I. SCOPE AND METHODOLOGY
II. REPORT SYNOPSIS
1. Introduction
Agonist
Antagonist
GEFs (Guanine Nucleotide Exchange Factor)
Receptor Regulation
Receptor Desensitization
Ras SuperFamily
GPCR
Products of GPCR and Profiling Services
GPCRs as Drug Targets
Cell Surface Receptor Expression of a High Order
Functionally Oriented GPCR
The Purpose of GPCR Profiling
The Speeding Up of Successful Drug Discovery
Secondary and Custom Assay Services
Advantages
History of GPCR
Other Receptors
G-Protein
History of G-Proteins
Segmentation of GPCR – Drug Targets
Exhibit 1: Segmentation of Global GPCR –Drug Targets Market by GPCR Families (Rhodopsin, Secretin,
Glutamate and Other) and by type of Ligands Targeting GPCRs (Peptides or Proteins
including enzymes, Biogenic Amines, Lipids and Other)
2. Global Market Analysis
Exhibit 2: GPCR – Drug Targets - Global Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Analysis by GPCR Family Type
Rhodopsin
Exhibit 3: Rhodopsin - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 4: Rhodopsin - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Secretin
Exhibit 5: Secretin - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 6: Secretin - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Glutamate
Exhibit 7: Glutamate - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 8: Glutamate - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Other
Exhibit 9: Other - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 10: Other - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Analysis by Ligands Targeting GPCR
Peptides or Proteins
Exhibit 11: Peptides or Proteins - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 12: Peptides or Proteins - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Biogenic Amines
Exhibit 13: Biogenic Amines - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 14: Biogenic Amines - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Lipids
Exhibit 15: Lipids - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 16: Lipids - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Other
Exhibit 17: Other - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 18: Other - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
Exhibit 19: List of Major Global Companies
3. Regional Market Analysis
United States
Exhibit 20: GPCR - Drug Targets - United States Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Europe
Exhibit 21: GPCR - Drug Targets - European Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Japan
Exhibit 22: GPCR - Drug Targets - Japanese Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Asia-Pacific
Exhibit 23: GPCR - Drug Targets - Asia-Pacific Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Rest of World
Exhibit 24: GPCR - Drug Targets - Rest of World Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
III. MARKET DYNAMICS
Market Overview
1. Global Market Analysis
Global Pharmaceuticals Market
Exhibit 25: Pharmaceuticals - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 26: Pharmaceuticals - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
2. GPCR-Drug Targets
Exhibit 27: GPCRs- Drug Targets - Global Value Market Estimations & Predictions (2005 -2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World in US$ Billion (Graphical Representation Included)
Exhibit 28: GPCRs- Drug Targets - Global Value Market Shares (2009 & 2015) by Geographic Region for United States, Europe, Japan, Asia-Pacific and Rest of World
3. Major Companies in GPCR - Drug Target Market
Arena Pharmaceuticals, Inc. (USA)
Aureus Pharma (France)
Caliper Life Sciences, Inc. (USA)
Euroscreen S.A. (Belgium)
Exalpha Biologicals, Inc. (USA)
Faust Pharmaceuticals S.A
More………….
4. Major Activities in GPCR Drug Market
Merck Serono Partners with Domain to Develop mGluR4 PAM Candidates
Receptos and Lilly Signs Agreement Focused on a GPCR Target?
Receptos Grants License to OMJPI for GPCR Crystal Structure
Evotec Enters into Agreement with Takeda Cambridge?
Mercator Therapeutics Establishes Research and Licensing Collaboration with Pepscan Therapeutics
More….
