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Article ; Online: FS118, a Bispecific Antibody Targeting LAG-3 and PD-L1, Enhances T-Cell Activation Resulting in Potent Antitumor Activity.

Kraman, Matthew / Faroudi, Mustapha / Allen, Natalie L / Kmiecik, Katarzyna / Gliddon, Daniel / Seal, Claire / Koers, Alexander / Wydro, Mateusz M / Batey, Sarah / Winnewisser, Julia / Young, Lesley / Tuna, Mihriban / Doody, Jacqueline / Morrow, Michelle / Brewis, Neil

Clinical cancer research : an official journal of the American Association for Cancer Research

2020 Volume 26, Issue 13, Page(s) 3333–3344

Abstract: Purpose: Although programmed death-ligand 1 (PD-L1) antibody-based therapy has improved the outcome of patients with cancer, acquired resistance to these treatments limits their clinical efficacy. FS118 is a novel bispecific, tetravalent antibody (mAb!## ...

Abstract	Purpose: Although programmed death-ligand 1 (PD-L1) antibody-based therapy has improved the outcome of patients with cancer, acquired resistance to these treatments limits their clinical efficacy. FS118 is a novel bispecific, tetravalent antibody (mAb Experimental design: This study characterizes the binding activity and immune function of FS118 in cell lines and human peripheral blood mononuclear cells and further investigates its antitumor activity and mechanism of action using a surrogate murine bispecific antibody (mLAG-3/PD-L1 mAb Results: FS118 demonstrated simultaneous binding to LAG-3 and PD-L1 with high affinity and comparable or better activity than the combination of the single component parts of the mAb Conclusions: This study demonstrates a novel benefit of the bispecific approach over a combination of mAbs and supports the further development of FS118 for the treatment of patients with cancer.
MeSH term(s)	Animals ; Antibodies, Bispecific/pharmacology ; Antibody Affinity ; Antigens, CD/metabolism ; Antineoplastic Agents, Immunological/pharmacology ; B7-H1 Antigen/antagonists & inhibitors ; Biomarkers, Tumor ; Cell Line, Tumor ; Disease Models, Animal ; Humans ; Immunophenotyping ; Lymphocyte Activation/drug effects ; Lymphocyte Activation/immunology ; Mice ; Protein Binding ; T-Lymphocytes/drug effects ; T-Lymphocytes/immunology ; T-Lymphocytes/metabolism ; Xenograft Model Antitumor Assays
Chemical Substances	Antibodies, Bispecific ; Antigens, CD ; Antineoplastic Agents, Immunological ; B7-H1 Antigen ; Biomarkers, Tumor ; CD223 antigen ; CD274 protein, human
Language	English
Publishing date	2020-04-16
Publishing country	United States
Document type	Journal Article
ZDB-ID	1225457-5
ISSN	1557-3265 ; 1078-0432
ISSN (online)	1557-3265
ISSN	1078-0432
DOI	10.1158/1078-0432.CCR-19-3548
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Article ; Online: Generation of Fcabs targeting human and murine LAG-3 as building blocks for novel bispecific antibody therapeutics.

Everett, Katy L / Kraman, Matthew / Wollerton, Francisca P G / Zimarino, Carlo / Kmiecik, Katarzyna / Gaspar, Miguel / Pechouckova, Sarka / Allen, Natalie L / Doody, Jacqueline F / Tuna, Mihriban

Methods (San Diego, Calif.)

2018 Volume 154, Page(s) 60–69

Abstract: The immunoglobulin superfamily protein lymphocyte-activation gene 3 (LAG-3) participates in immune suppression and has been identified as a suitable target for cancer therapies. In order to generate bispecific antibodies targeting LAG-3, Fcabs (Fc-region ...

