User profiles for A. C. Kruse

Andrew C. Kruse

Professor of Biological Chemistry and Molecular Pharmacology, Harvard Medical School
Verified email at hms.harvard.edu
Cited by 19571

[HTML][HTML] Muscarinic acetylcholine receptors: novel opportunities for drug development

AC Kruse, BK Kobilka, D Gautam, PM Sexton… - Nature reviews Drug …, 2014 - nature.com
… This latter study is of particular relevance because TBPB, together with other novel M 1
receptor-selective agonists such as AC-42 and 77-LH-28-1, was originally classified as an …

Structural basis for G protein-coupled receptor activation

A Manglik, AC Kruse - Biochemistry, 2017 - ACS Publications
G protein-coupled receptors (GPCRs) are critical regulators of human physiology and make
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …

The molecular function of σ receptors: past, present, and future

HR Schmidt, AC Kruse - Trends in pharmacological sciences, 2019 - cell.com
The σ 1 and σ 2 receptors are enigmatic proteins that have attracted attention for decades
due to the chemical diversity and therapeutic potential of their ligands. However, despite …

Crystal structure of the β2 adrenergic receptor–Gs protein complex

SGF Rasmussen, BT DeVree, Y Zou, AC Kruse… - Nature, 2011 - nature.com
… The subunits regulate their respective effector proteins adenylyl cyclase (AC) and Ca 2+
channels. The Gs heterotrimer reassembles from α and βγ subunits following hydrolysis of GTP …

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

A Manglik, AC Kruse, TS Kobilka, FS Thian… - Nature, 2012 - nature.com
Opium is one of the world’s oldest drugs, and its derivatives morphine and codeine are among
the most used clinical drugs to relieve severe pain. These prototypical opioids produce …

Structure and dynamics of the M3 muscarinic acetylcholine receptor

AC Kruse, J Hu, AC Pan, DH Arlow, DM Rosenbaum… - Nature, 2012 - nature.com
Acetylcholine, the first neurotransmitter to be identified 1 , exerts many of its physiological
actions via activation of a family of G-protein-coupled receptors (GPCRs) known as muscarinic …

Activation and allosteric modulation of a muscarinic acetylcholine receptor

AC Kruse, AM Ring, A Manglik, J Hu, K Hu, K Eitel… - Nature, 2013 - nature.com
Despite recent advances in crystallography and the availability of G-protein-coupled receptor
(GPCR) structures, little is known about the mechanism of their activation process, as only …

Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist

K Haga, AC Kruse, H Asada, T Yurugi-Kobayashi… - Nature, 2012 - nature.com
The parasympathetic branch of the autonomic nervous system regulates the activity of multiple
organ systems. Muscarinic receptors are G-protein-coupled receptors that mediate the …

Structure of the δ-opioid receptor bound to naltrindole

S Granier, A Manglik, AC Kruse, TS Kobilka, FS Thian… - Nature, 2012 - nature.com
The opioid receptor family comprises three members, the µ-, δ- and κ-opioid receptors,
which respond to classical opioid alkaloids such as morphine and heroin as well as to …

Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody

AM Ring, A Manglik, AC Kruse, MD Enos, WI Weis… - Nature, 2013 - nature.com
… Nanobodies were cloned into the periplasmic expression vector pET26b, containing an N-terminal
signal sequence and a C-terminal 8× histidine tag, and transformed into BL21(DE3) …