5. Regional Market Analysis
A. The United States
Market Analysis
Exhibit 29: GPCR- Drug Targets - United States Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Exhibit 30: List of Major Companies in United States
Analysis by GPCR Families
Exhibit 31: GPCR - Drug Targets - United States Value Market Estimations & Predictions (2005 -2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other in US$ Billion (Graphical Representation Included)
Exhibit 32: GPCR - Drug Targets - United States Value Market Shares (2009 & 2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other (Graphical Representation Included)
Analysis by GPCR Targeting Ligands
Exhibit 33: GPCR - Drug Targets - United States Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other in US$ Billion (Graphical Representation Included)
Exhibit 34: GPCR - Drug Targets - United States Value Market Shares (2009 & 2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other (Graphical Representation Included)
B. Japan
Market Analysis
Exhibit 35: GPCR – Drug Targets - Japanese Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Exhibit 36: List of Major Companies in Japan
Analysis by GPCR Families
Exhibit 37: GPCR - Drug Targets - Japanese Value Market Estimations & Predictions (2005 -2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other in US$ Billion (Graphical Representation Included)
Exhibit 38: GPCR - Drug Targets - Japanese Value Market Shares (2009 & 2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other (Graphical Representation Included)
Analysis by GPCR Targeting Ligands
Exhibit 39: GPCR - Drug Targets - Japanese Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other in US$ Billion (Graphical Representation Included)
Exhibit 40: GPCR - Drug Targets - Japanese Value Market Shares (2009 & 2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other (Graphical Representation Included)
C. Europe
Market Analysis
Exhibit 41: GPCR – Drug Targets - European Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Exhibit 41: List of Major Companies in Europe
Analysis by GPCR Families
Exhibit 42: GPCR – Drug Targets - European Value Market Estimations & Predictions (2005 -2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other in US$ Billion (Graphical Representation Included)
Exhibit 43: GPCR - Drug Targets - European Value Market Shares (2009 & 2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other (Graphical Representation Included)
Analysis by GPCR Targeting Ligands
Exhibit 44: GPCR - Drug Targets - European Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other in US$ Billion (Graphical Representation Included)
Exhibit 45: GPCR - Drug Targets - European Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other (Graphical Representation Included)
D. Asia-Pacific
Market Analysis
Exhibit 46: GPCR - Drug Targets - Asia-Pacific Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Exhibit 47: List of Major Companies in Asia-Pacific
Analysis by GPCR Families
Exhibit 48: GPCR - Drug Targets - Asia-Pacific Value Market Estimations & Predictions (2005 -2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other in US$ Billion (Graphical Representation Included)
Exhibit 49: GPCR - Drug Targets - Asia-Pacific Value Market Shares (2009 & 2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other (Graphical Representation Included)
Analysis by GPCR Targeting Ligands
Exhibit 50: GPCR – Drug Targets - Asia-Pacific Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other in US$ Billion (Graphical Representation Included)
Exhibit 51: GPCR – Drug Targets - Asia-Pacific Value Market Shares (2009 & 2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other (Graphical Representation Included)
E. REST OF WORLD
Market Analysis
Exhibit 52: GPCR - Drug Targets - Rest of World Value Market Estimations & Predictions (2005 -2015) in US$ Billion (Graphical Representation Included)
Exhibit 53: List of Major Companies in Rest of World
Analysis by GPCR Families
Exhibit 54: GPCR - Drug Targets - Rest of World Value Market Estimations & Predictions (2005 -2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other in US$ Billion (Graphical Representation Included)
Exhibit 55: GPCR – Drug Targets - Rest of World Value Market Shares (2009 & 2015) by GPCR Families for Rhodopsin, Secretin, Glutamate and Other (Graphical Representation Included)
Analysis by GPCR Targeting Ligands
Exhibit 56: GPCR – Drug Targets - Rest of World Value Market Estimations & Predictions (2005 -2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other in US$ Billion (Graphical Representation Included)
Exhibit 57: GPCR – Drug Targets - Rest of World Value Market Shares (2009 & 2015) by GPCR Targeting Ligands for Peptides or Proteins, Biogenic Amines, Lipids and Other (Graphical Representation Included)
IV. PRODUCT/TECHNOLOGY RESARCH
1. Introduction
GPCR Tractability: Current Therapeutics
GPCR
History of GPCR
Other Receptors
Structure of GPCR
Distribution
Role
G-Protein
History of G-Proteins
Structure
Role
Signal Transduction and Cell Response
Discoveries Pertaining to Signal Transduction
Mechanism of Signal Transduction
Regulation of Signal Transduction
Receptors of Signal Transduction
Legends
Exhibit 59: Extracellular Ligands and the Receptor they Bind
Exhibit 60: Intracellular Ligands and the Receptors they Bind
Receptors
Intracellular Receptors
Cell Surface Receptors
Receptor Tyrosine Kinases
Integrins
Toll-Like Receptors
Ligand-Gated Ion Channel Receptors
G-Proteins
Second Messengers
Diseases Associated with Signal Transduction
Dimerization & Oligomerization of GPCR
Dimerization of GPCR
Ontogeny
Regulation of Ligand
Dimerization in Signal Transduction
Internalization
Physiological Characteristics
Functional Dimerization of GPCRs
Homo and Hetero Dimerization
Function of GPCRs and Ligands
Is Every GPCR a Dimer?