Abstract	The immunoglobulin superfamily protein lymphocyte-activation gene 3 (LAG-3) participates in immune suppression and has been identified as a suitable target for cancer therapies. In order to generate bispecific antibodies targeting LAG-3, Fcabs (Fc-region with antigen binding) targeting human and murine LAG-3 were generated from phage libraries. These Fcabs bind to LAG-3, inhibiting its interaction with MHC class II, and induce IL-2 production in a T cell assay. Bispecific antibodies, known as mAb
MeSH term(s)	Animals ; Antibodies, Bispecific ; Antigens, CD/immunology ; Humans ; Immunoglobulin Fc Fragments ; Macaca fascicularis/metabolism ; Mice ; Protein Engineering
Chemical Substances	Antibodies, Bispecific ; Antigens, CD ; CD223 antigen ; Immunoglobulin Fc Fragments
Language	English
Publishing date	2018-09-09
Publishing country	United States
Document type	Journal Article
ZDB-ID	1066584-5
ISSN	1095-9130 ; 1046-2023
ISSN (online)	1095-9130
ISSN	1046-2023
DOI	10.1016/j.ymeth.2018.09.003
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Zs.A 3239: Show issues

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Article: Synthesis of polysubstituted 4-fluoroquinolinones.

Kiselyov, Alexander S / Piatnitski, Evgueni L / Doody, Jacqueline

Organic letters

2004 Volume 6, Issue 22, Page(s) 4061–4063

Abstract: reaction: see text] A convenient one-pot synthesis of 4-fluoroquinolinones that are active against KDR kinase is described. The mechanism of the reaction is believed to involve the formation of a quinone methide intermediate. ...

Abstract	[reaction: see text] A convenient one-pot synthesis of 4-fluoroquinolinones that are active against KDR kinase is described. The mechanism of the reaction is believed to involve the formation of a quinone methide intermediate.
Language	English
Publishing date	2004-10-28
Publishing country	United States
Document type	Journal Article
ISSN	1523-7060
ISSN	1523-7060
DOI	10.1021/ol048257f
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Article: Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy.

Chekler, Eugene L Piatnitski / Kiselyov, Alexander S / Ouyang, Xiaohu / Chen, Xiaoling / Pattaropong, Vatee / Wang, Ying / Tuma, M Carolina / Doody, Jacqueline F

ACS medicinal chemistry letters

2010 Volume 1, Issue 9, Page(s) 488–492

Abstract: In an effort to develop potent, orally bioavailable compounds for the treatment of neoplastic diseases, we developed a class of dual VEGFR-2 kinase and tubulin inhibitors. Targeting the VEGFR receptor kinase and tubulin structure allows for inhibition of ...

Abstract	In an effort to develop potent, orally bioavailable compounds for the treatment of neoplastic diseases, we developed a class of dual VEGFR-2 kinase and tubulin inhibitors. Targeting the VEGFR receptor kinase and tubulin structure allows for inhibition of both tumor cells and tumor vasculature. Previously, a combination of two compounds, a VEGF receptor tyrosine kinase inhibitor and tubulin agent, was demonstrated to produce an enhanced antitumor response in animal studies. We have reaffirmed their results, with the added benefit that both activities are found in one compound.
Language	English
Publishing date	2010-08-20
Publishing country	United States
Document type	Journal Article
ISSN	1948-5875
ISSN	1948-5875
DOI	10.1021/ml1001568
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Article: Human single-domain neutralizing intrabodies directed against Etk kinase: a novel approach to impair cellular transformation.

Paz, Keren / Brennan, Laura A / Iacolina, Michelle / Doody, Jacqueline / Hadari, Yaron R / Zhu, Zhenping

Molecular cancer therapeutics

2005 Volume 4, Issue 11, Page(s) 1801–1809

Abstract: Etk, the 70-kDa member of the Tec family of nonreceptor protein tyrosine kinases, is expressed in a variety of hematopoietic, epithelial, and endothelial cells and was shown to be involved in several cellular processes, including proliferation, ... ...

