Small Molecules Drive Big Improvements in Immuno-Oncology Therapies

Rationale for stimulator of interferon genes–targeted cancer immunotherapy

(2017) Thaiz Rivera Vargas et al.   EUROPEAN JOURNAL OF CANCER

Promising Targets for Cancer Immunotherapy: TLRs, RLRs, and STING-Mediated Innate Immune Pathways

(2017) Kai Li et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Effective combinatorial immunotherapy for castration-resistant prostate cancer

(2017) Xin Lu et al.   NATURE

Caffeine and Adenosine

(2017) Joaquim A. Ribeiro et al.   JOURNAL OF ALZHEIMERS DISEASE

Independent predictors of overall survival and recurrence in biphenotypic hepatocellular cancer.

(2017) Manik Amin et al.   JOURNAL OF CLINICAL ONCOLOGY

Tumoral Immune Cell Exploitation in Colorectal Cancer Metastases Can Be Targeted Effectively by Anti-CCR5 Therapy in Cancer Patients

(2016) Niels Halama et al.   CANCER CELL

CXCR2 Inhibition Profoundly Suppresses Metastases and Augments Immunotherapy in Pancreatic Ductal Adenocarcinoma

(2016) Colin W. Steele et al.   CANCER CELL

Cancer Immunotherapy: Selected Targets and Small-Molecule Modulators

(2016) Hilmar Weinmann   ChemMedChem

IDO1 inhibitors for cancer immunotherapy

(2016) S. Hatem   DRUGS OF THE FUTURE

Epigenetic modifiers in immunotherapy: a focus on checkpoint inhibitors

(2016) Manuela Terranova-Barberio et al.   Immunotherapy

The host STING pathway at the interface of cancer and immunity

(2016) Leticia Corrales et al.   JOURNAL OF CLINICAL INVESTIGATION

Change in Pattern ofHER2Fluorescent in Situ Hybridization (FISH) Results in Breast Cancers Submitted for FISH Testing: Experience of a Reference Laboratory Using US Food and Drug Administration Criteria and American Society of Clinical Oncology and College of American Pathologists Guidelines

(2016) Mithun Vinod Shah et al.   JOURNAL OF CLINICAL ONCOLOGY

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

PI3Kγ is a molecular switch that controls immune suppression

(2016) Megan M. Kaneda et al.   NATURE

Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy

(2016) Hong Jiang et al.   NATURE MEDICINE

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

(2016) Catherine A. Evans et al.   ACS Medicinal Chemistry Letters

Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)

(2016) Krzysztof M. Zak et al.   Oncotarget

Combination Approaches with Immune-Checkpoint Blockade in Cancer Therapy

(2016) Maarten Swart et al.   Frontiers in Oncology

Small Molecules for Immunomodulation in Cancer: A Review

(2015) Vidhya Iyer   Anti-Cancer Agents in Medicinal Chemistry

Topical resiquimod can induce disease regression and enhance T-cell effector functions in cutaneous T-cell lymphoma

(2015) A. H. Rook et al.   BLOOD

The BRAF and MEK Inhibitors Dabrafenib and Trametinib: Effects on Immune Function and in Combination with Immunomodulatory Antibodies Targeting PD-1, PD-L1, and CTLA-4

(2015) L. Liu et al.   CLINICAL CANCER RESEARCH

Cytosolic sensing of aberrant DNA: arming STING on the endoplasmic reticulum

(2015) Qiang Wang et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

History and Perspectives of A2AAdenosine Receptor Antagonists as Potential Therapeutic Agents

(2015) Delia Preti et al.   MEDICINAL RESEARCH REVIEWS

Big opportunities for small molecules in immuno-oncology

(2015) Jerry L. Adams et al.   NATURE REVIEWS DRUG DISCOVERY

Therapeutic antitumor immunity by checkpoint blockade is enhanced by ibrutinib, an inhibitor of both BTK and ITK

(2015) Idit Sagiv-Barfi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

On being less tolerant: Enhanced cancer immunosurveillance enabled by targeting checkpoints and agonists of T cell activation

(2015) Alexander M. Lesokhin et al.   Science Translational Medicine

Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1

(2015) Krzysztof M. Zak et al.   STRUCTURE

The Chemokine System in Innate Immunity

(2015) Caroline L. Sokol et al.   Cold Spring Harbor Perspectives in Biology

Direct Activation of STING in the Tumor Microenvironment Leads to Potent and Systemic Tumor Regression and Immunity

(2015) Leticia Corrales et al.   Cell Reports

Host A2B Adenosine Receptors Promote Carcinoma Growth

(2015) Sergey Ryzhov et al.   NEOPLASIA

Directing the Immune System with Chemical Compounds

(2014) Rock J. Mancini et al.   ACS Chemical Biology

A Phase I Dose-Finding Study of the Novel Toll-like Receptor 8 Agonist VTX-2337 in Adult Subjects with Advanced Solid Tumors or Lymphoma

(2014) D. W. Northfelt et al.   CLINICAL CANCER RESEARCH

Dabrafenib and Trametinib, Alone and in Combination for BRAF-Mutant Metastatic Melanoma

(2014) A. M. Menzies et al.   CLINICAL CANCER RESEARCH

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

Identification of LY2510924, a Novel Cyclic Peptide CXCR4 Antagonist That Exhibits Antitumor Activities in Solid Tumor and Breast Cancer Metastatic Models