Why GPCRs to be Dimers
GPCRs Permanent Dimers
GPCR Dimerization
Oligomeric Complex Containing Two GPCRs
Hypothesis II
The Inclination of GPCRs to Form Heterodimers
Altering of GPCR Dimers with Ligands
Oligomerization
Efficacy and Potency of a Ligand Differ for Monomeric and Oligomeric Receptors
Applications of Dimerization and Oligomerization
Dimerization
Dimer
Pharmacological Diversity
Effect of GPCR Dimerization on Ligand Pharmacology or Function
Effect of Dimerization of G-Protein Coupled Receptor
Heterodimerization of G-Protein Coupled Receptors
G-Protein Coupled Receptor Oligomerization for Neuroendocrine Pathways
Application of Computational Methods in Drug Designing
Concept for G-Protein Activation by G-Protein Coupled Receptor Dimers
G-Protein Coupled Receptor Heterodimerization
Oligomerization
Significance of G-Protein Coupled Receptor Oligomerization for Cell Signaling and
G-Protein Activation
Homo and Hetero-Oligomerization of G-Protein Coupled Receptors
Application of Oligomer Interface Prediction Method in Class A, G-Protein Coupled Receptors
Regulator of G-Protein Signaling
Introduction
G-Protein Subunit –Like Domain and Its Features
Regulation of RGS Expression and Effects of Various Factors
Sub Cellular Localization for Accomplishment of GAP Activity
Phosphorylation and Palmitoylation in RGS proteins
Protein and Lipid-Binding Partners
Receptor Selectivity
Regulator of G-Protein Signaling
Expression of Regulator of G-Protein Signaling Proteins
Expression of Regulator of G-Protein Signaling Proteins in Natural Killer Cells and Modulation
Regulator of G-Protein Signaling Proteins Applications
Novel Multifunctional Drug Targets
RGS Proteins as Drug Targets
RGS Proteins Differentially Control Chondrocyte Differentiation
Multi-Tasking Rgs Proteins in the Heart
Regulation of GPCR Signaling By Scaffold Proteins
RGS Proteins and the Cardiovascular System
1. RGS2
2. RGS4
3. GRK2
Human Heart Failure
Functioning of G-Protein Coupled Receptors
Mode of Action of G-Protein Coupled Receptors
GPCR – G-Protein Coupling
Receptor Structure
Heterotrimeric G-Proteins
Activation Cycle of G-Proteins by G-Protein Coupled Receptors
Receptor Activation
Molecular Switch
Receptor
Binding and Activation
Activation of G-Protein Coupled Receptors
Basic Method of Action
Pathway Description
Agonist-Specific Coupling
Agonists and Antagonists
Specific Coupling
Allosteric GPCR Agonists and Antagonists
G-Protein Coupled Receptor Kinases
Rhodopsin Kinase
Serine/Threonine-Specific Protein Kinases
Tyrosine-Specific Protein Kinases
Histidine-Specific Protein Kinases
Beta Adrenergic Receptor Kinase
Beta Adrenergic Receptor Kinase-2
Classification of GPCR
GPCR Classes
Class A Rhodopsin like
Retinylidene Protein
Structure
Types of Rhodopsins
Visual Opsins
Melanopsin
Parapinopsin
Peropsin
Neuropsin
Encephalopsin or Panopsin
Class B Secretin Like
Stimulus
Function
Structure
Class C Metabotropic Glutamate / Pheromone
Metabotropic Glutamate Receptors
Classification of Metabotropic Glutamate Receptors
Group I
Group II & Group III
Localization
Muscarinic Acetylcholine Receptor
The Form of Muscarinic Receptors
Class E cAMP Receptors
Cyclic Adenosine Monophosphate
Functions
cAMP Synthesis and Decomposition
Protein Kinase Activation
Cyclic Guanosine Monophosphate (cGMP)
Synthesis
Effects
Protein Kinase Activation
Class F Frizzled/Smoothened Family
Frizzled
Smoothened
The Structural Diversity of G-Protein Coupled Receptors and Their Role in Drug Discovery
The Rhodopsin Receptor Family/Class A
Recently De-orphanized Rhodopsin GPCRs
Exhibit 61: Classification of Rhodopsine SubFamilies Based on Type of Ligand Targeting
The Secretin Receptor Family – Class B
Exhibit 62: Sub-Families of Secretin Family Receptors
The Adhesion Receptor Family –Class B
De-Orphanized Adhesion Receptors
Orphan Adhesion Receptors
The Glutamate Family – Class C
Exhibit 63: Sub Families of Glutamate Family
The Frizzled/Taste2 Receptor
The Frizzled and Smoothened Receptors
Taste 2 Receptors
The Success of GPCRs