Abstract	Etk, the 70-kDa member of the Tec family of nonreceptor protein tyrosine kinases, is expressed in a variety of hematopoietic, epithelial, and endothelial cells and was shown to be involved in several cellular processes, including proliferation, differentiation, and motility. In this study, we describe a novel approach using a human single-domain antibody phage display library for the generation of intrabodies directed against Etk. These single-domain antibodies bind specifically to recombinant Etk and efficiently block its kinase activity. When expressed in transformed cells, these antibodies associated tightly with Etk, leading to significant blockade of Etk enzymatic activity and inhibition of clonogenic cell growth in soft agar. Our results indicate that Etk may play a role in Src-induced cellular transformation and thus may represent a good target for cancer intervention. Furthermore, our single-domain antibody-based intrabody system proves to be an excellent tool for future intracellular targeting of other signaling molecules.
MeSH term(s)	Agar/chemistry ; Animals ; Antineoplastic Agents/pharmacology ; Blotting, Western ; Cell Differentiation ; Cell Proliferation ; Cell Transformation, Neoplastic/metabolism ; Cloning, Molecular ; DNA/chemistry ; Dose-Response Relationship, Drug ; Enzyme Activation ; Glutathione Transferase/metabolism ; Humans ; Immunoprecipitation ; Mice ; NIH 3T3 Cells ; Peptide Library ; Phosphorylation ; Protein Binding ; Protein Structure, Tertiary ; Protein-Tyrosine Kinases/chemistry ; Protein-Tyrosine Kinases/physiology ; RNA Interference ; Recombinant Proteins/chemistry ; Signal Transduction ; Transfection
Chemical Substances	Antineoplastic Agents ; Peptide Library ; Recombinant Proteins ; Agar (9002-18-0) ; DNA (9007-49-2) ; Glutathione Transferase (EC 2.5.1.18) ; BMX protein, human (EC 2.7.1.-) ; Protein-Tyrosine Kinases (EC 2.7.10.1)
Language	English
Publishing date	2005-11-07
Publishing country	United States
Document type	Journal Article
ZDB-ID	2063563-1
ISSN	1538-8514 ; 1535-7163
ISSN (online)	1538-8514
ISSN	1535-7163
DOI	10.1158/1535-7163.MCT-05-0174
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Article ; Online: Antitumor Activity of IMC-038525, a Novel Oral Tubulin Polymerization Inhibitor.

Tuma, Maria Carolina / Malikzay, Asra / Ouyang, Xiaohu / Surguladze, David / Fleming, James / Mitelman, Stan / Camara, Margarita / Finnerty, Bridget / Doody, Jacqueline / Chekler, Eugene L P / Kussie, Paul / Tonra, James R

Translational oncology

2010 Volume 3, Issue 5, Page(s) 318–325

Abstract: Microtubules are a well-validated target for anticancer therapy. Molecules that bind tubulin affect dynamic instability of microtubules causing mitotic arrest of proliferating cells, leading to cell death and tumor growth inhibition. Natural antitubulin ... ...

