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Article ; Online: Homo- and Heterodimerization of Proteins in Cell Signaling: Inhibition and Drug Design.

Singh, Sitanshu S / Jois, Seetharama D

Advances in protein chemistry and structural biology

2017 Volume 111, Page(s) 1–59

Abstract: Protein dimerization controls many physiological processes in the body. Proteins form homo-, hetero-, or oligomerization in the cellular environment to regulate the cellular processes. Any deregulation of these processes may result in a disease state. ... ...

Abstract	Protein dimerization controls many physiological processes in the body. Proteins form homo-, hetero-, or oligomerization in the cellular environment to regulate the cellular processes. Any deregulation of these processes may result in a disease state. Protein-protein interactions (PPIs) can be inhibited by antibodies, small molecules, or peptides, and inhibition of PPI has therapeutic value. PPI drug discovery research has steadily increased in the last decade, and a few PPI inhibitors have already reached the pharmaceutical market. Several PPI inhibitors are in clinical trials. With advancements in structural and molecular biology methods, several methods are now available to study protein homo- and heterodimerization and their inhibition by drug-like molecules. Recently developed methods to study PPI such as proximity ligation assay and enzyme-fragment complementation assay that detect the PPI in the cellular environment are described with examples. At present, the methods used to design PPI inhibitors can be classified into three major groups: (1) structure-based drug design, (2) high-throughput screening, and (3) fragment-based drug design. In this chapter, we have described some of the experimental methods to study PPIs and their inhibition. Examples of homo- and heterodimers of proteins, their structural and functional aspects, and some of the inhibitors that have clinical importance are discussed. The design of PPI inhibitors of epidermal growth factor receptor heterodimers and CD2-CD58 is discussed in detail.
MeSH term(s)	Drug Design ; Humans ; Proteins/analysis ; Proteins/antagonists & inhibitors ; Proteins/metabolism ; Signal Transduction/drug effects
Chemical Substances	Proteins
Language	English
Publishing date	2017-10-06
Publishing country	Netherlands
Document type	Journal Article ; Review
ISSN	1876-1631 ; 1876-1623
ISSN (online)	1876-1631
ISSN	1876-1623
DOI	10.1016/bs.apcsb.2017.08.003
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Article: Peptide-functionalized liposomes as therapeutic and diagnostic tools for cancer treatment

Sonju, Jafrin Jobayer / Dahal, Achyut / Singh, Sitanshu S / Jois, Seetharama D

Journal of controlled release. 2021 Jan. 10, v. 329

2021

Abstract: Clinically efficacious medication in anticancer therapy has been successfully designed with liposome-based nanomedicine. The liposomal formulation in cancer drug delivery can be facilitated with a functionalized peptide that mediates the specific drug ... ...

Abstract	Clinically efficacious medication in anticancer therapy has been successfully designed with liposome-based nanomedicine. The liposomal formulation in cancer drug delivery can be facilitated with a functionalized peptide that mediates the specific drug delivery opportunities with increased drug penetrability, specific accumulation in the targeted site, and enhanced therapeutic efficacy. This review aims to focus on recent advances in peptide-functionalized liposomal formulation techniques in cancer diagnosis and treatment regarding recently published literature. It also will highlight different aspects of novel liposomal formulation techniques that incorporate surface functionalization with peptides for better anticancer effect and current challenges in peptide-functionalized liposomal drug formulation.
Keywords	antineoplastic activity ; antineoplastic agents ; cancer therapy ; diagnostic techniques ; drug therapy ; nanomedicine ; neoplasms ; peptides
Language	English
Dates of publication	2021-0110
Size	p. 624-644.
Publishing place	Elsevier B.V.
Document type	Article
ZDB-ID	632533-6
ISSN	1873-4995 ; 0168-3659
ISSN (online)	1873-4995
ISSN	0168-3659
DOI	10.1016/j.jconrel.2020.09.055
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Article ; Online: Peptide-functionalized liposomes as therapeutic and diagnostic tools for cancer treatment.

