Therapeutic options for targeting inflammatory osteoarthritis pain

PG Conaghan, AD Cook, JA Hamilton… - Nature Reviews …, 2019 - nature.com
Pain is the major symptom of osteoarthritis (OA) and is an important factor in strategies to
manage this disease. However, the current standard of care does not provide satisfactory …

[HTML][HTML] High-affinity TrkA and p75 neurotrophin receptor complexes: A twisted affair

JN Conroy, EJ Coulson - Journal of Biological Chemistry, 2022 - Elsevier
Neurotrophin signaling is essential for normal nervous system development and adult
function. Neurotrophins are secreted proteins that signal via interacting with two …

Allosteric modulator discovery: from serendipity to structure-based design

S Lu, X He, D Ni, J Zhang - Journal of medicinal chemistry, 2019 - ACS Publications
Allosteric modulators bound to structurally diverse allosteric sites can achieve better
pharmacological advantages than orthosteric ligands. The discovery of allosteric …

Peripheral voltage-gated cation channels in neuropathic pain and their potential as therapeutic targets

SRA Alles, PA Smith - Frontiers in Pain Research, 2021 - frontiersin.org
The persistence of increased excitability and spontaneous activity in injured peripheral
neurons is imperative for the development and persistence of many forms of neuropathic …

Neuropathic pain; what we know and what we should do about it

PA Smith - Frontiers in Pain Research, 2023 - frontiersin.org
Neuropathic pain can result from injury to, or disease of the nervous system. It is notoriously
difficult to treat. Peripheral nerve injury promotes Schwann cell activation and invasion of …

Small-molecule kinase inhibitors for the treatment of nononcologic diseases

Z ** small-molecule kinase inhibitors as
anticancer therapeutic agents. However, kinase deregulation plays essential roles not only …

Protein–ligand binding affinity prediction of cyclin‐dependent kinase‐2 inhibitors by dynamically averaged fragment molecular orbital‐based interaction energy

K Takaba, C Watanabe, A Tokuhisa… - Journal of …, 2022 - Wiley Online Library
Fragment molecular orbital (FMO) method is a powerful computational tool for structure‐
based drug design, in which protein–ligand interactions can be described by the inter …

Selective halogenation of pyridines using designed phosphine reagents

JN Levy, JV Alegre-Requena, R Liu… - Journal of the …, 2020 - ACS Publications
Halopyridines are key building blocks for synthesizing pharmaceuticals, agrochemicals, and
ligands for metal complexes, but strategies to selectively halogenate pyridine C–H …

Type II & III inhibitors of tropomyosin receptor kinase (Trk): a 2020–2022 patent update

P Iliev, C Jaworski, C Wängler, B Wängler… - Expert Opinion on …, 2024 - Taylor & Francis
ABSTRACT Introduction The Trk family proteins are membrane-bound kinases
predominantly expressed in neuronal tissues. Activated by neurotrophins, they regulate …

TRK xDFG mutations trigger a sensitivity switch from type I to II kinase inhibitors

E Cocco, JE Lee, S Kannan, AM Schram… - Cancer …, 2021 - aacrjournals.org
On-target resistance to next-generation TRK inhibitors in TRK fusion–positive cancers is
largely uncharacterized. In patients with these tumors, we found that TRK xDFG mutations …