GPCRs Applications
GPCR Expression in the Heart
Regulation of the Cardiovascular System
GPCR Signals and Heterotrimeric G-Protein Activation
GPCR for Classical and Nonclassical Agonists for Cardiac and Fibroblasts
The Role of GPCRs in Cardiac Activities and Signal Transduction
GPCRs-Polymorphic Nature
New Drugs
Orphan GPCR Applications
Orphan Receptors
GPR56
Bob/GPR15
GPR1
Adenine Receptor
Neuropeptides
GPR34, GPR44, & GPR45
Ligand-Independent Functions of GPCRs
Chemokine Identification
Identification of a Novel CC Chemokine
Xcr1 Expression in Rheumatoid Joints
Molecular Cloning and Chromosomal Localization of GPCR
Sensing of Protons in G-Protein Coupled Receptors
Ligand of the Human GPCR: Sphingosine 1-Phosphate
GPCRs in Human Neuropeptides
Characterization of Binding of Human Prolactin Releasing Peptide, A GPCR
Regulation of G-Protein Coupled Receptor Signaling and Trafficking
Protease-Activated Receptors
Where are PARS present?
PAR Activation and G-Protein Signaling
G-Protein Coupled Receptor Kinase (GRK)
GPCR Array Technology in the Process of Drug Discovery
Introduction
GPCR Microarrays in Pharmaceutical Industry
Other GPCR Receptors
Adenosine Receptor: Its Omnipresent Nature
GABA Receptor: Vital Neuro Transmitter
GABAA
GABAC
Angiotensin Receptor: A Variety of G-Protein Coupled Receptors
AT1
AT2
AT3 and AT4 Receptors
Cannabinoid Receptor: A Variety of G-Protein Coupled Receptors
Cannabinoid Receptor Subtypes
CB1
CB2
Cholecystokinin Receptor and Its Subtypes
Dopamine Receptor: A Metabotropic G-Protein Coupled Receptor
D1-Like Family (Excitatory)
D2-Like Family (Inhibitory)
Somatostatin Receptor or Growth Hormone Inhibiting Hormone
Histamine Receptor with Histamine as Their Endogenous Ligand
Olfactory Receptors: Class A Variety of G-Protein Coupled Receptor
Structure of Olfactory Receptors
Regeneration
Calcium-Sensing Receptor and its Key Role in Parathyroid Gland
Chemokine Receptor and Its Structure
Opioid Receptors
Muscarinic Cholinergic Receptors
Orphan Receptor
Rhodopsin
The Adrenergic Receptor and Its Applications
Introduction
Agonist-Binding Site of ß2 –Adrenergic Receptors
Binding Site for ß2 –Adrenergic Receptors – Selective Agonists
Binding to a Constitutively Active Receptor
The Role of Different Amino Acids in the Binding of Agonists and Antagonists
Adrenergic Receptors 325 Agonist-Specific Changes in Receptor Conformation
Relationship Between the ß2 –Adrenergic Receptor-Selective Binding Site and the
Exosite of Salmeterol
Agonist-Induced Specific Conformational Changes of Receptors
Responses to Partial Agonists
Desensitization and Partial Agonists
Internalization, Lysosome Targeting and Desensitization
Polymorphism of Human ß2 -Adrenergic Receptors
Polymorphism of ß2 - Adrenergic Receptors and Agonist Actions
Secretin
Glutamate
Other
Physiological Roles of G-Protein Coupled Receptors
Function of Molecule Binds to Receptors
GPCRs Involved in Physiological Processes
Opsin Functions
Neurotransmitters
Types of Neurotransmitters
Effects
Examples of Neurotransmitter Action
Neurotransmitters Functioning
Post-Synaptic Effect
Specifications
Neurotransmitters Specific Actions Targeted by Drugs
Common Neurotransmitters
Serotonin
Serotonin’s Role in Central Nervous System
Serotonin in the Body
The Pathway for the Synthesis of Serotonin from Tryptophan
Serotonin in Neurotransmission
Pharmacology
Receptors
Psychedelic Modulation
Therapeutic Modulation
Modulating Levels
Antidepressants
Antiemetics
Serotonin Syndrome
Serotonin Syndrome’s Effect
Bacteria, Yeast, Algae, Parasites
Exhibit 64: GPCR Targeted Cancer Drugs
Dopamine
Functions in the Brain
Movement
Cognition and Frontal Cortex
Regulating Prolactin Secretion
Motivation and Pleasure
Latent Inhibition and Creative Drive
Links to Psychosis
Dopamine Hypothesis of Psychosis
Therapeutic Use
Dopamine and Fruit Browning
Dopamine Like Family
D1-Like Family
D2-Like Family (inhibitory)
Role of Dopamine Receptors in the Central Nervous System
Cardio-Pulmonary System
Renal System
