Inhibition of farnesyl pyrophosphate (FPP) and/or geranylgeranyl pyrophosphate (GGPP) biosynthesis and its implication in the treatment of cancers

Preclinical investigation of a potent geranylgeranyl diphosphate synthase inhibitor

(2018) Staci L. Haney et al.   INVESTIGATIONAL NEW DRUGS

Unraveling the Prenylation-Cancer Paradox in Multiple Myeloma with Novel Geranylgeranyl Pyrophosphate Synthase (GGPPS) Inhibitors

(2018) Cyrus M. Lacbay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Isoprenoids and tau pathology in sporadic Alzheimer's disease

(2018) Sandra Pelleieux et al.   NEUROBIOLOGY OF AGING

Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration

(2018) Alexios N. Matralis et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase

(2017) Jaeok Park et al.   JOURNAL OF MEDICINAL CHEMISTRY

Senescent cells: an emerging target for diseases of ageing

(2017) Bennett G. Childs et al.   NATURE REVIEWS DRUG DISCOVERY

The Business of Anti-Aging Science

(2017) João Pedro de Magalhães et al.   TRENDS IN BIOTECHNOLOGY

Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product

(2017) Jaeok Park et al.   Nature Communications

Endoplasmic reticulum stress signaling and chemotherapy resistance in solid cancers

(2017) T Avril et al.   Oncogenesis

Zoledronic Acid Enhances Vδ2 T-Lymphocyte Antitumor Response to Human Glioma Cell Lines

(2017) E. Cimini et al.   INTERNATIONAL JOURNAL OF IMMUNOPATHOLOGY AND PHARMACOLOGY

Targeting protein geranylgeranylation slows tumor development in a murine model of prostate cancer metastasis

(2016) Jacqueline E. Reilly et al.   CANCER BIOLOGY & THERAPY

Statins Are Associated With Reduced Mortality in Multiple Myeloma

(2016) Kristen Marie Sanfilippo et al.   JOURNAL OF CLINICAL ONCOLOGY

Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase

(2015) Dimitrios Gritzalis et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pathogenesis beyond the cancer clone(s) in multiple myeloma

(2015) G. Bianchi et al.   BLOOD

Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding

(2015) Andreas L. Marzinzik et al.   ChemMedChem

Targeting geranylgeranylation reduces adrenal gland tumor burden in a murine model of prostate cancer metastasis

(2015) Jacqueline E. Reilly et al.   CLINICAL & EXPERIMENTAL METASTASIS

Targeting the isoprenoid pathway to abrogate progression of pulmonary fibrosis

(2015) Heather L. Osborn-Heaford et al.   FREE RADICAL BIOLOGY AND MEDICINE

Farnesyl Diphosphate Synthase Inhibitors With Unique Ligand-Binding Geometries

(2015) Yi-Liang Liu et al.   ACS Medicinal Chemistry Letters

Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase

(2015) Veronica S. Wills et al.   ACS Medicinal Chemistry Letters

How Do Bisphosphonates Inhibit Bone Metastasis In Vivo

(2015) Pierrick G. Fournier et al.   NEOPLASIA

Structure and Function of Human DnaJ Homologue Subfamily A Member 1 (DNAJA1) and Its Relationship to Pancreatic Cancer

(2014) Jaime L. Stark et al.   BIOCHEMISTRY

Airway mesenchymal cell death by mevalonate cascade inhibition: Integration of autophagy, unfolded protein response and apoptosis focusing on Bcl2 family proteins

(2014) Saeid Ghavami et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Geranyl and neryl triazole bisphosphonates as inhibitors of geranylgeranyl diphosphate synthase

(2014) Xiang Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Statins in oncological research: From experimental studies to clinical practice

(2014) Peter Kubatka et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Multistage Screening Reveals Chameleon Ligands of the Human Farnesyl Pyrophosphate Synthase: Implications to Drug Discovery for Neurodegenerative Diseases

(2014) Joris W. De Schutter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Protein Prenylation and Synaptic Plasticity: Implications for Alzheimer’s Disease