Sonju, Jafrin Jobayer / Dahal, Achyut / Singh, Sitanshu S / Jois, Seetharama D

Journal of controlled release : official journal of the Controlled Release Society

2020 Volume 329, Page(s) 624–644

Abstract	Clinically efficacious medication in anticancer therapy has been successfully designed with liposome-based nanomedicine. The liposomal formulation in cancer drug delivery can be facilitated with a functionalized peptide that mediates the specific drug delivery opportunities with increased drug penetrability, specific accumulation in the targeted site, and enhanced therapeutic efficacy. This review aims to focus on recent advances in peptide-functionalized liposomal formulation techniques in cancer diagnosis and treatment regarding recently published literature. It also will highlight different aspects of novel liposomal formulation techniques that incorporate surface functionalization with peptides for better anticancer effect and current challenges in peptide-functionalized liposomal drug formulation.
MeSH term(s)	Antineoplastic Agents/therapeutic use ; Drug Delivery Systems ; Humans ; Liposomes/therapeutic use ; Neoplasms/drug therapy ; Peptides/therapeutic use
Chemical Substances	Antineoplastic Agents ; Liposomes ; Peptides
Language	English
Publishing date	2020-10-01
Publishing country	Netherlands
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Review
ZDB-ID	632533-6
ISSN	1873-4995 ; 0168-3659
ISSN (online)	1873-4995
ISSN	0168-3659
DOI	10.1016/j.jconrel.2020.09.055
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Article ; Online: A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.

Singh, Sitanshu S / Mattheolabakis, George / Gu, Xin / Withers, Sita / Dahal, Achyut / Jois, Seetharama

European journal of medicinal chemistry

2021 Volume 216, Page(s) 113312

Abstract: Among the lung cancers, approximately 85% are histologically classified as non-small-cell lung cancer (NSCLC), a leading cause of cancer deaths worldwide. Epidermal growth factor receptors (EGFRs) are known to play a crucial role in lung cancer. HER2 ... ...

Abstract	Among the lung cancers, approximately 85% are histologically classified as non-small-cell lung cancer (NSCLC), a leading cause of cancer deaths worldwide. Epidermal growth factor receptors (EGFRs) are known to play a crucial role in lung cancer. HER2 overexpression is detected by immunohistochemistry in 2.4%-38% of NSCLC samples. EGFRs have been targeted with three generations of tyrosine kinase inhibitors (TKIs), and drug resistance has become a major issue; HER2 dimerization with EGFR also plays a major role in the development of resistance to TKI therapy. We have designed grafted peptides to bind to the HER2 extracellular domain (ECD) and inhibit protein-protein interactions of EGFR:HER2 and HER2:HER3. A sunflower trypsin inhibitor (SFTI-1) template was used to graft a peptidomimetic compound. Among several grafted peptides, SFTI-G5 exhibited antiproliferative activity in HER2-positive NSCLC cell lines such as Calu-3 cells with an IC
MeSH term(s)	Animals ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dimerization ; Drug Design ; Drug Screening Assays, Antitumor ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Female ; Humans ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Mice ; Mice, Nude ; Peptides/chemistry ; Peptides/metabolism ; Peptidomimetics/chemistry ; Peptidomimetics/metabolism ; Peptidomimetics/pharmacology ; Peptidomimetics/therapeutic use ; Phosphorylation/drug effects ; Protein Interaction Domains and Motifs/drug effects ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Transplantation, Heterologous
Chemical Substances	Peptides ; Peptidomimetics ; Protein Kinase Inhibitors ; ErbB Receptors (EC 2.7.10.1)
Language	English
Publishing date	2021-02-23
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2021.113312
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Article ; Online: Mini-Review: PDPK1 (3-phosphoinositide dependent protein kinase-1), An Emerging Cancer Stem Cell Target.

Domrachev, Bogdan / Singh, Sitanshu / Li, Dandan / Rudloff, Udo

Journal of cancer treatment & diagnosis

2018 Volume 5, Issue 1, Page(s) 30–35

Abstract: Cancer stem cells (CSCs) are subpopulations of tumor cells that possess abilities for self-renewal, differentiation, and tumor initiation. These rare but therapy-recalcitrant cells are assumed to repopulate tumors following administration of systemic ... ...

