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Cathepsin K Inhibitors for Osteoporosis: Biology, Potential Clinical Utility, and Lessons Learned

Endocrine reviews, 2017-08, Vol.38 (4), p.325-350

2017

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Tendon-derived cathepsin K-expressing progenitor cells activate Hedgehog signaling to drive heterotopic ossification

The Journal of clinical investigation, 2020-12, Vol.130 (12), p.6354-6365

2020

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The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K

Journal of the American Chemical Society, 2019-02, Vol.141 (8), p.3507-3514

2019

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Complexity of cancer protease biology: Cathepsin K expression and function in cancer progression

Seminars in cancer biology, 2015-12, Vol.35, p.71-84

2015

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Osteoclast-specific cathepsin K deletion stimulates S1P-dependent bone formation

The Journal of clinical investigation, 2013-02, Vol.123 (2), p.666-681

2013

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Inhibition of cathepsin K reduces cartilage degeneration in the anterior cruciate ligament transection rabbit and murine models of osteoarthritis

Bone (New York, N.Y.), 2012-06, Vol.50 (6), p.1250-1259

2012

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Cathepsin K-deficient osteocytes prevent lactation-induced bone loss and parathyroid hormone suppression

The Journal of clinical investigation, 2019-08, Vol.129 (8), p.3058-3071

2019

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Advances in the discovery of cathepsin K inhibitors on bone resorption

Journal of enzyme inhibition and medicinal chemistry, 2018-01, Vol.33 (1), p.890-904

2018

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Gut microbiota-stimulated cathepsin K secretion mediates TLR4-dependent M2 macrophage polarization and promotes tumor metastasis in colorectal cancer

Cell death and differentiation, 2019-11, Vol.26 (11), p.2447-2463

2019

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Emerging roles of cysteine cathepsins in disease and their potential as drug targets

Current pharmaceutical design, 2007-02, Vol.13 (4), p.387-403

2007

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A novel approach to inhibit bone resorption: exosite inhibitors against cathepsin K

British journal of pharmacology, 2016-01, Vol.173 (2), p.396-410

2016

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Increased Bone Resorption during Lactation in Pycnodysostosis

International journal of molecular sciences, 2021-02, Vol.22 (4), p.1810

2021

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Cathepsin K Controls Cortical Bone Formation by Degrading Periostin

Journal of bone and mineral research, 2017-07, Vol.32 (7), p.1432-1441

2017

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Novel selective proline-based peptidomimetics for human cathepsin K inhibition

Bioorganic & medicinal chemistry letters, 2024-09, Vol.110, p.129887, Article 129887

2024

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Pycnodysostosis in children and adults

Bone (New York, N.Y.), 2023-04, Vol.169, p.116674-116674, Article 116674

2023

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An Activity-Based Probe for Cathepsin K Imaging with Excellent Potency and Selectivity

Journal of medicinal chemistry, 2021-09, Vol.64 (18), p.13793-13806

2021

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Dipeptidyl peptidase‐4 disturbs adipocyte differentiation via the negative regulation of the glucagon‐like peptide‐1/adiponectin‐cathepsin K axis in mice under chronic stress conditions

The FASEB journal, 2024-05, Vol.38 (10), p.e23684-n/a

2024

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Inhibition of Ctsk modulates periodontitis with arthritis via downregulation of TLR9 and autophagy

Cell proliferation, 2020-01, Vol.53 (1), p.e12722-n/a

2020

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PDGF-BB secreted by preosteoclasts induces angiogenesis during coupling with osteogenesis

Nature medicine, 2014-11, Vol.20 (11), p.1270-1278

2014

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Human cathepsin X/Z is a biologically active homodimer

Biochimica et biophysica acta. Proteins and proteomics, 2021-02, Vol.1869 (2), p.140567-140567, Article 140567

2021

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Urolithin A suppresses RANKL-induced osteoclastogenesis and postmenopausal osteoporosis by, suppresses inflammation and downstream NF-κB activated pyroptosis pathways

Pharmacological research, 2021-12, Vol.174, p.105967-105967, Article 105967

2021

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Odanacatib for the treatment of postmenopausal osteoporosis: development history and design and participant characteristics of LOFT, the Long-Term Odanacatib Fracture Trial

Osteoporosis international, 2015-02, Vol.26 (2), p.699-712

2015

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Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor

Biochemical journal, 2015-01, Vol.465 (1), p.163-173

2015

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Ptpn11 deletion in a novel progenitor causes metachondromatosis by inducing hedgehog signalling

Nature (London), 2013-07, Vol.499 (7459), p.491-495

2013

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Breast cancer bone metastases: pathogenesis and therapeutic targets

The international journal of biochemistry & cell biology, 2018-03, Vol.96, p.63-78

2018

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Cathepsin K Inhibitors for Osteoporosis: Biology, Potential Clinical Utility, and Lessons Learned

Tendon-derived cathepsin K-expressing progenitor cells activate Hedgehog signaling to drive heterotopic ossification

The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K

Complexity of cancer protease biology: Cathepsin K expression and function in cancer progression

Osteoclast-specific cathepsin K deletion stimulates S1P-dependent bone formation

Inhibition of cathepsin K reduces cartilage degeneration in the anterior cruciate ligament transection rabbit and murine models of osteoarthritis

Cathepsin K-deficient osteocytes prevent lactation-induced bone loss and parathyroid hormone suppression

Advances in the discovery of cathepsin K inhibitors on bone resorption

Gut microbiota-stimulated cathepsin K secretion mediates TLR4-dependent M2 macrophage polarization and promotes tumor metastasis in colorectal cancer

Emerging roles of cysteine cathepsins in disease and their potential as drug targets

A novel approach to inhibit bone resorption: exosite inhibitors against cathepsin K

Increased Bone Resorption during Lactation in Pycnodysostosis

Cathepsin K Controls Cortical Bone Formation by Degrading Periostin

Novel selective proline-based peptidomimetics for human cathepsin K inhibition

Pycnodysostosis in children and adults

An Activity-Based Probe for Cathepsin K Imaging with Excellent Potency and Selectivity

Dipeptidyl peptidase‐4 disturbs adipocyte differentiation via the negative regulation of the glucagon‐like peptide‐1/adiponectin‐cathepsin K axis in mice under chronic stress conditions

Inhibition of Ctsk modulates periodontitis with arthritis via downregulation of TLR9 and autophagy

PDGF-BB secreted by preosteoclasts induces angiogenesis during coupling with osteogenesis

Human cathepsin X/Z is a biologically active homodimer

Urolithin A suppresses RANKL-induced osteoclastogenesis and postmenopausal osteoporosis by, suppresses inflammation and downstream NF-κB activated pyroptosis pathways

Odanacatib for the treatment of postmenopausal osteoporosis: development history and design and participant characteristics of LOFT, the Long-Term Odanacatib Fracture Trial

Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor

Ptpn11 deletion in a novel progenitor causes metachondromatosis by inducing hedgehog signalling

Breast cancer bone metastases: pathogenesis and therapeutic targets

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