Target-Based Small Molecule Drug Discovery Towards Novel Therapeutics for Inflammatory Bowel Diseases

Efficacy of Upadacitinib in a Randomized Trial of Patients With Active Ulcerative Colitis

(2020) William J. Sandborn et al.   GASTROENTEROLOGY

Efficacy and Safety of Upadacitinib in a Randomized Trial of Patients With Crohn’s Disease

(2020) William J. Sandborn et al.   GASTROENTEROLOGY

6 NOVEL BRD4 INHIBITORS BLOCK THE PATHOLOGICAL ACTIVATION OF BRD4-NFκB SIGNALING AND SUPPRESS COLONIC INFLAMMATION IN IBD MOUSE MODELS

(2020) Zhiqing Liu et al.   INFLAMMATORY BOWEL DISEASES

Development of Gut-Selective Pan-Janus Kinase Inhibitor TD-1473 for Ulcerative Colitis: A Translational Medicine Programme

(2020) William J Sandborn et al.   Journal of Crohns & Colitis

Advances in the development of phosphodiesterase-4 inhibitors

(2020) Ting Peng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation

(2020) Zhiqing Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

JAK–STAT pathway targeting for the treatment of inflammatory bowel disease

(2020) Azucena Salas et al.   Nature Reviews Gastroenterology & Hepatology

Small molecule oral targeted therapies in ulcerative colitis

(2020) Uday N Shivaji et al.   Lancet Gastroenterology & Hepatology

Small molecule drugs in the treatment of inflammatory bowel diseases

(2020) Laura A. Lucaciu et al.   EUROPEAN JOURNAL OF GASTROENTEROLOGY & HEPATOLOGY

Recent advances in the mechanisms of NLRP3 inflammasome activation and its inhibitors

(2019) Yang Yang et al.   Cell Death & Disease

Oral Treatment with BT-11 Ameliorates Inflammatory Bowel Disease by Enhancing Regulatory T Cell Responses in the Gut

(2019) Andrew Leber et al.   JOURNAL OF IMMUNOLOGY

OP09 Histological remission and mucosal healing in a randomised, placebo-controlled, Phase 2 study of etrasimod in patients with moderately to severely active ulcerative colitis

(2019) L Peyrin-Biroulet et al.   Journal of Crohns & Colitis

Nonclinical Toxicology and Toxicokinetic Profile of an Oral Lanthionine Synthetase C-Like 2 (LANCL2) Agonist, BT-11

(2019) Andrew Leber et al.   INTERNATIONAL JOURNAL OF TOXICOLOGY

The NLRP3 inflammasome mediates DSS-induced intestinal inflammation in Nod2 knockout mice

(2019) Benjamin Umiker et al.   Innate Immunity

Selective JAKinibs: Prospects in Inflammatory and Autoimmune Diseases

(2019) Anniina T. Virtanen et al.   BIODRUGS

Small-molecule agents for the treatment of inflammatory bowel disease

(2019) Kevin S. Currie et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Perspectives on Current and Novel Treatments for Inflammatory Bowel Disease

(2019) Soo-Young Na et al.   Gut and Liver

Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV

(2019) Qingli Niu et al.   JOURNAL OF CLINICAL INVESTIGATION

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)

(2019) Ryan Moslin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165

(2019) Stephen T. Wrobleski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bromodomains: a new target class for drug development

(2019) Andrea G. Cochran et al.   NATURE REVIEWS DRUG DISCOVERY

Bromodomain inhibitor JQ1 reversibly blocks IFN-γ production

(2019) Hunter R. Gibbons et al.   Scientific Reports

Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease

(2019) Germain Homerin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacoproteomics reveal novel protective activity of bromodomain containing 4 inhibitors on vascular homeostasis in TLR3-mediated airway remodeling

(2019) Yingxin Zhao et al.   Journal of Proteomics

Inflammatory Bowel Disease Presentation and Diagnosis

(2019) Sean Flynn et al.   SURGICAL CLINICS OF NORTH AMERICA

Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling

(2019) Allan R. Brasier et al.   DRUG DISCOVERY TODAY

Discovery of small-molecule candidates against inflammatory bowel disease

(2019) Renren Bai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Amiselimod (MT-1303), a novel sphingosine 1-phosphate receptor-1 functional antagonist, inhibits progress of chronic colitis induced by transfer of CD4+CD45RBhigh T cells

