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Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases

Journal of medicinal chemistry, 2014-06, Vol.57 (12), p.5023-5038

2014

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JAK inhibition using tofacitinib for inflammatory bowel disease treatment: a hub for multiple inflammatory cytokines

American journal of physiology: Gastrointestinal and liver physiology, 2016-02, Vol.310 (3), p.G155-G162

2016

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The rationale for Janus kinase inhibitors for the treatment of spondyloarthritis

Rheumatology (Oxford, England), 2019-02, Vol.58 (2), p.197-205

2019

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Parsing the Interferon Transcriptional Network and Its Disease Associations

Cell, 2016-01, Vol.164 (3), p.564-578

2016

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Target Occupancy and Functional Inhibition of JAK3 and TEC Family Kinases by Ritlecitinib in Healthy Adults: An Open-Label, Phase 1 Study

Journal of clinical pharmacology, 2024-01, Vol.64 (1), p.67-79

2024

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Janus kinase inhibitors for the treatment of rheumatoid arthritis demonstrate similar profiles of in vitro cytokine receptor inhibition

Pharmacology research & perspectives, 2019-12, Vol.7 (6), p.e00537-n/a

2019

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Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10665-10699

2018

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Inhibition of T-cell activity in alopecia areata: recent developments and new directions

Frontiers in immunology, 2023, Vol.14, p.1243556-1243556

2023

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MAPKAP Kinase 2-Deficient Mice Are Resistant to Collagen-Induced Arthritis

Journal of Immunology, 2006-08, Vol.177 (3), p.1913-1917

2006

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The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis

Clinical and experimental rheumatology, 2016-03, Vol.34 (2), p.318

2016

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Distinct Cellular Functions of MK2

Molecular and Cellular Biology, 2002-07, Vol.22 (13), p.4827-4835

2002

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The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

Bioorganic & medicinal chemistry, 2021-01, Vol.29, p.115865-115865, Article 115865

2021

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Identification and SAR of a new series of thieno[3,2- d]pyrimidines as Tpl2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2011-10, Vol.21 (19), p.5952-5956

2011

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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.1130-1152

2018

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PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor

ACS chemical biology, 2019-06, Vol.14 (6), p.1235-1242

2019

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Pharmacologic Inhibition of Tpl2 Blocks Inflammatory Responses in Primary Human Monocytes, Synoviocytes, and Blood

The Journal of biological chemistry, 2007-11, Vol.282 (46), p.33295-33304

2007

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Network pharmacology of JAK inhibitors

Proceedings of the National Academy of Sciences - PNAS, 2016-08, Vol.113 (35), p.9852-9857

2016

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The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans

Drug metabolism and disposition, 2022-08, Vol.50 (8), p.1106-1118

2022

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Editorial: JAK inhibition in autoimmune and inflammatory diseases

Frontiers in immunology, 2022-12, Vol.13, p.1120281-1120281

2022

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Therapeutic Drug Monitoring for Current and Investigational Inflammatory Bowel Disease Treatments

Journal of clinical gastroenterology, 2021-03, Vol.55 (3), p.195-206

2021

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Hippocampus-dependent learning and memory is impaired in mice lacking the Ras-guanine-nucleotide releasing factor 1 (Ras-GRF1)

Neuropharmacology, 2001-11, Vol.41 (6), p.791-800

2001

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ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

ACS chemical biology, 2014-07, Vol.9 (7), p.1552-1558

2014

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Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells

ACS chemical biology, 2017-12, Vol.12 (12), p.2970-2974

2017

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Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases

JAK inhibition using tofacitinib for inflammatory bowel disease treatment: a hub for multiple inflammatory cytokines

The rationale for Janus kinase inhibitors for the treatment of spondyloarthritis

Parsing the Interferon Transcriptional Network and Its Disease Associations

Target Occupancy and Functional Inhibition of JAK3 and TEC Family Kinases by Ritlecitinib in Healthy Adults: An Open-Label, Phase 1 Study

Janus kinase inhibitors for the treatment of rheumatoid arthritis demonstrate similar profiles of in vitro cytokine receptor inhibition

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

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

Inhibition of T-cell activity in alopecia areata: recent developments and new directions

MAPKAP Kinase 2-Deficient Mice Are Resistant to Collagen-Induced Arthritis

The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis

Distinct Cellular Functions of MK2

The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

Identification and SAR of a new series of thieno[3,2- d]pyrimidines as Tpl2 kinase inhibitors

Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor

Pharmacologic Inhibition of Tpl2 Blocks Inflammatory Responses in Primary Human Monocytes, Synoviocytes, and Blood

Network pharmacology of JAK inhibitors

The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans

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

Editorial: JAK inhibition in autoimmune and inflammatory diseases

Therapeutic Drug Monitoring for Current and Investigational Inflammatory Bowel Disease Treatments

Hippocampus-dependent learning and memory is impaired in mice lacking the Ras-guanine-nucleotide releasing factor 1 (Ras-GRF1)

ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells

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