UB Paderborn / Katalog / Suche / in CDI

Translation control of the immune checkpoint in cancer and its therapeutic targeting

Nature medicine, 2019-02, Vol.25 (2), p.301-311

2019

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Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase

Journal of medicinal chemistry, 2020-06, Vol.63 (11), p.5879-5955

2020

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Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations

Molecular cancer therapeutics, 2021-12, Vol.20 (12), p.2446-2456

2021

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Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A

Molecular cancer therapeutics, 2021-01, Vol.20 (1), p.26-36

2021

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Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors

Organic letters, 2020-08, Vol.22 (16), p.6257-6261

2020

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1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties

Bioorganic & medicinal chemistry letters, 2021-09, Vol.47, p.128111-128111, Article 128111

2021

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Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series

Journal of medicinal chemistry, 1996-07, Vol.39 (14), p.2781-2794

1996

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Abstract 1119: Molecular characteristics of repotrectinib that enable potent inhibition of TRK fusion proteins and broad mutant selectivity

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.1119-1119

2021

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Bis Tertiary Amide Inhibitors of the HIV-1 Protease Generated via Protein Structure-Based Iterative Design

Journal of medicinal chemistry, 1996-07, Vol.39 (14), p.2795-2811

1996

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Tripeptide Aldehyde Inhibitors of Human Rhinovirus 3C Protease: Design, Synthesis, Biological Evaluation, and Cocrystal Structure Solution of P1 Glutamine Isosteric Replacements

Journal of medicinal chemistry, 1998-07, Vol.41 (15), p.2786-2805

1998

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Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis

Journal of medicinal chemistry, 1992-03, Vol.35 (5), p.847-858

1992

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Structure-Based Design of a Parallel Synthetic Array Directed Toward the Discovery of Irreversible Inhibitors of Human Rhinovirus 3C Protease

Journal of medicinal chemistry, 2002-05, Vol.45 (10), p.2016-2023

2002

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Enantioselective total synthesis of 9S-dihydroerythronolide A seco acid

Journal of the American Chemical Society, 1989-08, Vol.111 (16), p.6247-6256

1989

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Substituted Benzamide Inhibitors of Human Rhinovirus 3C Protease: Structure-Based Design, Synthesis, and Biological Evaluation

Journal of medicinal chemistry, 2000-05, Vol.43 (9), p.1670-1683

2000

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Abstract B33: Targeting PI3K/mTOR signaling with potent, selective and orally-available small-molecule inhibitors of eIF4E

Molecular cancer research, 2020-10, Vol.18 (10_Supplement), p.B33-B33

2020

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Abstract 1302: Targeting hormone receptor-dependent cancers with potent, selective and orally-available small molecule inhibitors of eIF4E

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.1302-1302

2019

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Abstract 2698: eFT226, a potent and selective inhibitor of eIF4A, is efficacious in preclinical models of lymphoma

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.2698-2698

2019

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Abstract B133: eFT226, a first in class inhibitor of eIF4A1, targets FGFR1/2 and HER2 driven cancers

Molecular cancer therapeutics, 2019-12, Vol.18 (12_Supplement), p.B133-B133

2019

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Abstract DDT02-05: eFT226: A selective and highly potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a novel approach for the treatment of cancer

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.DDT02-05-DDT02-05

2018

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Abstract 596: eFT508, a potent and highly selective inhibitor of MNK1/2 regulates immune checkpoint and cytokine expression promoting anti-tumor immunity

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.596-596

2017

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Abstract PR11: eFT508: An oral, potent and highly selective inhibitor of MNK1 and MNK2, promotes anti-tumor immunity as a monotherapy and in combination with immune checkpoint blockade

Cancer research (Chicago, Ill.), 2017-03, Vol.77 (6_Supplement), p.PR11-PR11

2017

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Translation control of the immune checkpoint in cancer and its therapeutic targeting

Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase

Structure-based Design of Pyridone–Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition

Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations

Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A

Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors

1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties

SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo

Structure-Based Design and Synthesis of Substituted 2-Butanols as Nonpeptidic Inhibitors of HIV Protease: Secondary Amide Series

Abstract 1119: Molecular characteristics of repotrectinib that enable potent inhibition of TRK fusion proteins and broad mutant selectivity

Bis Tertiary Amide Inhibitors of the HIV-1 Protease Generated via Protein Structure-Based Iterative Design

Tripeptide Aldehyde Inhibitors of Human Rhinovirus 3C Protease: Design, Synthesis, Biological Evaluation, and Cocrystal Structure Solution of P1 Glutamine Isosteric Replacements

Design and synthesis of novel 6,7-imidazotetrahydroquinoline inhibitors of thymidylate synthase using iterative protein crystal structure analysis

Structure-Based Design of a Parallel Synthetic Array Directed Toward the Discovery of Irreversible Inhibitors of Human Rhinovirus 3C Protease

Enantioselective total synthesis of 9S-dihydroerythronolide A seco acid

Substituted Benzamide Inhibitors of Human Rhinovirus 3C Protease: Structure-Based Design, Synthesis, and Biological Evaluation

Abstract B33: Targeting PI3K/mTOR signaling with potent, selective and orally-available small-molecule inhibitors of eIF4E

Abstract 1302: Targeting hormone receptor-dependent cancers with potent, selective and orally-available small molecule inhibitors of eIF4E

Abstract 2698: eFT226, a potent and selective inhibitor of eIF4A, is efficacious in preclinical models of lymphoma

Abstract B133: eFT226, a first in class inhibitor of eIF4A1, targets FGFR1/2 and HER2 driven cancers

Abstract DDT02-05: eFT226: A selective and highly potent inhibitor of eukaryotic initiation factor 4A (eIF4A), a novel approach for the treatment of cancer

Preclinical Evaluation of eFT226, a Novel, Potent and Selective eIF4A Inhibitor with Anti-Tumor Activity in B-Cell Malignancies

Abstract 596: eFT508, a potent and highly selective inhibitor of MNK1/2 regulates immune checkpoint and cytokine expression promoting anti-tumor immunity

Abstract PR11: eFT508: An oral, potent and highly selective inhibitor of MNK1 and MNK2, promotes anti-tumor immunity as a monotherapy and in combination with immune checkpoint blockade

eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL)

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