(2019) Kyoko Shimano et al.   PLoS One

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

(2018) Zhiqing Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Janus kinase inhibitors for the treatment of inflammatory bowel diseases: developments from phase I and phase II clinical trials

(2018) Ferdinando D’Amico et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

349 - BMS-986165 is a Highly Potent and Selective Allosteric Inhibitor of TYK2, Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease

(2018) Jenny H. Xie et al.   GASTROENTEROLOGY

Activation of LANCL2 by BT-11 Ameliorates IBD by Supporting Regulatory T Cell Stability Through Immunometabolic Mechanisms

(2018) Andrew Leber et al.   INFLAMMATORY BOWEL DISEASES

OP006 Apremilast for active ulcerative colitis: a phase 2, randomised, double-blind, placebo-controlled induction study

(2018) S Danese et al.   Journal of Crohns & Colitis

Gut-selective integrin-targeted therapies for inflammatory bowel disease

(2018) Christopher A Lamb et al.   Journal of Crohns & Colitis

Peficitinib, an Oral Janus Kinase Inhibitor, in Moderate-to-severe Ulcerative Colitis: Results From a Randomised, Phase 2 Study

(2018) Bruce E Sands et al.   Journal of Crohns & Colitis

Central Role of the NF-κB Pathway in the Scgb1a1 -Expressing Epithelium in Mediating Respiratory Syncytial Virus-Induced Airway Inflammation

(2018) Bing Tian et al.   JOURNAL OF VIROLOGY

The current state of the art for biological therapies and new small molecules in inflammatory bowel disease

(2018) Sudarshan Paramsothy et al.   Mucosal Immunology

Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus

(2018) Kristen R. Taylor Meadows et al.   PLoS One

MCC950, a specific small molecule inhibitor of NLRP3 inflammasome attenuates colonic inflammation in spontaneous colitis mice

(2018) Agampodi Promoda Perera et al.   Scientific Reports

Selective Antagonists of the Bronchiolar Epithelial NF-κB-Bromodomain-Containing Protein 4 Pathway in Viral-Induced Airway Inflammation

(2018) Bing Tian et al.   Cell Reports

Efficacy of Novel Highly Specific Bromodomain-Containing Protein 4 Inhibitors in Innate Inflammation-Driven Airway Remodeling

(2018) Bing Tian et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor

(2018) Hisao Hamaguchi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tofacitinib Induction Therapy Reduces Symptoms Within 3 Days for Patients With Ulcerative Colitis

(2018) Stephen Hanauer et al.   Clinical Gastroenterology and Hepatology

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

(2018) Andrew Fensome et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benzo[d]thiazol-2(3H)-ones as new potent selective CB2 agonists with anti-inflammatory properties

(2018) Natascha Leleu-Chavain et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Mucosal bromodomain-containing protein 4 mediates aeroallergen-induced inflammation and remodeling

(2018) Bing Tian et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases

(2018) Heng Li et al.   Frontiers in Pharmacology

Tofacitinib for induction and maintenance therapy of Crohn's disease: results of two phase IIb randomised placebo-controlled trials

(2017) Julian Panés et al.   GUT

The P2X7 Receptor in Infection and Inflammation

(2017) Francesco Di Virgilio et al.   IMMUNITY

PDE4 Inhibition and Inflammatory Bowel Disease: A Novel Therapeutic Avenue

(2017) Marco Spadaccini et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The Future of Janus Kinase Inhibitors in Inflammatory Bowel Disease

(2017) L.C.S. De Vries et al.   Journal of Crohns & Colitis

DOP078 Pharmacology and safety of etrasimod (APD334), an oral, potent, next-generation, selective S1P receptor modulator

(2017) T. Kühbacher et al.   Journal of Crohns & Colitis

P469 Safety, tolerability, and pharmacokinetics of the intestine-restricted oral pan-Janus kinase inhibitor TD-1473 after single and multiple oral doses in healthy subjects

(2017) B. Ferslew et al.   Journal of Crohns & Colitis

Drug Discovery Targeting Bromodomain-Containing Protein 4

(2017) Zhiqing Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans

(2017) Atli Thorarensen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

(2017) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease

(2017) Mattia Cocco et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model

(2017) Misato Ito et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

BRD4 Couples NF-κB/RelA with Airway Inflammation and the IRF-RIG-I Amplification Loop in Respiratory Syncytial Virus Infection

