List of works - Caroline J Springer

2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth

scientific article published on 04 September 2019

A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors

scientific article published in December 2015

A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.

scientific article

A phase I study of single administration of antibody-directed enzyme prodrug therapy with the recombinant anti-carcinoembryonic antigen antibody-enzyme fusion protein MFECP1 and a bis-iodo phenol mustard prodrug.

scientific article published in November 2006

Abstract 3704: Novel panRAF inhibitors active in melanomas that are resistant to BRAF-selective, or BRAF-selective/MEK inhibitor combinations

article

Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin

scientific article published on December 2005

Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships

scientific article published on 23 May 2019

Attenuated Salmonella targets prodrug activating enzyme carboxypeptidase G2 to mouse melanoma and human breast and colon carcinomas for effective suicide gene therapy

scientific article

B-RAF is a therapeutic target in melanoma

scientific article published on August 2004

BRAF as a therapeutic target: a patent review (2006 - 2012).

scientific article published on 07 January 2013

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring

scientific article

BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling

scientific article published on 25 March 2014

Bacterial-directed enzyme prodrug therapy.

scientific article published on 17 May 2013

C-end your drugs using peptide tags

article

Contrasting effects of sunitinib within in vivo models of metastasis

scientific article

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

article

Design of prodrugs for suicide gene therapy.

scientific article published on January 2004

Detection of the prodrug-activating enzyme carboxypeptidase G2 activity with chemical exchange saturation transfer magnetic resonance.

scientific article

Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group

scientific article

Gatekeeper mutations mediate resistance to BRAF-targeted therapies.

scientific article published on June 2010

Gene regulation in cancer gene therapy strategies

scientific article

Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen

scientific article published on 16 December 2005

In melanoma, RAS mutations are accompanied by switching signaling from BRAF to CRAF and disrupted cyclic AMP signaling

scientific article published on October 2006

Inducible expression of (V600E) Braf using tyrosinase-driven Cre recombinase results in embryonic lethality.

scientific article published on 11 December 2009

Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma

scientific article published on 14 December 2012

Introduction to the background, principles, and state of the art in suicide gene therapy.

scientific article

Introduction to vectors for suicide gene therapy.

scientific article published on January 2004

Investigating the Contribution of Collagen to the Tumor Biomechanical Phenotype with Noninvasive Magnetic Resonance Elastography

scientific article published on 11 October 2019

Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF

scientific article

Long functionalized poly(ethylene glycol)s of defined molecular weight: synthesis and application in solid-phase synthesis of conjugates.

scientific article published on 2 April 2008

Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface.

scientific article

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

scientific article

Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia

scientific article

Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors

scientific article published in August 2010

Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead

scientific article published in January 2006

Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold

scientific article

Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.

scientific article published in July 2009

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

scientific article

Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma

article

Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma

scientific article

Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents

scientific article published on 3 January 2013

Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma ⬇️

scientific article published on 20 October 2015

Primary melanoma of the CNS in children is driven by congenital expression of oncogenic NRAS in melanocytes.

scientific article published on 09 January 2013

Prodrug-activating systems in suicide gene therapy.

scientific article

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

scientific article published on April 2009

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors

scientific article published on January 2012

Self-immolative nitrogen mustards prodrugs cleavable by carboxypeptidase G2 (CPG2) showing large cytotoxicity differentials in GDEPT.

scientific article published on April 2003

Small molecule inhibitors of BRAF in clinical trials

scientific article published on 03 December 2011

Structure-activity relationship in cationic lipid mediated gene transfection.

scientific article

Suicide gene therapy of human colon carcinoma xenografts using an armed oncolytic adenovirus expressing carboxypeptidase G2.

scientific article published on May 2007

Synthesis of Novel Cationic Lipids: Effect of Structural Modification on the Efficiency of Gene Transfer ⬇️

scientific article published on January 3, 2002

Systemic gene-directed enzyme prodrug therapy of hepatocellular carcinoma using a targeted adenovirus armed with carboxypeptidase G2.

