Combinatorial Approach to Improve Cancer Immunotherapy: Rational Drug Design Strategy to Simultaneously Hit Multiple Targets to Kill Tumor Cells and to Activate the Immune System

Dual inhibition of BRD4 and PI3K by SF2523 suppresses human prostate cancer cell growth in vitro and in vivo

(2018) Gang Shen et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Mechanisms of resistance to immune checkpoint inhibitors

(2018) Russell W Jenkins et al.   BRITISH JOURNAL OF CANCER

Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously

(2018) Jie Zang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Role of Immunotherapy in Head and Neck Cancer

(2018) Diane C. Ling et al.   SEMINARS IN RADIATION ONCOLOGY

Robust Antitumor Responses Result from Local Chemotherapy and CTLA-4 Blockade

(2018) Charlotte E. Ariyan et al.   Cancer Immunology Research

Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents

(2018) Shipeng He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of tranylcypromine derivatives as novel LSD1/HDACs dual inhibitors for cancer treatment

(2017) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Immunomodulation by ionizing radiation-impact for design of radio-immunotherapies and for treatment of inflammatory diseases

(2017) Benjamin Frey et al.   IMMUNOLOGICAL REVIEWS

Epigenetics and immunotherapy: The current state of play

(2017) Jennifer Dunn et al.   MOLECULAR IMMUNOLOGY

Tumour-associated macrophages as treatment targets in oncology

(2017) Alberto Mantovani et al.   Nature Reviews Clinical Oncology

Radiotherapy and immunotherapy: a beneficial liaison?

(2017) Ralph R. Weichselbaum et al.   Nature Reviews Clinical Oncology

Dual-activity PI3K–BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis

(2017) Forest H. Andrews et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Barriers to Radiation-Induced In Situ Tumor Vaccination

(2017) Erik Wennerberg et al.   Frontiers in Immunology

Discovery of Dual Inhibitors of MDM2 and XIAP for Cancer Treatment

(2016) Lubing Gu et al.   CANCER CELL

Phase I clinical trial of a five-peptide cancer vaccine combined with cyclophosphamide in advanced solid tumors

(2016) Mutsunori Murahashi et al.   CLINICAL IMMUNOLOGY

Radiotherapy and Immunotherapy Combinations in Non-small Cell Lung Cancer: A Promising Future?

(2016) G.G. Hanna et al.   CLINICAL ONCOLOGY

Immunogenic Chemotherapy Sensitizes Tumors to Checkpoint Blockade Therapy

(2016) Christina Pfirschke et al.   IMMUNITY

Resistance Mechanisms to Immune-Checkpoint Blockade in Cancer: Tumor-Intrinsic and -Extrinsic Factors

(2016) Jonathan M. Pitt et al.   IMMUNITY

BET bromodomain inhibition enhances T cell persistence and function in adoptive immunotherapy models

(2016) Yuki Kagoya et al.   JOURNAL OF CLINICAL INVESTIGATION

Combinatorial approach to cancer immunotherapy: strength in numbers

(2016) Anna E. Vilgelm et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Targeting tumour-associated macrophages with CCR2 inhibition in combination with FOLFIRINOX in patients with borderline resectable and locally advanced pancreatic cancer: a single-centre, open-label, dose-finding, non-randomised, phase 1b trial

(2016) Timothy M Nywening et al.   LANCET ONCOLOGY

Single Agent and Synergistic Activity of the "First-in-Class" Dual PI3K/BRD4 Inhibitor SF1126 with Sorafenib in Hepatocellular Carcinoma

(2016) A. R. Singh et al.   MOLECULAR CANCER THERAPEUTICS

Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells

(2016) Olivier De Henau et al.   NATURE

PI3Kγ is a molecular switch that controls immune suppression

(2016) Megan M. Kaneda et al.   NATURE

Association of high microvessel αvβ3 and low PTEN with poor outcome in stage 3 neuroblastoma: rationale for using first in class dual PI3K/BRD4 inhibitor, SF1126

(2016) Anat Erdreich-Epstein et al.   Oncotarget

BET Bromodomain Inhibition Promotes Anti-tumor Immunity by Suppressing PD-L1 Expression

(2016) Hengrui Zhu et al.   Cell Reports

Macrophages and Therapeutic Resistance in Cancer

(2015) Brian Ruffell et al.   CANCER CELL

Pan-PI-3 kinase inhibitor SF1126 shows antitumor and antiangiogenic activity in renal cell carcinoma

(2015) Shweta Joshi et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Immune modulation in advanced radiotherapies: Targeting out-of-field effects

(2015) Gerard G. Hanna et al.   CANCER LETTERS

Tadalafil Augments Tumor Specific Immunity in Patients with Head and Neck Squamous Cell Carcinoma

