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Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

Journal of medicinal chemistry, 2010-04, Vol.53 (7), p.2681-2694

2010

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Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death

Nature chemical biology, 2013-09, Vol.9 (9), p.548-556

2013

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PARP inhibitors in cancer therapy: an update

Expert opinion on therapeutic patents, 2013-04, Vol.23 (4), p.503-514

2013

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3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding

Journal of medicinal chemistry, 2004-06, Vol.47 (13), p.3367-3380

2004

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Optimization of 6,6-dimethyl pyrrolo[3,4- c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing

Bioorganic & medicinal chemistry, 2010-03, Vol.18 (5), p.1844-1853

2010

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The target landscape of clinical kinase drugs

Science (American Association for the Advancement of Science), 2017-12, Vol.358 (6367), p.1148-1148

2017

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Dimer Formation through Domain Swapping in the Crystal Structure of the Grb2-SH2−Ac-pYVNV Complex

Biochemistry (Easton), 2000-11, Vol.39 (44), p.13376-13382

2000

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Stereoselective synthesis of 3,4‐dihydropyrrolo[1,2‐a]pyrazin‐1(2H)‐one derivatives as PIM kinase inhibitors inspired from marine alkaloids

Chirality (New York, N.Y.), 2022-11, Vol.34 (11), p.1437-1452

2022

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Stereoselective synthesis of 3,4‐dihydropyrrolopyrazin‐1(2H)‐one derivatives as PIM kinase inhibitors inspired from marine alkaloids

Chirality (New York, N.Y.), 2022-11, Vol.34 (11), p.1437-1452

2022

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Around the Black Box: Applying the Carltona Principle to Challenge Machine Learning Algorithms in Public Sector Decision-Making

LSE Law Review, 2022-03, Vol.7 (3), p.369-389

Casale, Elena

2022

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Alkylsulfanyl-1,2,4-triazoles, a New Class of Allosteric Valosine Containing Protein Inhibitors. Synthesis and Structure–Activity Relationships

Journal of medicinal chemistry, 2013-01, Vol.56 (2), p.437-450

2013

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Identification of unprecedented ATP-competitive choline kinase inhibitors

Bioorganic & medicinal chemistry letters, 2021-11, Vol.51, p.128310-128310, Article 128310

2021

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Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors

Bioorganic & medicinal chemistry, 2014-08, Vol.22 (15), p.4135-4150

2014

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Discovery of Stereospecific PARP‑1 Inhibitor Isoindolinone NMS-P515

ACS medicinal chemistry letters, 2019-04, Vol.10 (4), p.534-538

2019

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Crystal structure of the T315I abl mutant in complex with the aurora kinases inhibitor PHA-739358

Cancer research (Chicago, Ill.), 2007-09, Vol.67 (17), p.7987-7990

2007

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Abstract 4790: Identification and characterization of ATP-mimetic choline kinase inhibitors

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.4790-4790

2019

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Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design

Biochemistry (Easton), 2013-09, Vol.52 (37), p.6380-6387

2013

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Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases

Bioorganic & medicinal chemistry, 2013-12, Vol.21 (23), p.7364-7380

2013

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Abstract 5163: Characterization of NMS-E194, a selective and potent PERK inhibitor with efficacy in the KMS-11 multiple myeloma

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.5163-5163

2017

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Abstract 2082: NMS-E668, a potent and selective RET kinase inhibitor characterized by specificity towards VEGFR2 and high antitumor efficacy against RET-driven models

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.2082-2082

2017

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Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)

Bioorganic & medicinal chemistry, 2013-11, Vol.21 (22), p.7047-7063

2013

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NMS-E973, a Novel Synthetic Inhibitor of Hsp90 with Activity against Multiple Models of Drug Resistance to Targeted Agents, Including Intracranial Metastases

Clinical cancer research, 2013-07, Vol.19 (13), p.3520-3532

2013

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Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors

Journal of medicinal chemistry, 2010-03, Vol.53 (5), p.2171-2187

2010

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Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death

Discovery of 2‑[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro‑1H‑isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP‑1 Inhibitor for Cancer Therapy

PARP inhibitors in cancer therapy: an update

3-Aminopyrazole Inhibitors of CDK2/Cyclin A as Antitumor Agents. 1. Lead Finding

Optimization of 6,6-dimethyl pyrrolo[3,4- c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing

The target landscape of clinical kinase drugs

Dimer Formation through Domain Swapping in the Crystal Structure of the Grb2-SH2−Ac-pYVNV Complex

Stereoselective synthesis of 3,4‐dihydropyrrolo[1,2‐a]pyrazin‐1(2H)‐one derivatives as PIM kinase inhibitors inspired from marine alkaloids

Stereoselective synthesis of 3,4‐dihydropyrrolopyrazin‐1(2H)‐one derivatives as PIM kinase inhibitors inspired from marine alkaloids

Around the Black Box: Applying the Carltona Principle to Challenge Machine Learning Algorithms in Public Sector Decision-Making

Alkylsulfanyl-1,2,4-triazoles, a New Class of Allosteric Valosine Containing Protein Inhibitors. Synthesis and Structure–Activity Relationships

Identification of unprecedented ATP-competitive choline kinase inhibitors

Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors

Discovery of Stereospecific PARP‑1 Inhibitor Isoindolinone NMS-P515

Crystal structure of the T315I abl mutant in complex with the aurora kinases inhibitor PHA-739358

Abstract 4790: Identification and characterization of ATP-mimetic choline kinase inhibitors

Structural Insight into Maternal Embryonic Leucine Zipper Kinase (MELK) Conformation and Inhibition toward Structure-Based Drug Design

Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases

Abstract 5163: Characterization of NMS-E194, a selective and potent PERK inhibitor with efficacy in the KMS-11 multiple myeloma

Abstract 2082: NMS-E668, a potent and selective RET kinase inhibitor characterized by specificity towards VEGFR2 and high antitumor efficacy against RET-driven models

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90)

NMS-E973, a Novel Synthetic Inhibitor of Hsp90 with Activity against Multiple Models of Drug Resistance to Targeted Agents, Including Intracranial Metastases

Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors

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