scientific article published on June 2005

Targeting the LOX/hypoxia axis reverses many of the features that make pancreatic cancer deadly: inhibition of LOX abrogates metastasis and enhances drug efficacy.

scientific article published on 15 June 2015

The EGF Receptor Hokey-Cokey

article

The emerging fields of suicide gene therapy and virotherapy.

scientific article

Topical 5-fluorouracil elicits regressions of BRAF inhibitor-induced cutaneous squamous cell carcinoma

scientific article published on 16 August 2012

V599EB-RAF is an oncogene in melanocytes

scientific article published on April 2004

Viral vectors for gene-directed enzyme prodrug therapy.

scientific article published on December 2006

List of works by Caroline J Springer

2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth

A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors

A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.

A phase I study of single administration of antibody-directed enzyme prodrug therapy with the recombinant anti-carcinoembryonic antigen antibody-enzyme fusion protein MFECP1 and a bis-iodo phenol mustard prodrug.

Abstract 3704: Novel panRAF inhibitors active in melanomas that are resistant to BRAF-selective, or BRAF-selective/MEK inhibitor combinations

Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin

Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships

Attenuated Salmonella targets prodrug activating enzyme carboxypeptidase G2 to mouse melanoma and human breast and colon carcinomas for effective suicide gene therapy

B-RAF is a therapeutic target in melanoma

BRAF as a therapeutic target: a patent review (2006 - 2012).

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring

BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling

Bacterial-directed enzyme prodrug therapy.

C-end your drugs using peptide tags

Contrasting effects of sunitinib within in vivo models of metastasis

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

Design of prodrugs for suicide gene therapy.

Detection of the prodrug-activating enzyme carboxypeptidase G2 activity with chemical exchange saturation transfer magnetic resonance.

Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group

Gatekeeper mutations mediate resistance to BRAF-targeted therapies.

Gene regulation in cancer gene therapy strategies

Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen

In melanoma, RAS mutations are accompanied by switching signaling from BRAF to CRAF and disrupted cyclic AMP signaling

Inducible expression of (V600E) Braf using tyrosinase-driven Cre recombinase results in embryonic lethality.

Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma

Introduction to the background, principles, and state of the art in suicide gene therapy.

Introduction to vectors for suicide gene therapy.

Investigating the Contribution of Collagen to the Tumor Biomechanical Phenotype with Noninvasive Magnetic Resonance Elastography

Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF

Long functionalized poly(ethylene glycol)s of defined molecular weight: synthesis and application in solid-phase synthesis of conjugates.

Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface.

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia

Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors

Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead

Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold

Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma

Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma

Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents

Preclinical Evidence That Trametinib Enhances the Response to Antiangiogenic Tyrosine Kinase Inhibitors in Renal Cell Carcinoma ⬇️

Primary melanoma of the CNS in children is driven by congenital expression of oncogenic NRAS in melanocytes.

Prodrug-activating systems in suicide gene therapy.

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors

Self-immolative nitrogen mustards prodrugs cleavable by carboxypeptidase G2 (CPG2) showing large cytotoxicity differentials in GDEPT.

Small molecule inhibitors of BRAF in clinical trials

Structure-activity relationship in cationic lipid mediated gene transfection.

Suicide gene therapy of human colon carcinoma xenografts using an armed oncolytic adenovirus expressing carboxypeptidase G2.

Synthesis of Novel Cationic Lipids: Effect of Structural Modification on the Efficiency of Gene Transfer ⬇️

Systemic gene-directed enzyme prodrug therapy of hepatocellular carcinoma using a targeted adenovirus armed with carboxypeptidase G2.

Targeting the LOX/hypoxia axis reverses many of the features that make pancreatic cancer deadly: inhibition of LOX abrogates metastasis and enhances drug efficacy.

The EGF Receptor Hokey-Cokey

The emerging fields of suicide gene therapy and virotherapy.

Topical 5-fluorouracil elicits regressions of BRAF inhibitor-induced cutaneous squamous cell carcinoma

V599EB-RAF is an oncogene in melanocytes

Viral vectors for gene-directed enzyme prodrug therapy.