(2017) Bing Tian et al.   JOURNAL OF VIROLOGY

Worldwide incidence and prevalence of inflammatory bowel disease in the 21st century: a systematic review of population-based studies

(2017) Siew C Ng et al.   LANCET

Distinct Roles of Brd2 and Brd4 in Potentiating the Transcriptional Program for Th17 Cell Differentiation

(2017) Ka Lung Cheung et al.   MOLECULAR CELL

Oncostatin M drives intestinal inflammation and predicts response to tumor necrosis factor–neutralizing therapy in patients with inflammatory bowel disease

(2017) Nathaniel R West et al.   NATURE MEDICINE

JAK inhibition as a therapeutic strategy for immune and inflammatory diseases

(2017) Daniella M. Schwartz et al.   NATURE REVIEWS DRUG DISCOVERY

Current and emerging therapeutic targets for IBD

(2017) Markus F. Neurath   Nature Reviews Gastroenterology & Hepatology

The emerging safety profile of JAK inhibitors in rheumatic disease

(2017) Kevin L. Winthrop   Nature Reviews Rheumatology

Tofacitinib as Induction and Maintenance Therapy for Ulcerative Colitis

(2017) William J. Sandborn et al.   NEW ENGLAND JOURNAL OF MEDICINE

BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice

(2017) Kalung Cheung et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression

(2017) Geoffrey Burnstock et al.   Purinergic Signalling

BET bromodomain inhibition suppresses innate inflammatory and profibrotic transcriptional networks in heart failure

(2017) Qiming Duan et al.   Science Translational Medicine

Sphingosine-1-Phosphate Signaling in Inflammatory Bowel Disease

(2017) Ole Haagen Nielsen et al.   TRENDS IN MOLECULAR MEDICINE

Novel Targeted Therapies for Inflammatory Bowel Disease

(2017) Mehmet Coskun et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Coordinate activities of BRD4 and CDK9 in the transcriptional elongation complex are required for TGFβ-induced Nox4 expression and myofibroblast transdifferentiation

(2017) Talha Ijaz et al.   Cell Death & Disease

Frontiers in Drug Research and Development for Inflammatory Bowel Disease

(2017) Diego Currò et al.   Frontiers in Pharmacology

Canonical and Non-Canonical Activation of NLRP3 Inflammasome at the Crossroad between Immune Tolerance and Intestinal Inflammation

(2017) Carolina Pellegrini et al.   Frontiers in Immunology

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

(2016) Jean-Baptiste Telliez et al.   ACS Chemical Biology

BRD4 mediates NF-κB-dependent epithelial-mesenchymal transition and pulmonary fibrosis via transcriptional elongation

(2016) Bing Tian et al.   AMERICAN JOURNAL OF PHYSIOLOGY-LUNG CELLULAR AND MOLECULAR PHYSIOLOGY

Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk

(2016) Kunio Sugahara et al.   BRITISH JOURNAL OF PHARMACOLOGY

Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1) and receptor-5 (S1P5) agonist with autoimmune disease-modifying activity

(2016) F L Scott et al.   BRITISH JOURNAL OF PHARMACOLOGY

Tu1889 Targeting of NLRP3 Inflammasome With a Novel Selective Inhibitor as a Suitable Strategy for the Pharmacological Treatment of Bowel Inflammation

(2016) Carolina Pellegrini et al.   GASTROENTEROLOGY

RIPK1 and RIPK3 Kinases Promote Cell-Death-Independent Inflammation by Toll-like Receptor 4

(2016) Malek Najjar et al.   IMMUNITY

JAK1-STAT3 blockade by JAK inhibitor SHR0302 attenuates inflammatory responses of adjuvant-induced arthritis rats and decreases Th17 and total B cells

(2016) Huaxun Wu et al.   JOINT BONE SPINE

An N,N-Bis(benzimidazolylpicolinoyl)piperazine (BT-11): A Novel Lanthionine Synthetase C-Like 2-Based Therapeutic for Inflammatory Bowel Disease

