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This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins.

Table of Contents

Section I-- Identification and Measurement of Constitutive Activity



Constitutive activity at the cannabinoid CB1 receptor and behavioral responses
Katherine E. Hanlon and Todd W. Vanderah

Detecting constitutive activity and protean agonism at the cannabinoid-2 receptor.
Massimiliano Beltramo, Rossella Brusa, Isabella Mancini, Paola Scandroglio, Massimiliano. Beltramo

Modulation of constitutive activity of the ghrelin receptor by use of pharmacological tools as well as mutagenesis
Birgitte Holst and Jacek Mokrosiński

Assessment of constitutive activity and internalization of GPR54 (Kiss1-r).
Macarena Pampillo and Andy Videsh Babwah

Assessment of Constitutive Activity in EP Prostanoid Receptors
Hiromichi Fujino, Toshihiko Murayama, and John W. Regan

α1D-Adrenergic receptors: constitutive activity and reduced expression at the plasma membrane
J Adolfo Garcia-Sáinz, M. Teresa Romero-Ávila and Luz del Carmen Medina

Constitutive activity of the histamine H1 receptor
Saskia Nijmeijer, Rob Leurs and Henry F Vischer

Constitutive activity of somatostatin receptor subtypes
Anat Ben-Shlomo, Kolja Wawrowsky and Shlomo Melmed

Assessment of homologous internalization of constitutively active N111G mutant of AT1 receptor
Mohiuddin Ahmed Bhuiyan and Takafumi Nagatomo

Methods to detect cell surface expression and constitutive activity of GPR6
Balakrishna M. Prasad, Bettye Hollins and Nevin A. Lambert

β3-adrenoceptor agonists and (antagonists as) inverse agonists: history, perspective, constitutive activity and stereospecific binding.
Maria Grazia Perrone and Antonio Scilimati

Constitutive Activity of the Lutropin Receptor and its Allosteric Modulation by Receptor Heterodimerization
Deborah L. Segaloff

Assessing Constitutive Activity of Extracellular Calcium-Sensing Receptors in Vitro and in Bone
Wenhan Chang, Melita Dvorak, and Dolores Shoback

Constitutive Activity of Neural Melanocortin Receptors.
Ya-Xiong Tao, Hui Huang, Zhi-Qiang Wang, Fan Yang, Jessica N. Williams, and Gregory V. Nikiforovich

Measurement of Constitutive Activity of BMP Type I receptors
Peter ten Dijke

Probing the CA among dopamine D1 and D5 receptors and their mutants
Bianca Plouffe, Jean-Philippe D’Aoust, Vincent Laquerre, Binhui Liang and Mario Tiberi

Identification of Gain-of-Function Variants of the Human Prolactin Receptor
Vincent Goffin, Roman L. Bogorad, and Philippe Touraine

Investigations of Activated ACVR1/ALK2, a Bone Morphogenetic Protein (BMP) Type I Receptor that Causes Fibrodysplasia Ossificans Progressiva
Frederick. Kaplan, Petra Seemann, Julia Haupt, Meiqi Xu, Vitali Lounev, Mary Mullins, Eileen M. Shore

Identification and evaluation of constitutively active thyroid stimulating hormone receptor mutations
Joaquin Lado-Abeal, Leah R. Quisenberry, and Isabel Castro-Piedras

Assessment of constitutive activity of a G protein-coupled receptor, Cpr2, in Cryptococcus neoformans by heterologous and homologous methods
Chaoyang Xue, Yina Wang, and Yen-Ping Hsueh

In vitro and in vivo assessment of mu opioid receptor constitutive activity.
Edward J. Bilsky, Denise Giuvelis, Melissa D. Osborn, Christina M. Dersch, Heng Xu and Richard B. Rothman

Constitutively active µ-opioid methods
Mark. Connor and John Traynor

Protein Kinase Ck2 is a Constitutively-Active Enzyme That Promotes Cell Survival: Strategies To Identify Ck2 Substrates and Manipulate Its Activity In Mammalian Cells
Jacob P. Turowec, James S. Duncan, Ashley C. French, Laszlo Gyenis, Nicole A. St. Denis, Greg J. Vilk, and David W. Litchfield

Assessment of Ck2 Constitutive Activity In Cancer Cells
Maria Ruzzene, Giovanni Di Maira, Kendra Tosoni, and Lorenzo A. Pinna

Structural basis of the constitutive activity of protein kinase CK2
Birgitte B. Olsen, Barbara Guerra, Karsten Niefind and Olar-Georg Issinger font error

Measuring the Constitutive Activation of c-Jun N-terminal Kinase Isoforms
Ryan T. Nitta, Shawn S. Badal, and Albert J. Wong

Measurement of constitutive MAPK and PI3K/AKT signaling activity in human cancer cell lines.
Keiran S.M. Smalley

Constitutive activity of GPR40/FFA1: Intrinsic or assay dependent?
Leigh A Stoddart and Graeme Milligan

Constitutive activity of TRP channels: methods for measuring the activity and its outcome
Baruch Minke

Measurement of Orexin (Hypocretin) and Substance P Effects On Constitutively Active Inward Rectifier K+ Channels in Brain Neurons
Yasuko Nakajima and Shigehiro Nakajima

Characterization of G protein receptor kinase 4 and measuring its constitutive activity in vivo
Bradley T. Andresen

Voltage-clamp based methods for the detection of constitutively active acetylcholine-gated IK,ACh channels in the diseased heart
Niels Voigt, Samy Makary, Stanley Nattel, Dobromir Dobrev

Assaying Wave and WASH complex constitutive activities towards the Arp2/3 complex.

Emmanuel DERIVERY and Alexis GAUTREAU