a high-fidelity antibody against nerve growth factor using library scanning mutagenesis and validation with structures of the initial and optimized Fab-antigen complexes.
Sherry L La Porte, Charles Eigenbrot, Mark Ultsch, Wei-Hsien Ho, Davide Foletti

MAbs· February 2015

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Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Sharada Labadie, Peter S Dragovich, Jinhua Chen, Benjamin P Fauber, Jason Boggs, Mark Ultsch

Bioorg Med Chem Lett· January 2015

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Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.
Benjamin P Fauber, Peter S Dragovich, Jinhua Chen, Laura B Corson, Charles Z Ding, Mark Ultsch

Bioorg Med Chem Lett· December 2014

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Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Kirk D Robarge, Wendy Lee, Charles Eigenbrot, Mark Ultsch, Christian Wiesmann

Bioorg Med Chem Lett· October 2014

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Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Peter S Dragovich, Benjamin P Fauber, Jason Boggs, Jinhua Chen, Laura B Corson, Mark Ultsch

Bioorg Med Chem Lett· August 2014

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Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition.
Patrick J Lupardus, Mark Ultsch, Heidi Wallweber, Pawan Bir Kohli, Adam R Johnson

Proc Natl Acad Sci U S A· June 2014

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Antiparallel conformation of knob and hole aglycosylated half-antibody homodimers is mediated by a CH2-CH3 hydrophobic interaction.
J Michael Elliott, Mark Ultsch, Joshua Lee, Raymond Tong, Kentaro Takeda

J Mol Biol· May 2014

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