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Recent Developments in Fragment-Based Drug Discovery

Journal of medicinal chemistry, 2008-07, Vol.51 (13), p.3661-3680

2008

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From fragment to clinical candidate—a historical perspective

Drug discovery today, 2009-07, Vol.14 (13), p.668-675

2009

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Fragment-to-Lead Medicinal Chemistry Publications in 2022

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2287-2304

2024

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Protein engineering enables a soakable crystal form of human CDK7 primed for high-throughput crystallography and structure-based drug design

Structure (London), 2024-08, Vol.32 (8), p.1040-1048.e3

2024

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Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function

Nature chemical biology, 2012-11, Vol.8 (11), p.920-925

2012

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Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency

Journal of medicinal chemistry, 2010-08, Vol.53 (16), p.5942-5955

2010

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Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

Journal of medicinal chemistry, 2005-01, Vol.48 (2), p.414-426

2005

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Relationship Between Diabetic Variables and Outcomes After Coronary Artery Bypass Grafting in Diabetic Patients

Heart, lung & circulation, 2017-04, Vol.26 (4), p.371-375

2017

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Masseter muscle rigidity and the role of DNA analysis to confirm malignant hyperthermia susceptibility

Anaesthesia and intensive care, 2019-01, Vol.47 (1), p.60-68

2019

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Fragment-to-Lead Medicinal Chemistry Publications in 2021

Journal of medicinal chemistry, 2023-01, Vol.66 (2), p.1137-1156

2023

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Meaningful co-production to bring meaningful change: Developing the Allied Health Professionals Dementia Framework for Wales together

Dementia (London, England), 2024-07, Vol.23 (5), p.724-740

2024

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Abstract A142: Fragment based discovery of inhibitors of the eIF4E:eIF4G interaction

Molecular cancer therapeutics, 2023-12, Vol.22 (12_Supplement), p.A142-A142

2023

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Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase‑2 (SHP2)

Journal of medicinal chemistry, 2024-03, Vol.67 (6), p.4655-4675

2024

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Abstract A143: Coupling fragment-based screening with targeted protein degradation and genetic rescue to identify and explore the function of a non-canonical pocket on eIF4E

Molecular cancer therapeutics, 2023-12, Vol.22 (12_Supplement), p.A143-A143

2023

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Abstract 3722: Exploring the role of eIF4E in cancer cells with targeted protein degradation

Cancer research (Chicago, Ill.), 2023-04, Vol.83 (7_Supplement), p.3722-3722

2023

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Abstract 5902: Targeting MAPK-driven tumors via inhibition of MAP2K4

Cancer research (Chicago, Ill.), 2024-03, Vol.84 (6_Supplement), p.5902-5902

2024

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Abstract 7073: Integrating fragment-based crystallographic screening with dTAG-PROTAC degradation and genetic rescue to explore the function of eIF4E

Cancer research (Chicago, Ill.), 2024-03, Vol.84 (6_Supplement), p.7073-7073

2024

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Abstract A110: Identifying sensitive patient populations for CDK7 inhibitors using cell panel screens and bioinformatic approaches

Molecular cancer therapeutics, 2023-12, Vol.22 (12_Supplement), p.A110-A110

2023

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Revision rates after primary hip and knee replacement in England between 2003 and 2006

PLoS medicine, 2008-09, Vol.5 (9), p.e179-e179

2008

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Identification of novel allosteric inhibitors through fragment-based drug discovery and X-ray crystallography

Acta crystallographica. Section A, Foundations and advances, 2015-08, Vol.71 (a1), p.s38-s38

2015

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Abstract A211: Fragment-based drug discovery of the synthetic small molecule HSP90 inhibitor AT13387

Molecular cancer therapeutics, 2009-12, Vol.8 (12_Supplement), p.A211-A211

2009

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Recent Developments in Fragment-Based Drug Discovery

From fragment to clinical candidate—a historical perspective

Fragment-to-Lead Medicinal Chemistry Publications in 2022

Protein engineering enables a soakable crystal form of human CDK7 primed for high-throughput crystallography and structure-based drug design

Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design

Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function

Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency

Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

Relationship Between Diabetic Variables and Outcomes After Coronary Artery Bypass Grafting in Diabetic Patients

Masseter muscle rigidity and the role of DNA analysis to confirm malignant hyperthermia susceptibility

Fragment-to-Lead Medicinal Chemistry Publications in 2021

Meaningful co-production to bring meaningful change: Developing the Allied Health Professionals Dementia Framework for Wales together

Abstract A142: Fragment based discovery of inhibitors of the eIF4E:eIF4G interaction

Fragment-Based Discovery of Allosteric Inhibitors of SH2 Domain-Containing Protein Tyrosine Phosphatase‑2 (SHP2)

Fragment-Based Discovery of a Series of Allosteric-Binding Site Modulators of β‑Glucocerebrosidase

Abstract A143: Coupling fragment-based screening with targeted protein degradation and genetic rescue to identify and explore the function of a non-canonical pocket on eIF4E

Abstract 3722: Exploring the role of eIF4E in cancer cells with targeted protein degradation

Abstract 5902: Targeting MAPK-driven tumors via inhibition of MAP2K4

Abstract 7073: Integrating fragment-based crystallographic screening with dTAG-PROTAC degradation and genetic rescue to explore the function of eIF4E

Abstract A110: Identifying sensitive patient populations for CDK7 inhibitors using cell panel screens and bioinformatic approaches

Revision rates after primary hip and knee replacement in England between 2003 and 2006

Identification of novel allosteric inhibitors through fragment-based drug discovery and X-ray crystallography

Abstract A211: Fragment-based drug discovery of the synthetic small molecule HSP90 inhibitor AT13387

Identification of N -(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1 H -pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

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