Abstract	Microtubules are a well-validated target for anticancer therapy. Molecules that bind tubulin affect dynamic instability of microtubules causing mitotic arrest of proliferating cells, leading to cell death and tumor growth inhibition. Natural antitubulin agents such as taxanes and Vinca alkaloids have been successful in the treatment of cancer; however, several limitations have encouraged the development of synthetic small molecule inhibitors of tubulin function. We have previously reported the discovery of two novel chemical series of tubulin polymerization inhibitors, triazoles (Ouyang et al. Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors. Bioorg Med Chem Lett. 2005; 15:5154-5159) and oxadiazole derivatives (Ouyang et al. Oxadiazole derivatives as a novel class of antimitotic agents: synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines. Bioorg Med Chem Lett. 2006; 16:1191-1196). Here, we report on the anticancer effects of a lead oxadiazole derivative in vitro and in vivo. In vitro, IMC-038525 caused mitotic arrest at nanomolar concentrations in epidermoid carcinoma and breast tumor cells, including multidrug-resistant cells. In vivo, IMC-038525 had a desirable pharmacokinetic profile with sustained plasma levels after oral dosing. IMC-038525 reduced subcutaneous xenograft tumor growth with significantly greater efficacy than the taxane paclitaxel. At efficacious doses, IMC-038525 did not cause substantial myelosuppression or peripheral neurotoxicity, as evaluated by neutrophil counts and changes in myelination of the sciatic nerve, respectively. These data indicate that IMC-038525 is a promising candidate for further development as a chemotherapeutic agent.
Language	English
Publishing date	2010-10-01
Publishing country	United States
Document type	Journal Article
ZDB-ID	2443840-6
ISSN	1936-5233 ; 1936-5233
ISSN (online)	1936-5233
ISSN	1936-5233
DOI	10.1593/tlo.10160
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Article ; Online: Tumor necrosis factor-alpha and interleukin-1 antagonists alleviate inflammatory skin changes associated with epidermal growth factor receptor antibody therapy in mice.

Surguladze, David / Deevi, Dhanvanthri / Claros, Nidia / Corcoran, Erik / Wang, Su / Plym, Mary Jane / Wu, Yan / Doody, Jacqueline / Mauro, David J / Witte, Larry / Busam, Klaus J / Pytowski, Bronek / Rodeck, Ulrich / Tonra, James R

Cancer research

2009 Volume 69, Issue 14, Page(s) 5643–5647

Abstract: Cancer patients receiving epidermal growth factor receptor (EGFR) antibody therapy often experience an acneiform rash of uncertain etiology in skin regions rich in pilosebaceous units. Currently, this condition is treated symptomatically with very ... ...

Abstract	Cancer patients receiving epidermal growth factor receptor (EGFR) antibody therapy often experience an acneiform rash of uncertain etiology in skin regions rich in pilosebaceous units. Currently, this condition is treated symptomatically with very limited, often anecdotal success. Here, we show that a monoclonal antibody targeting murine EGFR, ME1, caused a neutrophil-rich hair follicle inflammation in mice, similar to that reported in patients. This effect was preceded by the appearance of lipid-filled hair follicle distensions adjacent to enlarged sebaceous glands. The cytokine tumor necrosis factor-alpha (TNFalpha), localized immunohistochemically to this affected region of the pilosebaceous unit, was specifically up-regulated by ME1 in skin but not in other tissues examined. Moreover, skin inflammation was reduced by cotreatment with the TNFalpha signaling inhibitor, etanercept, indicating the involvement of TNFalpha in this inflammatory process. Interleukin-1, a cytokine that frequently acts in concert with TNFalpha, is also involved in this process given the efficacy of the interleukin-1 antagonist Kineret. Our results provide a mechanistic framework to develop evidence-based trials for EGFR antibody-induced skin rash in patients with cancer.
MeSH term(s)	Animals ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Antibodies, Monoclonal/adverse effects ; Antibodies, Monoclonal/therapeutic use ; Dermatitis/etiology ; Dermatitis/pathology ; Dermatitis/prevention & control ; Disease Models, Animal ; Enzyme-Linked Immunosorbent Assay ; Etanercept ; Exanthema/chemically induced ; Exanthema/prevention & control ; Female ; Humans ; Immunoglobulin G/pharmacology ; Interleukin 1 Receptor Antagonist Protein/pharmacology ; Interleukin-1/antagonists & inhibitors ; Interleukin-1/genetics ; Interleukin-1/metabolism ; Mice ; Mice, SCID ; Receptor, Epidermal Growth Factor/antagonists & inhibitors ; Receptor, Epidermal Growth Factor/immunology ; Receptors, Tumor Necrosis Factor ; Reverse Transcriptase Polymerase Chain Reaction ; Skin/drug effects ; Skin/metabolism ; Skin/pathology ; Tumor Necrosis Factor-alpha/antagonists & inhibitors ; Tumor Necrosis Factor-alpha/genetics ; Tumor Necrosis Factor-alpha/metabolism
Chemical Substances	Anti-Inflammatory Agents, Non-Steroidal ; Antibodies, Monoclonal ; Immunoglobulin G ; Interleukin 1 Receptor Antagonist Protein ; Interleukin-1 ; Receptors, Tumor Necrosis Factor ; Tumor Necrosis Factor-alpha ; Receptor, Epidermal Growth Factor (EC 2.7.10.1) ; Etanercept (OP401G7OJC)
Language	English
Publishing date	2009-07-15
Publishing country	United States
Document type	Journal Article
ZDB-ID	1432-1
ISSN	1538-7445 ; 0008-5472
ISSN (online)	1538-7445
ISSN	0008-5472
DOI	10.1158/0008-5472.CAN-09-0487
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Article ; Online: Synthesis and evaluation of heteroaryl-ketone derivatives as a novel class of VEGFR-2 inhibitors.

