[HTML][HTML] Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease
…, SP Jones, A Keeley, GM Keserü, HF Klein… - Nature …, 2020 - nature.com
COVID-19, caused by SARS-CoV-2, lacks effective therapeutics. Additionally, no antiviral
drugs or vaccines were developed against the closely related coronavirus, SARS-CoV-1 or …
drugs or vaccines were developed against the closely related coronavirus, SARS-CoV-1 or …
[HTML][HTML] Escape from planarity in fragment-based drug discovery: A synthetic strategy analysis of synthetic 3D fragment libraries
HF Klein, DJ Hamilton, IJP de Esch, M Wijtmans… - Drug discovery today, 2022 - Elsevier
In fragment-based drug discovery (FBDD), there is a developing appreciation that 3D fragments
could offer opportunities that are not provided by 2D fragments. This review provides an …
could offer opportunities that are not provided by 2D fragments. This review provides an …
[HTML][HTML] Design and Synthesis of 56 Shape‐Diverse 3D Fragments
TD Downes, SP Jones, HF Klein… - … (Weinheim an der …, 2020 - ncbi.nlm.nih.gov
Fragment‐based drug discovery is now widely adopted for lead generation in the pharmaceutical
industry. However, fragment screening collections are often predominantly populated …
industry. However, fragment screening collections are often predominantly populated …
Escape from planarity in fragment-based drug discovery: A physicochemical and 3D property analysis of synthetic 3D fragment libraries
DJ Hamilton, T Dekker, HF Klein, GV Janssen… - Drug Discovery Today …, 2020 - Elsevier
Fragment-based drug discovery (FBDD) has grown into a well-established approach in the
pursuit of new therapeutics. Key to the success of FBDD is the low molecular complexity of …
pursuit of new therapeutics. Key to the success of FBDD is the low molecular complexity of …
Puckering the Planar Landscape of Fragments: Design and Synthesis of a 3D Cyclobutane Fragment Library
…, J Elsayed, REM Huiberts, HF Klein… - …, 2022 - Wiley Online Library
Fragment‐based drug discovery (FBDD) has a growing need for unique screening libraries.
The cyclobutane moiety was identified as an underrepresented yet attractive three‐…
The cyclobutane moiety was identified as an underrepresented yet attractive three‐…
Latent warheads for targeted cancer therapy: Design and synthesis of pro-pyrrolobenzodiazepines and conjugates
…, F You, JF Vaughn, SJ Hahn, HF Klein… - Bioconjugate …, 2017 - ACS Publications
Pyrrolobenzodiazepines (PBDs) and their dimers (bis-PBDs) have emerged as some of the
most potent chemotherapeutic compounds, and are currently under development as novel …
most potent chemotherapeutic compounds, and are currently under development as novel …
Design and synthesis of a folate-receptor targeted diazepine-ring-opened pyrrolobenzodiazepine prodrug conjugate
…, K Wang, F You, JF Vaughn, SJ Hahn, HF Klein… - Bioorganic & Medicinal …, 2020 - Elsevier
Pyrrolobenzodiazepines (PBDs) and their dimers (bis-PBDs) have emerged as some of the
most potent chemotherapeutic compounds and are currently under development as novel …
most potent chemotherapeutic compounds and are currently under development as novel …
[HTML][HTML] Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors
EA FitzGerald, D Vagrys, G Opassi, HF Klein… - SLAS Discovery, 2024 - Elsevier
Surface plasmon resonance (SPR) biosensor methods are ideally suited for fragment-based
lead discovery. However, generally applicable experimental procedures and detailed …
lead discovery. However, generally applicable experimental procedures and detailed …
Design and Synthesis of 56 Shape Diverse 3-D Fragments
P O'Brien, TD Downes, SP Jones, HF Klein… - … : A European Journal, 2020 - pure.york.ac.uk
Fragment-based drug discovery is now widely adopted for lead generation in the pharmaceutical
industry. However, fragment screening collections are often predominantly populated …
industry. However, fragment screening collections are often predominantly populated …
Hyponatraemia, hypothyroidism, and role of arginine-vasopressin
FWF Hanna, MF Scanlon - The Lancet, 1997 - thelancet.com
Hyponatraemia is well recognised in hypothyroidism, especially in the severe forms. The
hypothyroidism is usually primary, but there are reports of hyponatraemia in patients with …
hypothyroidism is usually primary, but there are reports of hyponatraemia in patients with …