Abstract	Cancer stem cells (CSCs) are subpopulations of tumor cells that possess abilities for self-renewal, differentiation, and tumor initiation. These rare but therapy-recalcitrant cells are assumed to repopulate tumors following administration of systemic chemotherapy driving therapy failure, tumor recurrence, and disease progression. In early clinical trials, anti-CSC therapies have found limited success to-date possibly due to the inherent heterogeneity and plasticity of CSCs and the incomplete characterization of essential CSC targets. Here, we review the role of 3-phosphoinositide dependent protein kinase-1 (PDPK1) as an emerging CSC target. While most previous studies have relied on CSC models which are based on lineage and tissue-specific marker profiles to define the relationships between putative target and CSC traits, this review discusses PDPK1 and its role in CSC biology with an emphasis on CSC systems which are based on proposed function like label-retaining cancer cells (LRCCs).
Language	English
Publishing date	2018-05-04
Publishing country	United States
Document type	Journal Article
ISSN	2578-2967
ISSN (online)	2578-2967
DOI	10.29245/2578-2967/2021/1.1194
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Article ; Online: Design of novel lipidated peptidomimetic conjugates for targeting EGFR heterodimerization in HER2 + cancer.

Naik, Himgauri / Gauthier, Ted / Singh, Sitanshu / Jois, Seetharama

Bioorganic & medicinal chemistry letters

2018 Volume 28, Issue 22, Page(s) 3506–3513

Abstract: The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. ...

Abstract	The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. Overexpression of these receptors is known to play a significant role in heterodimerization of these receptors leading to the development of cancer. We have designed peptidomimetic molecules to inhibit the EGFR heterodimerization interaction that have shown antiproliferative activity and specificity for HER2-positive cancer cell lines. Among these, a peptidomimetic, compound 5, exhibited antiproliferative activity at low nanomolar concentrations in HER2-overexpressing cancer cell lines. To improve the stability of this peptidomimetic, we have designed and synthesized a novel conjugate of peptidomimetic compound 5 with a lipid, stearic acid. The antiproliferative activity of this conjugate was evaluated in HER2-positive cancer cell lines. Results suggested that the conjugate exhibited selective antiproliferative activity in HER2-overexpressing breast and lung cancer cell lines and was able to block HER2:HER3 heterodimerization. Also, the conjugate showed improved stability with a half-life of 5 h in human serum compared to the half-life of 2 h for parent compound 5. The binding affinity of the conjugate to HER2 protein was evaluated by SPR analysis, and the mode of binding of the lipid conjugate to domain IV of HER2 protein was demonstrated by docking analysis. Thus, this novel lipid conjugate can be used to target HER2-overexpressing cancers.
MeSH term(s)	Binding Sites ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dimerization ; Drug Design ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Female ; Half-Life ; Humans ; Lung Neoplasms/metabolism ; Lung Neoplasms/pathology ; Molecular Docking Simulation ; Peptidomimetics/chemistry ; Peptidomimetics/metabolism ; Peptidomimetics/pharmacology ; Protein Binding ; Receptor, ErbB-3/antagonists & inhibitors ; Receptor, ErbB-3/metabolism ; Stearic Acids/chemistry ; Surface Plasmon Resonance
Chemical Substances	Peptidomimetics ; Stearic Acids ; stearic acid (4ELV7Z65AP) ; EGFR protein, human (EC 2.7.10.1) ; ErbB Receptors (EC 2.7.10.1) ; Receptor, ErbB-3 (EC 2.7.10.1)
Language	English
Publishing date	2018-10-03
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2018.10.005
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Article ; Online: Targeting protein-protein interaction for immunomodulation: A sunflower trypsin inhibitor analog peptidomimetic suppresses RA progression in CIA model.

Dahal, Achyut / Parajuli, Pravin / Singh, Sitanshu S / Shrestha, Leeza / Sonju, Jafrin Jobayer / Shrestha, Prajesh / Chatzistamou, Ioulia / Jois, Seetharama

Journal of pharmacological sciences

2022 Volume 149, Issue 3, Page(s) 124–138

Abstract: Protein-protein interactions (PPI) of co-stimulatory molecules CD2-CD58 are important in the early stage of an immune response, and increased expression of these co-stimulatory molecules is observed in the synovial region of joints in rheumatoid ... ...

