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Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy

Proceedings of the National Academy of Sciences - PNAS, 2013-09, Vol.110 (36), p.E3445-E3454

2013

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Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

Journal of medicinal chemistry, 2010-06, Vol.53 (12), p.4701-4719

2010

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Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists

Nature communications, 2024-01, Vol.15 (1), p.489-489, Article 489

2024

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Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties

Molecules (Basel, Switzerland), 2019-06, Vol.24 (12), p.2292

2019

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The novel peptide LCGM-10 attenuates metabotropic glutamate receptor 5 activity and demonstrates behavioral effects in animal models

Frontiers in behavioral neuroscience, 2024-02, Vol.18, p.1333258-1333258

2024

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De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits

ACS medicinal chemistry letters, 2020-10, Vol.11 (10), p.1993-2001

2020

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Probing theα-Helical Structural Stability of Stapled p53 Peptides: Molecular Dynamics Simulations and Analysis

Chemical biology & drug design, 2010-04, Vol.75 (4), p.348-359

2010

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Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML

Blood, 2004-10, Vol.104 (8), p.2532-2539

2004

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Aqueous remote loading of setmelanotide in poly(lactic-co-glycolic acid) microspheres for long-term obesity treatment

Journal of controlled release, 2023-12, Vol.364, p.589-600

2023

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Targeting anti-cancer agents to bone using bisphosphonates

Bone (New York, N.Y.), 2020-09, Vol.138, p.115492-115492, Article 115492

2020

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Activity of Dual SRC-ABL Inhibitors Highlights the Role of BCR/ABL Kinase Dynamics in Drug Resistance

Proceedings of the National Academy of Sciences - PNAS, 2006-06, Vol.103 (24), p.9244-9249

2006

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Photoredox Ni-catalyzed peptide C(sp)-O cross-coupling: from intermolecular reactions to side chain-to-tail macrocyclization

Chemical science (Cambridge), 2019-05, Vol.1 (19), p.573-578

2019

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Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α‑Helical Peptide in Clinical Development

Journal of medicinal chemistry, 2023-07, Vol.66 (14), p.9401-9417

2023

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Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors

Expert opinion on investigational drugs, 2004-01, Vol.13 (1), p.1-19

Sawyer, Tomi K

2004

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Editor's Note: Identification of Src-Specific Phosphorylation Site on Focal Adhesion Kinase: Dissection of the Role of Src SH2 and Catalytic Functions and Their Consequences for Tumor Cell Behavior

Cancer research (Chicago, Ill.), 2022-07, Vol.82 (13), p.2500-2500

2022

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AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes

Molecular cancer therapeutics, 2005-12, Vol.4 (12), p.1900-1911

2005

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Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges

Bioorganic & medicinal chemistry, 2018-06, Vol.26 (10), p.2807-2815

2018

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Molecular Simulations Identify Binding Poses and Approximate Affinities of Stapled α‑Helical Peptides to MDM2 and MDMX

Journal of chemical theory and computation, 2017-02, Vol.13 (2), p.863-869

2017

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Demonstration of a Common DPhe 7 to DNal(2') 7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides

Journal of medicinal chemistry, 2022-04, Vol.65 (8), p.5990-6000

2022

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Demonstration of a Common DPhe7 to DNal(2′)7 Peptide Ligand Antagonist Switch for Melanocortin‑3 and Melanocortin‑4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides

Journal of medicinal chemistry, 2022-04, Vol.65 (8), p.5990-6000

2022

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Novel chemistry for undruggable targets

European journal of medicinal chemistry, 2015-04, Vol.94, p.458-458

2015

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Macrocyclization of an all- d linear α-helical peptide imparts cellular permeability

Chemical science (Cambridge), 2020-06, Vol.11 (21), p.5577-5591

2020

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Liposome Click Membrane Permeability Assay for Identifying Permeable Peptides

Pharmaceutical research, 2021-05, Vol.38 (5), p.843-850

2021

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NanoClick: A High Throughput, Target-Agnostic Peptide Cell Permeability Assay

ACS chemical biology, 2021-02, Vol.16 (2), p.293-309

2021

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Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists

Incorporation of Putative Helix-Breaking Amino Acids in the Design of Novel Stapled Peptides: Exploring Biophysical and Cellular Permeability Properties

The novel peptide LCGM-10 attenuates metabotropic glutamate receptor 5 activity and demonstrates behavioral effects in animal models

De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits

Probing theα-Helical Structural Stability of Stapled p53 Peptides: Molecular Dynamics Simulations and Analysis

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML

Aqueous remote loading of setmelanotide in poly(lactic-co-glycolic acid) microspheres for long-term obesity treatment

Targeting anti-cancer agents to bone using bisphosphonates

Activity of Dual SRC-ABL Inhibitors Highlights the Role of BCR/ABL Kinase Dynamics in Drug Resistance

Photoredox Ni-catalyzed peptide C(sp)-O cross-coupling: from intermolecular reactions to side chain-to-tail macrocyclization

Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α‑Helical Peptide in Clinical Development

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

Cancer metastasis therapeutic targets and drug discovery: emerging small-molecule protein kinase inhibitors

Editor's Note: Identification of Src-Specific Phosphorylation Site on Focal Adhesion Kinase: Dissection of the Role of Src SH2 and Catalytic Functions and Their Consequences for Tumor Cell Behavior

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes

Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges

Molecular Simulations Identify Binding Poses and Approximate Affinities of Stapled α‑Helical Peptides to MDM2 and MDMX

Demonstration of a Common DPhe 7 to DNal(2') 7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides

Demonstration of a Common DPhe7 to DNal(2′)7 Peptide Ligand Antagonist Switch for Melanocortin‑3 and Melanocortin‑4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides

Novel chemistry for undruggable targets

Macrocyclization of an all- d linear α-helical peptide imparts cellular permeability

Liposome Click Membrane Permeability Assay for Identifying Permeable Peptides

NanoClick: A High Throughput, Target-Agnostic Peptide Cell Permeability Assay

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