(2015) J. A. Califano et al.   CLINICAL CANCER RESEARCH

511 Updated results from a phase 1/2 study of epacadostat (INCB024360) in combination with ipilimumab in patients with metastatic melanoma

(2015) G. Gibney et al.   EUROPEAN JOURNAL OF CANCER

Colony stimulating factor 1 receptor inhibition delays recurrence of glioblastoma after radiation by altering myeloid cell recruitment and polarization

(2015) Jason H. Stafford et al.   NEURO-ONCOLOGY

Pembrolizumab for the Treatment of Non–Small-Cell Lung Cancer

(2015) Edward B. Garon et al.   NEW ENGLAND JOURNAL OF MEDICINE

Mutational landscape determines sensitivity to PD-1 blockade in non-small cell lung cancer

(2015) N. A. Rizvi et al.   SCIENCE

Bruton Tyrosine Kinase-Dependent Immune Cell Cross-talk Drives Pancreas Cancer

(2015) A. J. Gunderson et al.   Cancer Discovery

Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway

(2015) Michael Lahn et al.   Drug Design Development and Therapy

The Interplay of Immunotherapy and Chemotherapy: Harnessing Potential Synergies

(2015) Leisha A. Emens et al.   Cancer Immunology Research

Differential Activity of Nivolumab, Pembrolizumab and MPDL3280A according to the Tumor Expression of Programmed Death-Ligand-1 (PD-L1): Sensitivity Analysis of Trials in Melanoma, Lung and Genitourinary Cancers

(2015) Luisa Carbognin et al.   PLoS One

Targeting Tumor-Associated Macrophages with Anti-CSF-1R Antibody Reveals a Strategy for Cancer Therapy

(2014) Carola H. Ries et al.   CANCER CELL

Indoleamine 2,3-dioxygenase pathways of pathogenic inflammation and immune escape in cancer

(2014) George C. Prendergast et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Tumor-Associated Macrophages: From Mechanisms to Therapy

(2014) Roy Noy et al.   IMMUNITY

New and emerging HDAC inhibitors for cancer treatment

(2014) Alison C. West et al.   JOURNAL OF CLINICAL INVESTIGATION

Irradiation and anti–PD-L1 treatment synergistically promote antitumor immunity in mice

(2014) Liufu Deng et al.   JOURNAL OF CLINICAL INVESTIGATION

Gemcitabine and capecitabine with or without telomerase peptide vaccine GV1001 in patients with locally advanced or metastatic pancreatic cancer (TeloVac): an open-label, randomised, phase 3 trial

(2014) Gary Middleton et al.   LANCET ONCOLOGY

A Macrophage-Dominant PI3K Isoform Controls Hypoxia-Induced HIF1α and HIF2α Stability and Tumor Growth, Angiogenesis, and Metastasis

(2014) Shweta Joshi et al.   MOLECULAR CANCER RESEARCH

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

(2014) Pietro Ciceri et al.   Nature Chemical Biology

Disruption of CXCR2-Mediated MDSC Tumor Trafficking Enhances Anti-PD1 Efficacy

(2014) S. L. Highfill et al.   Science Translational Medicine

Carlumab, an anti-C-C chemokine ligand 2 monoclonal antibody, in combination with four chemotherapy regimens for the treatment of patients with solid tumors: an open-label, multicenter phase 1b study

(2014) Irene Brana et al.   Targeted Oncology

A Systemic Complete Response of Metastatic Melanoma to Local Radiation and Immunotherapy

(2014) Susan M. Hiniker et al.   Translational Oncology

Immune Cell-Poor Melanomas Benefit from PD-1 Blockade after Targeted Type I IFN Activation

(2014) T. Bald et al.   Cancer Discovery

Targeting tumor-associated macrophages in cancer therapy and understanding their complexity

(2014) Michael A. Cannarile et al.   OncoImmunology

Ipilimumab alone or in combination with radiotherapy in metastatic castration-resistant prostate cancer: results from an open-label, multicenter phase I/II study

(2013) S. F. Slovin et al.   ANNALS OF ONCOLOGY

Role of Macrophage Targeting in the Antitumor Activity of Trabectedin

(2013) Giovanni Germano et al.   CANCER CELL

A first-in-human, first-in-class, phase I study of carlumab (CNTO 888), a human monoclonal antibody against CC-chemokine ligand 2 in patients with solid tumors

(2013) Shahneen K. Sandhu et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Therapeutic regulation of myeloid-derived suppressor cells and immune response to cancer vaccine in patients with extensive stage small cell lung cancer

(2013) Cristina Iclozan et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Dendritic cell immunotherapy combined with gemcitabine chemotherapy enhances survival in a murine model of pancreatic carcinoma