(2014) David A. Hottman et al.   MOLECULAR NEUROBIOLOGY

Chemistry: Chemical con artists foil drug discovery

(2014) Jonathan Baell et al.   NATURE

Metabolic control of YAP and TAZ by the mevalonate pathway

(2014) Giovanni Sorrentino et al.   NATURE CELL BIOLOGY

Zoledronic acid induces apoptosis and S-phase arrest in mesothelioma through inhibiting Rab family proteins and topoisomerase II actions

(2014) S Okamoto et al.   Cell Death & Disease

Structure of human farnesyl pyrophosphate synthase in complex with an aminopyridine bisphosphonate and two molecules of inorganic phosphate

(2014) Jaeok Park et al.   Acta Crystallographica Section F-Structural Biology Communications

Syntheses and characterization of non-bisphosphonate quinoline derivatives as new FPPS inhibitors

(2013) Jinggong Liu et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase—Parallel synthesis of analogs via a trimethylsilyl ylidene intermediate

(2013) Chun-Yuen Leung et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Thienopyrimidine Bisphosphonate (ThPBP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Optimization and Characterization of the Mode of Inhibition

(2013) Chun Yuen Leung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Expression of matrix macromolecules and functional properties of breast cancer cells are modulated by the bisphosphonate zoledronic acid

(2012) P.G. Dedes et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Dual Structure–Activity Relationship of Osteoclastogenesis Inhibitor Methyl Gerfelin Based on TEG Scanning

(2012) Naoki Kanoh et al.   BIOCONJUGATE CHEMISTRY

Design of potent bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase via targeted interactions with the active site ‘capping’ phenyls

(2012) Joris W. De Schutter et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Effects of induction and maintenance plus long-term bisphosphonates on bone disease in patients with multiple myeloma: the Medical Research Council Myeloma IX Trial

(2012) G. J. Morgan et al.   BLOOD

Drug response in a genetically engineered mouse model of multiple myeloma is predictive of clinical efficacy

(2012) M. Chesi et al.   BLOOD

In Vivo Phosphoantigen Levels in Bisphosphonate-Treated Human Breast Tumors Trigger V 9V 2 T-cell Antitumor Cytotoxicity through ICAM-1 Engagement

(2012) I. Benzaid et al.   CLINICAL CANCER RESEARCH

Design and Synthesis of Active Site Inhibitors of the Human Farnesyl Pyrophosphate Synthase: Apoptosis and Inhibition of ERK Phosphorylation in Multiple Myeloma Cells

(2012) Yih-Shyan Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lamin B1 loss is a senescence-associated biomarker

(2012) Adam Freund et al.   MOLECULAR BIOLOGY OF THE CELL

Brain Isoprenoids Farnesyl Pyrophosphate and Geranylgeranyl Pyrophosphate are Increased in Aged Mice

(2012) Gero P. Hooff et al.   MOLECULAR NEUROBIOLOGY

Statin Use and Reduced Cancer-Related Mortality

(2012) Sune F. Nielsen et al.   NEW ENGLAND JOURNAL OF MEDICINE

Zoledronic acid influences growth, migration and invasive activity of prostate cancer cells in vitro

(2012) J Mani et al.   PROSTATE CANCER AND PROSTATIC DISEASES

Altered expression of farnesyl pyrophosphate synthase in prostate cancer: evidence for a role of the mevalonate pathway in disease progression?

(2012) Tilman Todenhöfer et al.   WORLD JOURNAL OF UROLOGY

Apoptosis, autophagy and ER stress in mevalonate cascade inhibition-induced cell death of human atrial fibroblasts

(2012) S Ghavami et al.   Cell Death & Disease

Ternary complex structures of human farnesyl pyrophosphate synthase bound with a novel inhibitor and secondary ligands provide insights into the molecular details of the enzyme’s active site closure

(2012) Jaeok Park et al.   BMC STRUCTURAL BIOLOGY

Correlation between time-dependent inhibition of human farnesyl pyrophosphate synthase and blockade of mevalonate pathway by nitrogen-containing bisphosphonates in cultured cells

(2011) Johanna Räikkönen et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Bisphosphonates for postmenopausal osteoporosis