Dopamine Receptors in Disease
Attention-Deficit Hyperactivity Disorder
Recreational Drug Use and Abuse
Dopamine Hypothesis of Schizophrenia
Genetic Hypertension
Exhibit 65: GPCR Targeted CNS Drugs
Gamma Amino Butyric Acid
Metabotropic Glutamate Receptors Functions
Modulation of Other Receptors
Role in Plasticity
Role in Disease
Synthesis
Pharmacology
In Metabolism
As a Neurotransmitter
Fast Excitatory Neurotransmitter
The Mechanisms of Cell Death Include
Glutamic Acid Implicated in Epileptic Seizures
In Brain Nonsynaptic Glutamatergic Signaling Circuits
GABA Precursor
Pharmacology
Response to GABA Basis of Pharmacological Properties
Molecular Determinants Involved In the Allosteric Control of Agonist
Muscarinic Acetylcholine Receptor
Types of Muscarinic Acetylcholine Receptors
The Form or Class of Muscarinic Receptors
Categorization Strategies for Muscarinic Receptors
M2 CHRM2
M3 CHRM3
Application of Muscarinic Acetylcholine Receptors on Various Parts of the body
Application/Role of Acetylcholine in Brain
Acetylcholine and its Application as Postganglionic Neurons
Acetylcholine as Neurotransmitter and its Use in Autonomic Nervous System
Acetylcholine and its Role as Postganglionic Neurons in the Innervated tissue
Muscarinic Acetylcholine Receptors and its Presence in Central Nervous System
Role in Regulation of Acetylcholine Release along the Presynaptic Membrane
Exhibit 66: GPCR Targeted Cardiovascular Drugs
Adenosine
Adenosine Receptor a Part of the Endogenous Adenosine Group
Histamine
Histamine H3receptor: Auto Receptors in Presynaptic Histaminergic Neurons
H3 Receptors in Central Nervous System
Pharmacology
H3 Receptors Agonists and Antagonists
Formation of H3-receptor Agonists
Varieties of H3-Receptor Antagonists
Antihistamines - H3-Receptor Antagonists
Antihistamine
H1 Antihistamine its Role in Eliminating Effects Mediated by Histamine
Antihistamine Pharmacology
Clinical Applications of Antihistamines
Indications
Adverse Drug Reactions Caused by Antihistamines
First-generation (Non-Selective and Classical) Antihistamines
Different Classes of H1-Antihistamines
Exhibit 67: GPCR Targeted Respiratory Drugs
Ethylenediamines
Diphenhydramin
Tricyclics and Tetracyclics
Second-Generation and Third-Generation (Selective and Non-Sedative)
Antihistamine Drugs
Role of Histamines in Neurophysiology
Applications of Histamines
Approved
Unapproved /Off-Label/Investigational Applications
Chlorpromazine
A Phenothiazine Antipsychotic in Treatment of Schizophrenia
Other Applications
Off-label and Controversial Applications
Chlorpromazine Pharmacology
Pharmacokinetics
Central Effects
Peripheral Effects
Doxepin
Doxepin: a Psychotropic Agent
Doxepin Pharmacology
Promethazine
Cinnarizine
Olfactory (Smell Sensing) Receptors
Olfactory Epithelium
Olfactory Receptors
Olfactory Receptor Neuron
Function
Variety & Diversity
Exhibit 68: Other GPCR Targeted Drugs
Somatostatin Receptor
Digestive System
Brain
Functions
Substitutes for Somatostatin
cAMP Receptors (cAMP)
Synthesis of cAMP
Kinase Activation
Decomposition of Glycogen
Role of cAMP in Bacteria
cAMP Function in Slime Moulds
cAMP Regulation in Human Carcinoma
Role of cAMP in Prefrontal Cortex Disorders
Activating the Receptors
Preventing Skin Infections
Production of AMP
Estrogen Receptor Activation
Receptor Activation in Breast Cancer
Activation of Liver X Receptor
Viral Repression of Fungal Pheromone
Peptides or Proteins
Biogenic Amines
Lipids
Other
Ligand
Receptor Regulation
Desensitization of GPCR
GRK
GRK1
GRK2 and GRK3
GRK4
GRK5
GRK6
GRK7
Other kinases
PKA
PKC
c-Src
Arrestins
Second Messengers
GPCR Screening
Introduction
Effective GPCR Screening Using ERK
Cellular Assay
Assay Applications
Orphan GPCR Screening
Pathway
A New Messenger for the GQ Pathway
Technologies Used in GPCR Screening
Protein Coupled Receptors and High Throughput Screening
Cellular Expression of GPCRs
High Throughput Ligand Binding Assays
Measurement of GPCR Ligand Binding
High Throughput Functional Assays
In Reporter Gene Assays.