(2013) Tomar Ghansah et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Chemoimmunotherapy: reengineering tumor immunity

(2013) Gang Chen et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

An Intact Immune System Is Required for the Anticancer Activities of Histone Deacetylase Inhibitors

(2013) A. C. West et al.   CANCER RESEARCH

Immune-based mechanisms of cytotoxic chemotherapy: implications for the design of novel and rationale-based combined treatments against cancer

(2013) L Bracci et al.   CELL DEATH AND DIFFERENTIATION

A Phase I Study of an Agonist CD40 Monoclonal Antibody (CP-870,893) in Combination with Gemcitabine in Patients with Advanced Pancreatic Ductal Adenocarcinoma

(2013) G. L. Beatty et al.   CLINICAL CANCER RESEARCH

Anti-PD-1 Blockade and Stereotactic Radiation Produce Long-Term Survival in Mice With Intracranial Gliomas

(2013) Jing Zeng et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

Indoleamine 2,3-dioxygenase is a critical resistance mechanism in antitumor T cell immunotherapy targeting CTLA-4

(2013) Rikke B. Holmgaard et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Synthesis and Cancer Stem Cell-Based Activity of Substituted 5-Morpholino-7H-thieno[3,2-b]pyran-7-ones Designed as Next Generation PI3K Inhibitors

(2013) Guillermo A. Morales et al.   JOURNAL OF MEDICINAL CHEMISTRY

CSF-1R inhibition alters macrophage polarization and blocks glioma progression

(2013) Stephanie M Pyonteck et al.   NATURE MEDICINE

Nivolumab plus Ipilimumab in Advanced Melanoma

(2013) Jedd D. Wolchok et al.   NEW ENGLAND JOURNAL OF MEDICINE

Anti-CCR4 mAb selectively depletes effector-type FoxP3+CD4+ regulatory T cells, evoking antitumor immune responses in humans

(2013) D. Sugiyama et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An Abscopal Response to Radiation and Ipilimumab in a Patient with Metastatic Non-Small Cell Lung Cancer

(2013) E. B. Golden et al.   Cancer Immunology Research

Ipilimumab in combination with paclitaxel and carboplatin as first-line therapy in extensive-disease-small-cell lung cancer: results from a randomized, double-blind, multicenter phase 2 trial†

(2012) M. Reck et al.   ANNALS OF ONCOLOGY

EZH2 inhibition: targeting the crossroad of tumor invasion and angiogenesis

(2012) Francesco Crea et al.   CANCER AND METASTASIS REVIEWS

Induction of Abscopal Anti-Tumor Immunity and Immunogenic Tumor Cell Death by Ionizing Irradiation - Implications for Cancer Therapies

(2012) B. Frey et al.   CURRENT MEDICINAL CHEMISTRY

The immunosuppressive tumour network: myeloid-derived suppressor cells, regulatory T cells and natural killer T cells

(2012) Dennis Lindau et al.   IMMUNOLOGY

Phase 2 study of carlumab (CNTO 888), a human monoclonal antibody against CC-chemokine ligand 2 (CCL2), in metastatic castration-resistant prostate cancer

(2012) Kenneth J. Pienta et al.   INVESTIGATIONAL NEW DRUGS

Ipilimumab in Combination With Paclitaxel and Carboplatin As First-Line Treatment in Stage IIIB/IV Non–Small-Cell Lung Cancer: Results From a Randomized, Double-Blind, Multicenter Phase II Study

(2012) Thomas J. Lynch et al.   JOURNAL OF CLINICAL ONCOLOGY

Intratumoral Injection of CpG Oligonucleotides Induces the Differentiation and Reduces the Immunosuppressive Activity of Myeloid-Derived Suppressor Cells

(2012) Y. Shirota et al.   JOURNAL OF IMMUNOLOGY

Multipeptide immune response to cancer vaccine IMA901 after single-dose cyclophosphamide associates with longer patient survival

(2012) Steffen Walter et al.   NATURE MEDICINE

Immunologic Correlates of the Abscopal Effect in a Patient with Melanoma

(2012) Michael A. Postow et al.   NEW ENGLAND JOURNAL OF MEDICINE

Safety and Activity of Anti–PD-L1 Antibody in Patients with Advanced Cancer

(2012) Julie R. Brahmer et al.   NEW ENGLAND JOURNAL OF MEDICINE

Safety, Activity, and Immune Correlates of Anti–PD-1 Antibody in Cancer

(2012) Suzanne L. Topalian et al.   NEW ENGLAND JOURNAL OF MEDICINE

Phase 1 Study of Stereotactic Body Radiotherapy and Interleukin-2--Tumor and Immunological Responses