(2011) Richard Eastell et al.   BONE

The relationship between the chemistry and biological activity of the bisphosphonates

(2011) Frank H. Ebetino et al.   BONE

Bisphosphonates: The first 40years

(2011) R. Graham G. Russell   BONE

Indirect Stimulation of Human Vγ2Vδ2 T Cells through Alterations in Isoprenoid Metabolism

(2011) Hong Wang et al.   JOURNAL OF IMMUNOLOGY

Initial genome sequencing and analysis of multiple myeloma

(2011) Michael A. Chapman et al.   NATURE

Integrating the mechanisms of apoptosis induced by endoplasmic reticulum stress

(2011) Ira Tabas et al.   NATURE CELL BIOLOGY

Breast-Cancer Adjuvant Therapy with Zoledronic Acid

(2011) Robert E. Coleman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Regional bone metabolism at the lumbar spine and hip following discontinuation of alendronate and risedronate treatment in postmenopausal women

(2011) M. L. Frost et al.   OSTEOPOROSIS INTERNATIONAL

Role of Rab GTPases in Membrane Traffic and Cell Physiology

(2011) Alex H. Hutagalung et al.   PHYSIOLOGICAL REVIEWS

The Unfolded Protein Response: From Stress Pathway to Homeostatic Regulation

(2011) P. Walter et al.   SCIENCE

Isoprenoids, small GTPases and Alzheimer's disease

(2010) Gero P. Hooff et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Synthesis and biological evaluation of a series of aromatic bisphosphonates

(2010) Rocky J. Barney et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and preliminary pharmacological characterisation of a new class of nitrogen-containing bisphosphonates (N-BPs)

(2010) Marco L. Lolli et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase

(2010) Joris W. De Schutter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Biochemical and molecular mechanisms of action of bisphosphonates

(2010) Michael J. Rogers et al.   BONE

An in vitro Assay to Measure Targeted Drug Delivery to Bone Mineral

(2010) Wolfgang Jahnke et al.   ChemMedChem

Molecular Targets of the Nitrogen Containing Bisphosphonates: The Molecular Pharmacology of Prenyl Synthase Inhibition

(2010) J. E. Dunford   CURRENT PHARMACEUTICAL DESIGN

Pamidronate inhibits antiapoptotic bcl-2 expression through inhibition of the mevalonate pathway in prostate cancer PC-3 cells

(2010) Kazuhiro Iguchi et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Geranylgeranyl diphosphate depletion inhibits breast cancer cell migration

(2010) Amel Dudakovic et al.   INVESTIGATIONAL NEW DRUGS

Molecular Characterization of a Novel Geranylgeranyl Pyrophosphate Synthase fromPlasmodiumParasites

(2010) Jennifer D. Artz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Delivery of zoledronic acid encapsulated in folate-targeted liposome results in potent in vitro cytotoxic activity on tumor cells

(2010) Hilary Shmeeda et al.   JOURNAL OF CONTROLLED RELEASE

First-line treatment with zoledronic acid as compared with clodronic acid in multiple myeloma (MRC Myeloma IX): a randomised controlled trial

(2010) Gareth J Morgan et al.   LANCET

Isoprenoid biosynthetic pathway inhibition disrupts monoclonal protein secretion and induces the unfolded protein response pathway in multiple myeloma cells

(2010) Sarah A. Holstein et al.   LEUKEMIA RESEARCH

Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery

(2010) Wolfgang Jahnke et al.   Nature Chemical Biology

The HSP70 chaperone machinery: J proteins as drivers of functional specificity

(2010) Harm H. Kampinga et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Zoledronate Stimulates γδ T Cells in Prostate Cancer Patients

(2010) Michio Naoe et al.   ONCOLOGY RESEARCH

Dysregulation of the mevalonate pathway promotes transformation

(2010) J. W. Clendening et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lipophilic Pyridinium Bisphosphonates: Potent γδT Cell Stimulators

(2009) Yonghui Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Mevalonate pathway intermediates downregulate zoledronic acid-induced isopentenyl pyrophosphate and ATP analog formation in human breast cancer cells

