NME digest

D Navarro, R Castaner… - Drugs of the Future, 2015 - access.portico.org
NME Digest highlights new, biologically active molecules revealed for the first time in current
literature, at congresses and in company communications that are identified by a code …

Identification of potent and selective small molecule inhibitors of the cation channel TRPM4

LC Ozhathil, C Delalande, B Bianchi… - British journal of …, 2018 - Wiley Online Library
Background and Purpose TRPM4 is a calcium‐activated non‐selective cation channel
expressed in many tissues and implicated in several diseases, and has not yet been …

Medicinal chemistry perspective of TRPM2 channel inhibitors: where we are and where we might be heading?

H Zhang, S Zhao, J Yu, W Yang, Z Liu, L Zhang - Drug Discovery Today, 2020 - Elsevier
Highlights•The structures and gating mechanisms of the TRPM2 channel are outlined.•The
reported TRPM2 inhibitors and their inhibitory properties are summarized.•The therapeutic …

Development and validation of a secondary screening assay for TRPM8 antagonists using QPatch HT

EJ Beck, TL Hutchinson, N Qin… - Assay and drug …, 2010 - liebertpub.com
QPatch HT is an automated patch clamp system with high data quality/content and greatly
increased throughput over conventional patch clamp methods. To determine whether this …

In Vitro and In Vivo Pharmacological Characterization of a Novel TRPM8 Inhibitor Chemotype Identified by Small-Scale Preclinical Screening

N Iraci, C Ostacolo, A Medina-Peris, T Ciaglia… - International Journal of …, 2022 - mdpi.com
Transient receptor potential melastatin type 8 (TRPM8) is a target for the treatment of
different physio-pathological processes. While TRPM8 antagonists are reported as potential …

[HTML][HTML] Identification of positive modulators of TRPM5 channel from a high-throughput screen using a fluorescent membrane potential assay

C Virginio, L Aldegheri, S Nola, D Brodbeck, L Brault… - SLAS Discovery, 2022 - Elsevier
Abstract Transient Receptor Potential Melastatin 5 (TRPM5) is an intracellular calcium-
activated cation-selective ion channel expressed in a variety of cell types. Dysfunction of this …

The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1, 2, 3, 4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human …

M Sabat, LF Raveglia, L Aldegheri, A Barilli… - Bioorganic & Medicinal …, 2022 - Elsevier
This publication details the discovery of a series of selective transient receptor potential
cation channel subfamily M member 5 (TRPM5) agonists culminating with the identification …

Design, synthesis and biological activities of 2, 3-dihydroquinazolin-4 (1H)-one derivatives as TRPM2 inhibitors

H Zhang, H Liu, X Luo, Y Wang, Y Liu, H Jin… - European Journal of …, 2018 - Elsevier
Transient receptor potential melastatin 2 (TRPM2), a Ca 2+-permeable cationic channel,
plays critical roles in insulin release, cytokine production, body temperature regulation and …

The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists

JM Matthews, N Qin, RW Colburn, SL Dax… - Bioorganic & medicinal …, 2012 - Elsevier
A series of benzothiophene-based phosphonates was synthesized and many analogs within
the series were shown to be potent antagonists of the TRPM8 channel. The compounds …

Synthesis, high-throughput screening and pharmacological characterization of β–lactam derivatives as TRPM8 antagonists

R de la Torre-Martínez, MA Bonache… - Scientific reports, 2017 - nature.com
The mammalian transient receptor potential melastatin channel 8 (TRPM8), highly
expressed in trigeminal and dorsal root ganglia, mediates the cooling sensation and plays …