Detalhe da pesquisa
1.
From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell
; 184(24): 5886-5901.e22, 2021 11 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-34822784
2.
Impact of GPCR Structures on Drug Discovery.
Cell
; 181(1): 81-91, 2020 04 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-32243800
3.
Accurate structure prediction of biomolecular interactions with AlphaFold 3.
Nature
; 2024 May 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-38718835
4.
Crystal structure of the GLP-1 receptor bound to a peptide agonist.
Nature
; 546(7657): 254-258, 2017 06 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-28562585
5.
Corrigendum: Crystal structure of the GLP-1 receptor bound to a peptide agonist.
Nature
; 548(7665): 122, 2017 08 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-28700581
6.
Intracellular allosteric antagonism of the CCR9 receptor.
Nature
; 540(7633): 462-465, 2016 12 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27926729
7.
Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M1 -acetylcholine receptor agonist: A randomized cross-over trial.
Br J Clin Pharmacol
; 87(11): 4439-4449, 2021 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-33891333
8.
First-in-man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1 -receptor partial agonist for the treatment of dementias.
Br J Clin Pharmacol
; 87(7): 2945-2955, 2021 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-33351971
9.
Accurate Prediction of GPCR Ligand Binding Affinity with Free Energy Perturbation.
J Chem Inf Model
; 60(11): 5563-5579, 2020 11 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-32539374
10.
X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A2A Adenosine Receptor Antagonists.
Angew Chem Int Ed Engl
; 59(38): 16536-16543, 2020 09 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-32542862
11.
Identification of a novel allosteric GLP-1R antagonist HTL26119 using structure- based drug design.
Bioorg Med Chem Lett
; 29(20): 126611, 2019 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31447084
12.
Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound ß1-Adrenergic Receptor.
Mol Pharmacol
; 88(6): 1024-34, 2015 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-26385885
13.
Structure-based drug design for G protein-coupled receptors.
Prog Med Chem
; 53: 1-63, 2014.
Artigo
em Inglês
| MEDLINE | ID: mdl-24418607
14.
A phase 1b/2a multicenter study of the safety and preliminary pharmacodynamic effects of selective muscarinic M1 receptor agonist HTL0018318 in patients with mild-to-moderate Alzheimer's disease.
Alzheimers Dement (N Y)
; 8(1): e12273, 2022.
Artigo
em Inglês
| MEDLINE | ID: mdl-35229025
15.
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
ACS Med Chem Lett
; 13(11): 1776-1782, 2022 Nov 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-36385934
16.
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
ACS Chem Neurosci
; 13(6): 751-765, 2022 03 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-35245037
17.
Acetylcholine prioritises direct synaptic inputs from entorhinal cortex to CA1 by differential modulation of feedforward inhibitory circuits.
Nat Commun
; 12(1): 5475, 2021 09 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-34531380
18.
Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study.
Alzheimers Res Ther
; 13(1): 87, 2021 04 21.
Artigo
em Inglês
| MEDLINE | ID: mdl-33883008
19.
Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors.
J Med Chem
; 63(3): 905-927, 2020 02 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-31577440
20.
Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
J Med Chem
; 63(14): 7906-7920, 2020 07 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-32558564