Piatnitski Chekler, Eugene L / Katoch-Rouse, Reeti / Kiselyov, Alexander S / Sherman, Dan / Ouyang, Xiaohu / Kim, Ki / Wang, Ying / Hadari, Yaron R / Doody, Jacqueline F

Bioorganic & medicinal chemistry letters

2008 Volume 18, Issue 15, Page(s) 4344–4347

Abstract: We have discovered novel inhibitors of VEGFR-2 kinase with low nanomolar potency in both enzymatic and cell-based assays. Active series are heteroaryl-ketone compounds containing a central aromatic ring with either an indazolyl or indolyl keto group in ... ...

Abstract	We have discovered novel inhibitors of VEGFR-2 kinase with low nanomolar potency in both enzymatic and cell-based assays. Active series are heteroaryl-ketone compounds containing a central aromatic ring with either an indazolyl or indolyl keto group in the ortho orientation to the benzylic amine group (Fig. 1). The best compounds were demonstrated to be inactive against a small select panel of tyrosine and serine/threonine kinases with the exception of VEGFR-1 kinase, a close family member. In addition, the lead candidate 8 displayed acceptable exposure levels when administered orally to mice.
MeSH term(s)	Administration, Oral ; Animals ; Combinatorial Chemistry Techniques ; Inhibitory Concentration 50 ; Ketones/chemical synthesis ; Ketones/chemistry ; Ketones/pharmacology ; Mice ; Molecular Structure ; Piperidines/pharmacology ; Quinazolines/pharmacology ; Structure-Activity Relationship ; Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors
Chemical Substances	Ketones ; Piperidines ; Quinazolines ; Vascular Endothelial Growth Factor Receptor-2 (EC 2.7.10.1) ; vandetanib (YO460OQ37K)
Language	English
Publishing date	2008-06-28
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2008.06.083
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Article: Inhibitory activity of cetuximab on epidermal growth factor receptor mutations in non small cell lung cancers.

Doody, Jacqueline F / Wang, Ying / Patel, Sheetal N / Joynes, Christopher / Lee, Sui Ping / Gerlak, Jason / Rolser, Robin L / Li, Yanxia / Steiner, Philipp / Bassi, Rajiv / Hicklin, Dan J / Hadari, Yaron R

Molecular cancer therapeutics

2007 Volume 6, Issue 10, Page(s) 2642–2651

Abstract: Mutations in the kinase domain of the epidermal growth factor receptor (EGFR) were identified in approximately 15% of all patients with non-small cell lung cancer (NSCLC). These mutations have been established as an indicator of superior response to ... ...