(2014) S.-B. Peng et al.   MOLECULAR CANCER THERAPEUTICS

Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer

(2014) Khaled Ali et al.   NATURE

Eradication of metastatic mouse cancers resistant to immune checkpoint blockade by suppression of myeloid-derived cells

(2014) K. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chemokines in Cancer

(2014) M. T. Chow et al.   Cancer Immunology Research

Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1-selective pressure in T lymphocytes

(2013) J. A. Dubovsky et al.   BLOOD

CXCR2-Expressing Myeloid-Derived Suppressor Cells Are Essential to Promote Colitis-Associated Tumorigenesis

(2013) Hiroshi Katoh et al.   CANCER CELL

TLR agonists: our best frenemy in cancer immunotherapy

(2013) Sabina Kaczanowska et al.   JOURNAL OF LEUKOCYTE BIOLOGY

The Yin and Yang of Toll-like receptors in cancer

(2013) J-P Pradere et al.   ONCOGENE

Baseline tumor growth and immune control in laboratory mice are significantly influenced by subthermoneutral housing temperature

(2013) K. M. Kokolus et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Aldara activates TLR7-independent immune defence

(2013) Anne Walter et al.   Nature Communications

Small Molecule Inhibitors of CXCR4

(2013) Bikash Debnath et al.   Theranostics

Statistical issues and challenges in immuno-oncology

(2013) Tai-Tsang Chen   Journal for ImmunoTherapy of Cancer

STAT3-Driven Upregulation of TLR2 Promotes Gastric Tumorigenesis Independent of Tumor Inflammation

(2012) Hazel Tye et al.   CANCER CELL

Promotion of Hepatocellular Carcinoma by the Intestinal Microbiota and TLR4

(2012) Dianne H. Dapito et al.   CANCER CELL

Cancer Epigenetics: From Mechanism to Therapy

(2012) Mark A. Dawson et al.   CELL

New developments in Toll-like receptor targeted therapeutics

(2012) Dympna J Connolly et al.   CURRENT OPINION IN PHARMACOLOGY

Resiquimod, a topical drug for viral skin lesions and skin cancer

(2012) Thomas Meyer et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

The Chemokine Superfamily Revisited

(2012) Albert Zlotnik et al.   IMMUNITY

Toll-like receptor 7 regulates pancreatic carcinogenesis in mice and humans

(2012) Atsuo Ochi et al.   JOURNAL OF CLINICAL INVESTIGATION

Anticancer TLR agonists on the ropes

(2012) Malini Guha   NATURE REVIEWS DRUG DISCOVERY

Targeting the TGFβ signalling pathway in disease

(2012) Rosemary J. Akhurst et al.   NATURE REVIEWS DRUG DISCOVERY

IDO inhibits a tryptophan sufficiency signal that stimulates mTOR: A novel IDO effector pathway targeted by D-1-methyl-tryptophan

(2012) Richard Metz et al.   OncoImmunology

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

A dual CCR2/CCR5 chemokine antagonist, BMS-813160?

(2011) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Randomized Phase III Placebo-Controlled Trial of Carboplatin and Paclitaxel With or Without the Vascular Disrupting Agent Vadimezan (ASA404) in Advanced Non–Small-Cell Lung Cancer

(2011) Primo N. Lara et al.   JOURNAL OF CLINICAL ONCOLOGY

Principles and mechanisms of vessel normalization for cancer and other angiogenic diseases

(2011) Peter Carmeliet et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist

(2011) Chu-Biao Xue et al.   ACS Medicinal Chemistry Letters

Sorafenib reduces the percentage of tumour infiltrating regulatory T cells in renal cell carcinoma patients

(2010) Ingrid M.E. Desar et al.   INTERNATIONAL JOURNAL OF CANCER

Triggering of TLR7 and TLR8 expressed by human lung cancer cells induces cell survival and chemoresistance

(2010) Julien Cherfils-Vicini et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting Toll-like receptors: emerging therapeutics?

(2010) Elizabeth J. Hennessy et al.   NATURE REVIEWS DRUG DISCOVERY

TGF-β and immune cells: an important regulatory axis in the tumor microenvironment and progression

(2010) Li Yang et al.   TRENDS IN IMMUNOLOGY

Functional Anatomy of T Cell Activation and Synapse Formation

(2009) David R. Fooksman et al.   Annual Review of Immunology

Toll-like receptor agonists in cancer therapy

(2009) Sylvia Adams   Immunotherapy

Targeting the phosphoinositide 3-kinase pathway in cancer

(2009) Pixu Liu et al.   NATURE REVIEWS DRUG DISCOVERY

Synthesis and immunostimulatory properties of the phosphorothioate analogues of cdiGMP

(2008) Hongbin Yan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antagonists of the Human A2AAdenosine Receptor. 4. Design, Synthesis, and Preclinical Evaluation of 7-Aryltriazolo[4,5-d]pyrimidines

(2008) Roger J. Gillespie et al.   JOURNAL OF MEDICINAL CHEMISTRY

The PD-1/PD-L1 complex resembles the antigen-binding Fv domains of antibodies and T cell receptors

(2008) D. Y.-w. Lin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA