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Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis

Cancer cell, 2015-11, Vol.28 (5), p.653-665

2015

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Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

Journal of medicinal chemistry, 2015-12, Vol.58 (24), p.9480-9497

2015

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Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity

Journal of medicinal chemistry, 2020-05, Vol.63 (10), p.5398-5420

2020

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EBV+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22

PLoS pathogens, 2022-01, Vol.18 (1), p.e1010200-e1010200

2022

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Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.8584-8607

2020

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The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma

Molecular cancer therapeutics, 2017-11, Vol.16 (11), p.2375-2386

2017

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Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy

Journal of medicinal chemistry, 2022-10, Vol.65 (19), p.12895-12924

2022

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Discovery of a Potent and Selective CCR4 Antagonist That Inhibits T reg Trafficking into the Tumor Microenvironment

Journal of medicinal chemistry, 2019-07, Vol.62 (13), p.6190-6213

2019

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Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment

Journal of medicinal chemistry, 2019-07, Vol.62 (13), p.6190-6213

2019

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Characterization of N-(adamantan-1-ylmethyl)-5-[(3R-amino-pyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 antagonist in animal models of pain and inflammation

The Journal of pharmacology and experimental therapeutics, 2008-12, Vol.327 (3), p.620

2008

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3-Substituted GABA analogs with central nervous system activity: A review

Medicinal research reviews, 1999-03, Vol.19 (2), p.149-177

1999

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Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein

Journal of medicinal chemistry, 2005-04, Vol.48 (7), p.2294-2307

2005

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Discovery of a novel potent GABA(B) receptor agonist

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6582-6585

2011

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Discovery of a novel potent GABAB receptor agonist

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (21), p.6582-6585

2011

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Tumors establish resistance to immunotherapy by regulating Treg recruitment via CCR4

Journal for immunotherapy of cancer, 2020-11, Vol.8 (2)

2020

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Oxadiazolone bioisosteres of pregabalin and gabapentin

Bioorganic & medicinal chemistry letters, 2009, Vol.19 (1), p.247-250

2009

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The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases

Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (9), p.2337-2340

2006

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Novel Cyclopropyl β-Amino Acid Analogues of Pregabalin and Gabapentin That Target the α2-δ Protein

Journal of medicinal chemistry, 2005-04, Vol.48 (8), p.3026-3035

2005

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Clinical and molecular effects of oral CCR4 antagonist RPT193 in atopic dermatitis: A Phase 1 study

Allergy (Copenhagen), 2024-04, Vol.79 (4), p.924-936

2024

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Tumors establish resistance to immunotherapy by regulating T reg recruitment via CCR4

Journal for immunotherapy of cancer, 2020-11, Vol.8 (2), p.e000764

2020

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1-Benzylbenzimidazoles : The discovery of a novel series of bradykinin B1 receptor antagonists

Bioorganic & medicinal chemistry letters, 2008-09, Vol.18 (18), p.5027-5031

2008

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Heteroaromatic side-chain analogs of pregabalin

Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (9), p.2329-2332

2006

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Isoindolinone enantiomers having affinity for the dopamine D4 receptor

Bioorganic & medicinal chemistry letters, 1998-06, Vol.8 (12), p.1499-1502

1998

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EBV.sup.+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22

PLoS pathogens, 2022-01, Vol.18 (1)

2022

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Aminopyrazine CB1 receptor inverse agonists

Bioorganic & medicinal chemistry, 2008-06, Vol.18 (11), p.3376-3381

2008

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Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis

Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)

Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity

EBV+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22

Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors

The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma

Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy

Discovery of a Potent and Selective CCR4 Antagonist That Inhibits T reg Trafficking into the Tumor Microenvironment

Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment

Characterization of N-(adamantan-1-ylmethyl)-5-[(3R-amino-pyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 antagonist in animal models of pain and inflammation

3-Substituted GABA analogs with central nervous system activity: A review

Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein

Discovery of a novel potent GABA(B) receptor agonist

Discovery of a novel potent GABAB receptor agonist

Tumors establish resistance to immunotherapy by regulating Treg recruitment via CCR4

Oxadiazolone bioisosteres of pregabalin and gabapentin

The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases

Novel Cyclopropyl β-Amino Acid Analogues of Pregabalin and Gabapentin That Target the α2-δ Protein

Clinical and molecular effects of oral CCR4 antagonist RPT193 in atopic dermatitis: A Phase 1 study

Tumors establish resistance to immunotherapy by regulating T reg recruitment via CCR4

1-Benzylbenzimidazoles : The discovery of a novel series of bradykinin B1 receptor antagonists

Heteroaromatic side-chain analogs of pregabalin

Isoindolinone enantiomers having affinity for the dopamine D4 receptor

EBV.sup.+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22

Aminopyrazine CB1 receptor inverse agonists

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