Abstract	Mutations in the kinase domain of the epidermal growth factor receptor (EGFR) were identified in approximately 15% of all patients with non-small cell lung cancer (NSCLC). These mutations have been established as an indicator of superior response to gefitinib and erlotinib, small molecule inhibitors of the EGFR kinase domain. Whether these mutations would also render patients more susceptible to treatment with cetuximab (Erbitux), an EGFR-neutralizing antibody, is yet to be determined. In this study, we attempted to evaluate the effect of cetuximab on several NSCLC lines harboring some of the more common EGFR mutations (L858R and delL747-T753insS), as well as the recently identified kinase inhibitor-resistant mutation, T790M. We could show that the kinase activity of the abovementioned EGFR mutants was hindered by cetuximab, as detected by both cell-based phosphorylation and proliferation assays. Interestingly, cetuximab also induced enhanced degradation of the EGFR mutants as compared with the wild-type receptor. Most importantly, cetuximab successfully inhibited the growth of NSCLC lines in xenograft models. These results indicate the promising potential of cetuximab as a regimen for patients with NSCLC bearing these mutations.
MeSH term(s)	Animals ; Antibodies, Monoclonal/pharmacology ; Antibodies, Monoclonal, Humanized ; Antineoplastic Agents/pharmacology ; Apoptosis ; Blotting, Western ; Carcinoma, Non-Small-Cell Lung/genetics ; Cell Line, Tumor ; Cetuximab ; Dimerization ; ErbB Receptors/genetics ; ErbB Receptors/metabolism ; Female ; Fluorescent Antibody Technique ; Humans ; Immunoblotting ; Immunoprecipitation ; Lung Neoplasms/genetics ; Mice ; Mice, Nude ; Mutation/drug effects ; Phosphorylation ; Protein Kinase Inhibitors/pharmacology ; Ubiquitin/metabolism
Chemical Substances	Antibodies, Monoclonal ; Antibodies, Monoclonal, Humanized ; Antineoplastic Agents ; Protein Kinase Inhibitors ; Ubiquitin ; ErbB Receptors (EC 2.7.10.1) ; Cetuximab (PQX0D8J21J)
Language	English
Publishing date	2007-10-03
Publishing country	United States
Document type	Journal Article
ZDB-ID	2063563-1
ISSN	1538-8514 ; 1535-7163
ISSN (online)	1538-8514
ISSN	1535-7163
DOI	10.1158/1535-7163.MCT-06-0506
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Article: Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.

Duncton, Matthew A J / Piatnitski, Evgueni L / Katoch-Rouse, Reeti / Smith, Leon M / Kiselyov, Alexander S / Milligan, Daniel L / Balagtas, Chris / Wong, Wai C / Kawakami, Joel / Doody, Jacqueline F

Bioorganic & medicinal chemistry letters

2006 Volume 16, Issue 6, Page(s) 1579–1581

Abstract: A novel class of 1-(isoquinolin-5-yl)-4-arylamino-phthalazines is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity with an IC(50) as low as 0.017 microM in an HTRF ... ...

Abstract	A novel class of 1-(isoquinolin-5-yl)-4-arylamino-phthalazines is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity with an IC(50) as low as 0.017 microM in an HTRF enzymatic assay. The compounds also inhibit VEGFR-1, a related tyrosine kinase.
MeSH term(s)	Fluoroimmunoassay ; Humans ; Inhibitory Concentration 50 ; Isoquinolines/chemical synthesis ; Isoquinolines/pharmacology ; Phthalazines/chemical synthesis ; Phthalazines/pharmacology ; Structure-Activity Relationship ; Vascular Endothelial Growth Factor Receptor-1/antagonists & inhibitors ; Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors
Chemical Substances	Isoquinolines ; Phthalazines ; Vascular Endothelial Growth Factor Receptor-1 (EC 2.7.10.1) ; Vascular Endothelial Growth Factor Receptor-2 (EC 2.7.10.1)
Language	English
Publishing date	2006-03-15
Publishing country	England
Document type	Journal Article
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2005.12.045
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