Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling

Setmelanotide: First Approval

(2021) Anthony Markham   DRUGS

Structural basis of ligand recognition and self-activation of orphan GPR52

(2020) Xi Lin et al.   NATURE

Effect of setmelanotide, a melanocortin‐4 receptor agonist, on obesity in Bardet‐Biedl syndrome

(2020) Robert Haws et al.   DIABETES OBESITY & METABOLISM

Structure of a D2 dopamine receptor–G-protein complex in a lipid membrane

(2020) Jie Yin et al.   NATURE

Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor

(2020) Kuglae Kim et al.   CELL

Alanine Scanning Mutagenesis of the DRYxxI Motif and Intracellular Loop 2 of Human Melanocortin-4 Receptor

(2020) Li-Kun Yang et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Efficacy and safety of setmelanotide, an MC4R agonist, in individuals with severe obesity due to LEPR or POMC deficiency: single-arm, open-label, multicentre, phase 3 trials

(2020) Karine Clément et al.   Lancet Diabetes & Endocrinology

Crystal Structure of the Human Cannabinoid Receptor CB2

(2019) Xiaoting Li et al.   CELL

Structure of a Signaling Cannabinoid Receptor 1-G Protein Complex

(2019) Kaavya Krishna Kumar et al.   CELL

Obesity: global epidemiology and pathogenesis

(2019) Matthias Blüher   Nature Reviews Endocrinology

Human Gain-of-Function MC4R Variants Show Signaling Bias and Protect against Obesity

(2019) Luca A. Lotta et al.   CELL

Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes

(2019) Shoji Maeda et al.   SCIENCE

Automated cryo-EM structure refinement using correlation-driven molecular dynamics

(2019) Maxim Igaev et al.   eLife

Illuminating G-Protein-Coupling Selectivity of GPCRs

(2019) Asuka Inoue et al.   CELL

Macromolecular structure determination using X-rays, neutrons and electrons: recent developments in Phenix

(2019) Dorothee Liebschner et al.   Acta Crystallographica Section D-Structural Biology

The constitutive activity of melanocortin‐4 receptors in cAMP pathway is allosterically modulated by zinc and copper ions

(2019) Reet Link et al.   JOURNAL OF NEUROCHEMISTRY

MC4R agonism promotes durable weight loss in patients with leptin receptor deficiency

(2018) Karine Clément et al.   NATURE MEDICINE

MC4R Agonists: Structural Overview on Antiobesity Therapeutics

(2018) Juliana Pereira Lopes Gonçalves et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Real-space refinement in PHENIX for cryo-EM and crystallography

(2018) Pavel V. Afonine et al.   Acta Crystallographica Section D-Structural Biology

Structure of the µ-opioid receptor–Gi protein complex

(2018) Antoine Koehl et al.   NATURE

Development of an antibody fragment that stabilizes GPCR/G-protein complexes

(2018) Shoji Maeda et al.   Nature Communications

New tools for automated high-resolution cryo-EM structure determination in RELION-3

(2018) Jasenko Zivanov et al.   eLife

MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopy

(2017) Shawn Q Zheng et al.   NATURE METHODS

Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency

(2017) Tinh-Hai Collet et al.   Molecular Metabolism

CHARMM-GUI Input Generator for NAMD, Gromacs, Amber, Openmm, and CHARMM/OpenMM Simulations using the CHARMM36 Additive Force Field

(2016) Jumin Lee et al.   BIOPHYSICAL JOURNAL

Structure of the adenosine A2A receptor bound to an engineered G protein

(2016) Byron Carpenter et al.   NATURE

Proopiomelanocortin Deficiency Treated with a Melanocortin-4 Receptor Agonist

(2016) Peter Kühnen et al.   NEW ENGLAND JOURNAL OF MEDICINE

Gq/11α and Gsα mediate distinct physiological responses to central melanocortins

(2015) Yong-Qi Li et al.   JOURNAL OF CLINICAL INVESTIGATION

CTFFIND4: Fast and accurate defocus estimation from electron micrographs

(2015) Alexis Rohou et al.   JOURNAL OF STRUCTURAL BIOLOGY

G-protein-independent coupling of MC4R to Kir7.1 in hypothalamic neurons

(2015) Masoud Ghamari-Langroudi et al.   NATURE

A neural basis for melanocortin-4 receptor–regulated appetite

(2015) Alastair S Garfield et al.   NATURE NEUROSCIENCE

Intracellular signaling mechanisms of the melanocortin receptors: current state of the art

(2014) Adriana R. Rodrigues et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

MC4R-expressing glutamatergic neurons in the paraventricular hypothalamus regulate feeding and are synaptically connected to the parabrachial nucleus

(2014) B. P. Shah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protein and ligand preparation: parameters, protocols, and influence on virtual screening enrichments

(2013) G. Madhavi Sastry et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

Structure of the CCR5 Chemokine Receptor-HIV Entry Inhibitor Maraviroc Complex

(2013) Q. Tan et al.   SCIENCE

Anhedonia requires MC4R-mediated synaptic adaptations in nucleus accumbens

(2012) Byung Kook Lim et al.   NATURE

Functional studies on twenty novel naturally occurring melanocortin-4 receptor mutations

(2011) Zhi-Qiang Wang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Melanocortin-4 Receptors Expressed by Cholinergic Neurons Regulate Energy Balance and Glucose Homeostasis

(2011) Jari Rossi et al.   Cell Metabolism

From brain to food: Analysis of phosphatidylcholins, lyso-phosphatidylcholins and phosphatidylcholin–plasmalogens derivates in Alzheimer's disease human post mortem brains and mice model via mass spectrometry

(2011) Marcus O.W. Grimm et al.   JOURNAL OF CHROMATOGRAPHY A

OPM database and PPM web server: resources for positioning of proteins in membranes

(2011) Mikhail A. Lomize et al.   NUCLEIC ACIDS RESEARCH

Pharmacological Characterization of 30 Human Melanocortin-4 Receptor Polymorphisms with the Endogenous Proopiomelanocortin-Derived Agonists, Synthetic Agonists, and the Endogenous Agouti-Related Protein Antagonist,‡

(2010) Zhimin Xiang et al.   BIOCHEMISTRY

Applications of the Restriction Free (RF) cloning procedure for molecular manipulations and protein expression

(2010) Tamar Unger et al.   JOURNAL OF STRUCTURAL BIOLOGY

electronic Ligand Builder and Optimization Workbench(eLBOW): a tool for ligand coordinate and restraint generation

(2009) Nigel W. Moriarty et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

MolProbity: all-atom structure validation for macromolecular crystallography

(2009) Vincent B. Chen et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Functional characterization and pharmacological rescue of melanocortin-4 receptor mutations identified from obese patients

(2009) Zhen-Chuan Fan et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Prevalence of Melanocortin-4 Receptor Deficiency in Europeans and Their Age-Dependent Penetrance in Multigenerational Pedigrees

(2008) F. Stutzmann et al.   DIABETES