(2012) S. K. Seung et al.   Science Translational Medicine

Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47

(2012) Joseph Weinstock et al.   ACS Medicinal Chemistry Letters

IDO Is a Nodal Pathogenic Driver of Lung Cancer and Metastasis Development

(2012) Courtney Smith et al.   Cancer Discovery

Targeting protein lysine methylation and demethylation in cancers

(2011) Yunlong He et al.   ACTA BIOCHIMICA ET BIOPHYSICA SINICA

A Lethally Irradiated Allogeneic Granulocyte-Macrophage Colony Stimulating Factor-Secreting Tumor Vaccine for Pancreatic Adenocarcinoma

(2011) Lutz Eric et al.   ANNALS OF SURGERY

Role of c-MYC in alternative activation of human macrophages and tumor-associated macrophage biology

(2011) O. M. Pello et al.   BLOOD

Coexpression of Tim-3 and PD-1 identifies a CD8+ T-cell exhaustion phenotype in mice with disseminated acute myelogenous leukemia

(2011) Q. Zhou et al.   BLOOD

Receptor Tyrosine Kinases and TLR/IL1Rs Unexpectedly Activate Myeloid Cell PI3Kγ, A Single Convergent Point Promoting Tumor Inflammation and Progression

(2011) Michael C. Schmid et al.   CANCER CELL

Immune Inhibitory Molecules LAG-3 and PD-1 Synergistically Regulate T-cell Function to Promote Tumoral Immune Escape

(2011) S.-R. Woo et al.   CANCER RESEARCH

Anti-PD-1 synergizes with cyclophosphamide to induce potent anti-tumor vaccine effects through novel mechanisms

(2011) Mikayel Mkrtichyan et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Immune parameters affecting the efficacy of chemotherapeutic regimens

(2011) Laurence Zitvogel et al.   Nature Reviews Clinical Oncology

Ipilimumab plus Dacarbazine for Previously Untreated Metastatic Melanoma

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

Chronic inflammation promotes myeloid-derived suppressor cell activation blocking antitumor immunity in transgenic mouse melanoma model

(2011) C. Meyer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Leukocyte Complexity Predicts Breast Cancer Survival and Functionally Regulates Response to Chemotherapy

(2011) David G. DeNardo et al.   Cancer Discovery

Monocyte Chemoattractant Protein–1 Blockade Inhibits Lung Cancer Tumor Growth by Altering Macrophage Phenotype and Activating CD8+Cells

(2010) Zvi G. Fridlender et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Myeloid-derived suppressor cells: more mechanisms for inhibiting antitumor immunity

(2010) Suzanne Ostrand-Rosenberg   CANCER IMMUNOLOGY IMMUNOTHERAPY

Local Radiation Therapy Inhibits Tumor Growth through the Generation of Tumor-Specific CTL: Its Potentiation by Combination with Th1 Cell Therapy

(2010) Tsuguhide Takeshima et al.   CANCER RESEARCH

Antitumor and Anti-inflammatory Effects of Trabectedin on Human Myxoid Liposarcoma Cells

(2010) G. Germano et al.   CANCER RESEARCH

Use of α,25-Dihydroxyvitamin D3 treatment to stimulate immune infiltration into head and neck squamous cell carcinoma

(2010) Jarrett E. Walsh et al.   HUMAN IMMUNOLOGY

Alternative Activation of Macrophages: Mechanism and Functions

(2010) Siamon Gordon et al.   IMMUNITY

Upregulation of Tim-3 and PD-1 expression is associated with tumor antigen–specific CD8+T cell dysfunction in melanoma patients

(2010) Julien Fourcade et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Chemotherapy Delivered After Viral Immunogene Therapy Augments Antitumor Efficacy Via Multiple Immune-mediated Mechanisms

(2010) Zvi G Fridlender et al.   MOLECULAR THERAPY

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Improved Survival with Ipilimumab in Patients with Metastatic Melanoma

(2010) F. Stephen Hodi et al.   NEW ENGLAND JOURNAL OF MEDICINE

PD-1 and CTLA-4 combination blockade expands infiltrating T cells and reduces regulatory T and myeloid cells within B16 melanoma tumors

(2010) M. A. Curran et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

T-cell modulation combined with intratumoral CpG cures lymphoma in a mouse model without the need for chemotherapy

(2008) R. Houot et al.   BLOOD

The effect of anti-VEGF therapy on immature myeloid cell and dendritic cells in cancer patients

(2008) Takuya Osada et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

A Vascular Targeted Pan Phosphoinositide 3-Kinase Inhibitor Prodrug, SF1126, with Antitumor and Antiangiogenic Activity

(2008) J. R. Garlich et al.   CANCER RESEARCH