(2016) Adria Carbo et al.   JOURNAL OF MEDICINAL CHEMISTRY

A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease

(2016) S. Barret Kalindjian et al.   JOURNAL OF MEDICINAL CHEMISTRY

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors

(2016) Philip A. Harris et al.   JOURNAL OF MEDICINAL CHEMISTRY

Integrin-based therapeutics: biological basis, clinical use and new drugs

(2016) Klaus Ley et al.   NATURE REVIEWS DRUG DISCOVERY

Mechanism and Regulation of NLRP3 Inflammasome Activation

(2016) Yuan He et al.   TRENDS IN BIOCHEMICAL SCIENCES

CXCR4 inhibitor attenuates ovalbumin-induced airway inflammation and hyperresponsiveness by inhibiting Th17 and Tc17 cell immune response

(2016) HUILONG CHEN et al.   Experimental and Therapeutic Medicine

Randomised clinical trial: vercirnon, an oral CCR9 antagonist, vs. placebo as induction therapy in active Crohn's disease

(2015) B. G. Feagan et al.   ALIMENTARY PHARMACOLOGY & THERAPEUTICS

The JAK-STAT Pathway: Impact on Human Disease and Therapeutic Intervention

(2015) John J. O'Shea et al.   Annual Review of Medicine

Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors

(2015) Michael Friedman et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Evaluation of 1H-Pyrrolo[2,3-b]pyridine Derivatives as Novel Immunomodulators Targeting Janus Kinase 3

(2015) Yutaka Nakajima et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Modeling of Filgotinib (GLPG0634), a Selective JAK1 Inhibitor, in Support of Phase IIB Dose Selection

(2015) Florence Namour et al.   CLINICAL PHARMACOKINETICS

Sphingosine 1-Phosphate Receptor Modulators in Multiple Sclerosis

(2015) Adnan M. Subei et al.   CNS DRUGS

Safety and Efficacy of AJM300, an Oral Antagonist of α4 Integrin, in Induction Therapy for Patients With Active Ulcerative Colitis

(2015) Naoki Yoshimura et al.   GASTROENTEROLOGY

The diverse role of RIP kinases in necroptosis and inflammation

(2015) John Silke et al.   NATURE IMMUNOLOGY

A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

(2015) Rebecca C Coll et al.   NATURE MEDICINE

BET protein Brd4 activates transcription in neurons and BET inhibitor Jq1 blocks memory in mice

(2015) Erica Korb et al.   NATURE NEUROSCIENCE

Biologic agents for IBD: practical insights

(2015) Silvio Danese et al.   Nature Reviews Gastroenterology & Hepatology

The global burden of IBD: from 2015 to 2025

(2015) Gilaad G. Kaplan   Nature Reviews Gastroenterology & Hepatology

Immunopathogenesis of IBD: current state of the art

(2015) Heitor S. P. de Souza et al.   Nature Reviews Gastroenterology & Hepatology

Inflammatory Bowel Disease Patients Are Frequently Nonadherent to Scheduled Induction and Maintenance Infliximab Therapy: A Canadian Cohort Study

(2015) Christopher Ma et al.   Canadian Journal of Gastroenterology and Hepatology

Tofacitinib

(2014) Deepti Vyas et al.   ANNALS OF PHARMACOTHERAPY

Structure–activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201

(2014) Nobuhiko Hayakawa et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Inducible STAT3 NH2 terminal mono-ubiquitination promotes BRD4 complex formation to regulate apoptosis

(2014) Sutapa Ray et al.   CELLULAR SIGNALLING

A Phase 2 Study of Tofacitinib, an Oral Janus Kinase Inhibitor, in Patients With Crohn’s Disease

(2014) William J. Sandborn et al.   Clinical Gastroenterology and Hepatology

Lanthionine Synthetase Component C-Like Protein 2: A New Drug Target for Inflammatory Diseases and Diabetes

(2014) Pinyi Lu et al.   CURRENT DRUG TARGETS

P072 GLPG0634, the first selective JAK1 inhibitor, shows strong activity in the mouse DSS-colitis model

(2014) D. Merciris et al.   Journal of Crohns & Colitis

Mechanisms of Jak/STAT Signaling in Immunity and Disease

(2014) Alejandro V. Villarino et al.   JOURNAL OF IMMUNOLOGY

Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice

(2014) S. B. Berger et al.   JOURNAL OF IMMUNOLOGY

Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634

(2014) Christel J. Menet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases

(2014) James D. Clark et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

(2014) David Cook et al.   NATURE REVIEWS DRUG DISCOVERY

Purinergic receptor P2X7: A novel target for anti-inflammatory therapy

(2013) Nisha Mehta et al.   BIOORGANIC & MEDICINAL CHEMISTRY

PIKfyve, a Class III PI Kinase, Is the Target of the Small Molecular IL-12/IL-23 Inhibitor Apilimod and a Player in Toll-like Receptor Signaling