Second Messenger Assays to Measure GPCR Function
Protein Redistribution Assays
Other GPCR Screening Assays
Applications for GPCR Screening
The Gq Pathway
GPCRs Kinetics
Ligand Channeling and Receptor Mixing
High Throughput Screening for Development of Cellular Tools
Ligand-Gated Ion Channel Assays
GPCR Screening Using Ion Channel Targets
High-Throughput Screening of G-Protein Coupled Receptors Using Technologies
Secondary Screening of GPCRs
G-Protein Coupled Receptor Motif Sequence Analysis
Application of G-Protein Coupled Receptors (GPCRs) Considered a
Machine Learning Approach
Various Steps in GPCR Activation
GPCR Research
GPCR omics
GPCR Informatics
Computational Methods Considered Mandatory for Detecting Additional and
Potentially Novel Aminergic GPCRS
Strengths and Weaknesses of the Present Protein Classification Tools
Iterative Unbiased Profile Alignment of Sequences an Effective Method for
Multiple Sequence Alignments
Analysis of Correlated Mutations
Bayesian Neural Networks with Correlating Residuals for Motif Analysis
Markov Chain Monte Carlo for Minimizing Squared Error
Addition of Neural Network Models to the Bayesian Inference Framework
GPCR Assay Technologies
Receptor/Ligand Binding
Two Agonists Having Comparable Binding Affinity
Receptor/ Protein Ligand Binding
Assay Development and Data Analysis of Receptor-Ligand Binding
Radioligand Binding Assays
GTP Binding Assay for Gs-Protein Coupled Receptors
Second Messenger Assays
Protein Interaction Assay
Protein Interactions Categories
Stable Interactions
Transient Interactions
The Yeast Two-Hybrid System, The “Bait-Prey” Model
Protein: Nucleic Acid Interaction Analysis Techniques In vitro
Protein: Nucleic Acid Interactions
In vitro Techniques for Protein: Nucleic Acid Interaction Analysis
Protein Coupled Receptor Trafficking
Membrane Trafficking of G-Protein Coupled Receptors
Opioid Receptors Oligomerization with ß2 -Adrenergic Receptors
GPCR Signaling Promiscuity and Trafficking of Receptor Stimulus
Reporter Gene Assays
Common Reporter Genes
Transformation and Transfection Assays
Gene Expression Assays
Bioimpedance Assays
Applications of GPCR Assay Technologies
Receptor Ligand Binding Assays
Protein Interaction
Protein –Protein Interaction
Co-Immunoprecipitation (Co-IP)
Far-Western Analysis
Protein Arrays/Protein Chips
Pull-Down Assays
Phenomenon of Surface Resonance
Nuclear Magnetic Resonance (NMR) Technology
Mass Spectroscopy
X-ray Crystallography
Protein Nucleic Acid Interaction Analysis
Electrophoretic Mobility Shift Assay
Supershift Assay
Protein: DNA Cross-Linking Method
Bioimpedance Applications
Evaluation by Bioimpedance
Major Bioimpedance Applications
Application of Bioimpedance Technique to Peritoneal Dialysis
Monitoring the Neurological State of a Patient
Gs-Coupled GPCR Reporter Assay
Bioluminescence Resonance Energy Transfer2 Assay Technology
Introduction
BRET2 Principle
BRET2 Features
BRET2 Configurations
2. Research Briefs
4. Product Trends
Screening of GPCR Ligands and Drugs Regulating GPCRs
Databases to Accelerate Drug Discovery
Identifying Ligand
More…………….
5. GPCR – Drug Targets - The Outlook
V. CORPORATE DIRECTORY
VI. PATENTS INFORMATION |