(2009) Johanna Räikkönen et al.   BIOCHEMICAL PHARMACOLOGY

The level of ATP analog and isopentenyl pyrophosphate correlates with zoledronic acid-induced apoptosis in cancer cells in vitro

(2009) Laura M. Mitrofan et al.   BONE

Fluvastatin reduces proliferation and increases apoptosis in women with high grade breast cancer

(2009) Elisabeth R. Garwood et al.   BREAST CANCER RESEARCH AND TREATMENT

Phase II Trial of Tipifarnib plus Neoadjuvant Doxorubicin-Cyclophosphamide in Patients with Clinical Stage IIB-IIIC Breast Cancer

(2009) J. A. Sparano et al.   CLINICAL CANCER RESEARCH

The bisphosphonate zoledronic acid has antimyeloma activityin vivoby inhibition of protein prenylation

(2009) Andreas Guenther et al.   INTERNATIONAL JOURNAL OF CANCER

Reduced Expression of the Mevalonate Pathway Enzyme Farnesyl Pyrophosphate Synthase Unveils Recognition of Tumor Cells by V 9V 2 T Cells

(2009) J. Li et al.   JOURNAL OF IMMUNOLOGY

Lipophilic Bisphosphonates as Dual Farnesyl/Geranylgeranyl Diphosphate Synthase Inhibitors: An X-ray and NMR Investigation

(2009) Yonghui Zhang et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Analysis of the eukaryotic prenylome by isoprenoid affinity tagging

(2009) Uyen T T Nguyen et al.   Nature Chemical Biology

Regulation of the brain isoprenoids farnesyl- and geranylgeranylpyrophosphate is altered in male Alzheimer patients

(2009) Gunter P. Eckert et al.   NEUROBIOLOGY OF DISEASE

Endocrine Therapy plus Zoledronic Acid in Premenopausal Breast Cancer

(2009) Michael Gnant et al.   NEW ENGLAND JOURNAL OF MEDICINE

Reduction of osteonecrosis of the jaw (ONJ) after implementation of preventive measures in patients with multiple myeloma treated with zoledronic acid

(2008) M. A. Dimopoulos et al.   ANNALS OF ONCOLOGY

Decreased occurrence of osteonecrosis of the jaw after implementation of dental preventive measures in solid tumour patients with bone metastases treated with bisphosphonates. The experience of the National Cancer Institute of Milan

(2008) C. I. Ripamonti et al.   ANNALS OF ONCOLOGY

Osteonecrosis of the jaw and bisphosphonate treatment for osteoporosis

(2008) René Rizzoli et al.   BONE

HMG-CoA reductase inhibitors activate the unfolded protein response and induce cytoprotective GRP78 expression

(2008) Jui-Ching Chen et al.   CARDIOVASCULAR RESEARCH

Biodistribution and Plasma Protein Binding of Zoledronic Acid

(2008) H. M. Weiss et al.   DRUG METABOLISM AND DISPOSITION

Frequency and Risk Factors Associated With Osteonecrosis of the Jaw in Cancer Patients Treated With Intravenous Bisphosphonates

(2008) Ana O Hoff et al.   JOURNAL OF BONE AND MINERAL RESEARCH

The Antiresorptive Effects of a Single Dose of Zoledronate Persist for Two Years: A Randomized, Placebo-Controlled Trial in Osteopenic Postmenopausal Women

(2008) Andrew Grey et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Design, Synthesis, and Biological Evaluation of Novel Aminobisphosphonates Possessing an in Vivo Antitumor Activity Through a γδ-T Lymphocytes-Mediated Activation Mechanism

(2008) Daniele Simoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of Geranylgeranyl Diphosphate Synthase by Bisphosphonates: A Crystallographic and Computational Investigation†

(2008) Michael P. Hudock et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationships Among the Nitrogen Containing Bisphosphonates in Clinical Use and Other Analogues: Time-Dependent Inhibition of Human Farnesyl Pyrophosphate Synthase

(2008) James E. Dunford et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structures of a potent phenylalkyl bisphosphonate inhibitor bound to farnesyl and geranylgeranyl diphosphate synthases

(2008) Rong Cao et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS