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Almeida et al., “NMR Reporter Assays for the Quantification of Weak-Affinity Receptor–Ligand Interactions”; SLAS Discovery,  April 2021

https://doi.org/10.1177/24725552211009782

Poon et al., “The role of SQSTM1 (p62) in mitochondrial function and clearance in human cortical neurons”; Stem Cell Reports 2021

Poon et al., “The role of SQSTM1 (p62) in mitochondrial function and clearance in human cortical neurons”; Stem Cell Reports 2021

https://doi.org/10.1016/j.stemcr.2021.03.030

Chessari at al. Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction; Med Chem 2021

Chessari at al., “Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction”; Med Chem 2021

https://doi.org/10.1021/acs.jmedchem.0c02188

Sethi et al., “Leveraging omic features with F3UTER enables identification of unannotated 3’UTRs for synaptic genes”

Sethi et al., “Leveraging omic features with F3UTER enables identification of unannotated 3’UTRs for synaptic genes

https://www.nature.com/articles/s41467-022-30017-z

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Brain et al., “The Discovery of Kisqali® (Ribociclib): A CDK4/6 Inhibitor for the Treatment of HR+/HER2− Advanced Breast Cancer”; Successful Drug Discovery; Vol 5; 2021; chapter 9

Brain et al., “The Discovery of Kisqali® (Ribociclib): A CDK4/6 Inhibitor for the Treatment of HR+/HER2− Advanced Breast Cancer”; Successful Drug Discovery; Vol 5; 2021; chapter 9

https://doi.org/10.1002/9783527826872.ch9

Grainger et al., “A Perspective on the Analytical Challenges Encountered in High-Throughput Experimentation”; Organic Process Research and Development, 2021

Grainger et al., “A Perspective on the Analytical Challenges Encountered in High-Throughput Experimentation”; Organic Process Research and Development, 2021

https://dx.doi.org/10.1021/acs.oprd.0c00463

St. Denis et al., “Fragment-based drug discovery: opportunities for organic synthesis”; RSC Medicinal Chemistry, 2021

St. Denis et al., “Fragment-based drug discovery: opportunities for organic synthesis”; RSC Medicinal Chemistry, 2021

https://pubs.rsc.org/en/content/articlelanding/2021/md/d0md00375a#!divAbstract

Holvey et al., “Identifying and Developing Small Molecule Inhibitors of Protein–Protein Interactions”; RSC Publications, 2020

Holvey et al., “Identifying and Developing Small Molecule Inhibitors of Protein–Protein Interactions”; RSC Publications, 2020

https://doi.org/10.1039/9781839160677

Jahnke et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2019”; Journal of Medicinal Chemistry, 2020

Jahnke et al., “Fragment-to-Lead Medicinal Chemistry Publications in 2019”; Journal of Medicinal Chemistry, 2020

https://doi.org/10.1021/acs.jmedchem.0c01608

2020 EORTC-NCI-AACR: The non-peptidomimetic cIAP1/2 and XIAP antagonist tolinapant promotes an anti-tumour immune response in T-cell lymphoma

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The non-peptidomimetic cIAP1/2 and XIAP antagonist tolinapant promotes an anti-tumour immune response in T-cell lymphoma

Summary

Tolinapant (ASTX660) is a potent, non-peptidomimetic antagonist of the cellular and X-linked inhibitors of apoptosis proteins (cIAP1/2 and XIAP) [1], which is currently being tested in a first in human phase I-II clinical trial in patients with advanced solid tumours and lymphomas (NCT02503423) [2]. IAP antagonists have been reported to exhibit broad immuno-modulatory effects on both the innate and adaptive immune systems. We have investigated the profile of tolinapant in preclinical T cell lymphoma models and evaluated tolinapant’s ability to enhance immune mediated killing of T cell lymphoma cells, both in vitro and in vivo.

References:

  1. G Ward et al., 2018, Mol Cancer Therapeutics Jul;17(7):1381-1391
  2. A Hollebecque et al., 2019, AACR-NCI-EORTC International Conference on Molecular
    Targets and Cancer Therapeutics