(2013) Xinming Cai et al.   CHEMISTRY & BIOLOGY

Intestinal Targeting of Drugs: Rational Design Approaches and Challenges

(2013) Kevin J. Filipski et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

The IκB kinase complex in NF-κB regulation and beyond

(2013) Michael Hinz et al.   EMBO REPORTS

The burden of inflammatory bowel disease in Europe

(2013) Johan Burisch et al.   Journal of Crohns & Colitis

Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice

(2013) Toshihiko Sugiura et al.   Journal of Crohns & Colitis

CDK9-Dependent Transcriptional Elongation in the Innate Interferon-Stimulated Gene Response to Respiratory Syncytial Virus Infection in Airway Epithelial Cells

(2013) B. Tian et al.   JOURNAL OF VIROLOGY

Regulation of RIP1 kinase signalling at the crossroads of inflammation and cell death

(2013) Dimitry Ofengeim et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Tumor Necrosis Factor Inhibitors for Inflammatory Bowel Disease

(2013) Ole Haagen Nielsen et al.   NEW ENGLAND JOURNAL OF MEDICINE

Effects of the Janus Kinase Inhibitor CP-690550 (Tofacitinib) in a Rat Model of Oxazolone-Induced Chronic Dermatitis

(2013) Yasutomo Fujii et al.   PHARMACOLOGY

A Randomized Controlled Trial of the Efficacy and Safety of CCX282-B, an Orally-Administered Blocker of Chemokine Receptor CCR9, for Patients with Crohn’s Disease

(2013) Satish Keshav et al.   PLoS One

Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator

(2013) Shifeng Pan et al.   ACS Medicinal Chemistry Letters

TRAIL induces necroptosis involving RIPK1/RIPK3-dependent PARP-1 activation

(2012) S Jouan-Lanhouet et al.   CELL DEATH AND DIFFERENTIATION

P2X7 Receptors: Channels, Pores and More

(2012) C. Volonte et al.   CNS & Neurological Disorders-Drug Targets

Recent Advances in the Development of Selective CB2 Agonists as Promising Anti-Inflammatory Agents

(2012) N. Leleu-Chavain et al.   CURRENT MEDICINAL CHEMISTRY

Jakinibs: a new class of kinase inhibitors in cancer and autoimmune disease

(2012) Apostolos Kontzias et al.   CURRENT OPINION IN PHARMACOLOGY

The JAK-STAT Pathway at Twenty

(2012) George R. Stark et al.   IMMUNITY

4-Oxo-1,4-dihydropyridines as Selective CB2 Cannabinoid Receptor Ligands Part 2: Discovery of New Agonists Endowed with Protective Effect Against Experimental Colitis

(2012) Jamal El Bakali et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and mechanism of ustekinumab

(2012) Jacqueline M. Benson et al.   mAbs

The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation

(2012) Zichong Li et al.   NUCLEIC ACIDS RESEARCH

Development of a Unique Small Molecule Modulator of CXCR4

(2012) Zhongxing Liang et al.   PLoS One

The JAK/STAT Pathway

(2012) D. A. Harrison   Cold Spring Harbor Perspectives in Biology

Reactivation of Latent HIV-1 by Inhibition of BRD4

(2012) Jian Zhu et al.   Cell Reports

Review article: loss of response to anti-TNF treatments in Crohn’s disease

(2011) S. Ben-Horin et al.   ALIMENTARY PHARMACOLOGY & THERAPEUTICS

Review article: remission rates achievable by current therapies for inflammatory bowel disease

(2011) L. Peyrin-Biroulet et al.   ALIMENTARY PHARMACOLOGY & THERAPEUTICS

Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)

(2011) Scott H. Watterson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibitory kappa B kinases as targets for pharmacological regulation

(2011) Carly Gamble et al.   BRITISH JOURNAL OF PHARMACOLOGY

Increasing Incidence and Prevalence of the Inflammatory Bowel Diseases With Time, Based on Systematic Review

(2011) Natalie A. Molodecky et al.   GASTROENTEROLOGY

Interleukin-23 and T helper 17-type responses in intestinal inflammation: from cytokines to T-cell plasticity

(2011) Peter J. Morrison et al.   IMMUNOLOGY

Oral fingolimod for the treatment of patients with relapsing forms of multiple sclerosis

(2011) B. Singer et al.   INTERNATIONAL JOURNAL OF CLINICAL PRACTICE

RelA Ser276 Phosphorylation-Coupled Lys310 Acetylation Controls Transcriptional Elongation of Inflammatory Cytokines in Respiratory Syncytial Virus Infection

(2011) A. R. Brasier et al.   JOURNAL OF VIROLOGY

Genetics and pathogenesis of inflammatory bowel disease

(2011) Bernard Khor et al.   NATURE

The Dual Functions of Receptor Interacting Protein 1 in Fas-Induced Hepatocyte Death During Sepsis

(2011) Sam I. McNeal et al.   SHOCK

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis

(2010) Alaric J. Dyckman et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Abscisic acid ameliorates experimental IBD by downregulating cellular adhesion molecule expression and suppressing immune cell infiltration

(2010) Amir J. Guri et al.   CLINICAL NUTRITION

Targeting IL-23 in human diseases

(2010) Mario M D'Elios et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Risk Factors Associated With Progression to Intestinal Complications of Crohn's Disease in a Population-Based Cohort

(2010) Kelvin T. Thia et al.   GASTROENTEROLOGY

4-Oxo-1,4-dihydropyridines as Selective CB2Cannabinoid Receptor Ligands: Structural Insights into the Design of a Novel Inverse Agonist Series

(2010) Jamal El Bakali et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection

(2010) Mark E. Flanagan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural and Thermodynamic Characterization of the TYK2 and JAK3 Kinase Domains in Complex with CP-690550 and CMP-6

(2010) Jill E. Chrencik et al.   JOURNAL OF MOLECULAR BIOLOGY

Characterization of CCX282-B, an Orally Bioavailable Antagonist of the CCR9 Chemokine Receptor, for Treatment of Inflammatory Bowel Disease

(2010) M. J. Walters et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Integrins as therapeutic targets: lessons and opportunities

(2010) Dermot Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis

(2010) Volker Brinkmann et al.   NATURE REVIEWS DRUG DISCOVERY

A Placebo-Controlled Trial of Oral Fingolimod in Relapsing Multiple Sclerosis

(2010) Ludwig Kappos et al.   NEW ENGLAND JOURNAL OF MEDICINE

Apremilast: a novel PDE4 inhibitor in the treatment of autoimmune and inflammatory diseases

(2010) Georg Schett et al.   Therapeutic Advances in Musculoskeletal Disease

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IκB kinase

(2009) James Kempson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Integrins

(2009) Malgorzata Barczyk et al.   CELL AND TISSUE RESEARCH

From interleukin-23 to T-helper 17 cells: human T-helper cell differentiation revisited

(2009) Katia Boniface et al.   IMMUNOLOGICAL REVIEWS

Janus kinases in immune cell signaling

(2009) Kamran Ghoreschi et al.   IMMUNOLOGICAL REVIEWS

LANCL2 Is Necessary for Abscisic Acid Binding and Signaling in Human Granulocytes and in Rat Insulinoma Cells

(2009) Laura Sturla et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Novel Tricyclic Inhibitors of IκB Kinase

(2009) James Kempson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (S)-N-{2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide (Apremilast), a Potent and Orally Active Phosphodiesterase 4 and Tumor Necrosis Factor-α Inhibitor

(2009) Hon-Wah Man et al.   JOURNAL OF MEDICINAL CHEMISTRY

Periodic, Partial Inhibition of I B Kinase  -Mediated Signaling Yields Therapeutic Benefit in Preclinical Models of Rheumatoid Arthritis

(2009) K. M. Gillooly et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Therapeutic targeting of Janus kinases

(2008) Marko Pesu et al.   IMMUNOLOGICAL REVIEWS

Leukocyte adhesion molecules in animal models of inflammatory bowel disease

(2008) Jesús Rivera-Nieves et al.   INFLAMMATORY BOWEL DISEASES

Brd4 Coactivates Transcriptional Activation of NF- B via Specific Binding to Acetylated RelA

(2008) B. Huang et al.   MOLECULAR AND CELLULAR BIOLOGY

Treatment of inflammatory bowel disease: A review of medical therapy

(2008) Patricia L Kozuch et al.   WORLD JOURNAL OF GASTROENTEROLOGY