Abstract	Protein-protein interactions (PPI) of co-stimulatory molecules CD2-CD58 are important in the early stage of an immune response, and increased expression of these co-stimulatory molecules is observed in the synovial region of joints in rheumatoid arthritis (RA) patients. A CD2 epitope region that binds to CD58 was grafted on to sunflower trypsin inhibitor (SFTI) template structure to inhibit CD2-CD58 PPI. The peptide was incorporated with an organic moiety dibenzofuran (DBF) in its structure. The designed peptidomimetic was studied for its ability to inhibit CD2-CD58 interactions in vitro, and its thermal and enzymatic stability was evaluated. Stability studies indicated that the grafted peptidomimetic was stable against trypsin cleavage. In vivo studies using the collagen-induced arthritis (CIA) model in mice indicated that the peptidomimetic was able to slow down the progress of arthritis, an autoimmune disease in the mice model. These studies suggest that with the grafting of organic functional groups in the stable peptide template SFTI stabilizes the peptide structure, and these peptides can be used as a template to design stable peptides for therapeutic purposes.
MeSH term(s)	Animals ; Arthritis, Experimental/drug therapy ; Arthritis, Rheumatoid/drug therapy ; CD58 Antigens/chemistry ; CD58 Antigens/metabolism ; Helianthus/chemistry ; Helianthus/metabolism ; Humans ; Immunity ; Immunomodulation ; Mice ; Peptides/pharmacology ; Peptides, Cyclic/metabolism ; Peptides, Cyclic/pharmacology ; Peptidomimetics/pharmacology ; Peptidomimetics/therapeutic use ; Trypsin Inhibitors/therapeutic use
Chemical Substances	CD58 Antigens ; Peptides ; Peptides, Cyclic ; Peptidomimetics ; Trypsin Inhibitors
Language	English
Publishing date	2022-04-25
Publishing country	Japan
Document type	Journal Article
ZDB-ID	2104264-0
ISSN	1347-8648 ; 1347-8613
ISSN (online)	1347-8648
ISSN	1347-8613
DOI	10.1016/j.jphs.2022.04.005
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Article ; Online: 1,3-diarylpyrazolones as potential anticancer agents for non-small cell lung cancer: Synthesis and antiproliferative activity evaluation.

Dahal, Achyut / Lo, Mary / Singh, Sitanshu / Vo, Huu / ElHage, Denzel / Jois, Seetharama D / Murru, Siva

Chemical biology & drug design

2022 Volume 99, Issue 4, Page(s) 620–633

Abstract: A series of pyrazolone compounds with different substitution patterns have been synthesized using microwave-assisted methods and evaluated their in vitro antiproliferative activity against human lung adenocarcinoma cell lines (A549 and NCI-H522). Among ... ...

Abstract	A series of pyrazolone compounds with different substitution patterns have been synthesized using microwave-assisted methods and evaluated their in vitro antiproliferative activity against human lung adenocarcinoma cell lines (A549 and NCI-H522). Among the tested compounds, the pyrazolone P7 exhibited high antiproliferative activity against both A549 and NCIH522 cancer cell lines while being 10 times less cytotoxic to non-cancerous cells. Moreover, our compounds P7 and P11 exhibited higher antiproliferative activity and selectivity against A549 and NCIH522 cells compared with the clinically approved drugs Afatinib and Gefitinib. The cell cycle analysis showed that the compound P7 and P11 arrests the cell cycle at G0/G1 phase, whereas the compounds P13 and P14 involved in G2/M phase arrest. The results from antiproliferative activity screening, cell cycle analysis, and kinase profiling indicate that the suitably substituted 1,3-diarylpyrazolones exhibit high antiproliferative activity against non-small cell lung cancer cells.
MeSH term(s)	Antineoplastic Agents ; Apoptosis ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/pathology ; Cell Line, Tumor ; Cell Proliferation ; Drug Screening Assays, Antitumor ; Humans ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Pyrazolones/pharmacology ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; Pyrazolones
Language	English
Publishing date	2022-03-01
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	2216600-2
ISSN	1747-0285 ; 1747-0277
ISSN (online)	1747-0285
ISSN	1747-0277
DOI	10.1111/cbdd.14030
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Article ; Online: Genotype Driven Therapy for Non-Small Cell Lung Cancer: Resistance, Pan Inhibitors and Immunotherapy.

Singh, Sitanshu S / Dahal, Achyut / Shrestha, Leeza / Jois, Seetharama D

Current medicinal chemistry

2019 Volume 27, Issue 32, Page(s) 5274–5316

Abstract: Eighty-five percent of patients with lung cancer present with Non-small Cell Lung Cancer (NSCLC). Targeted therapy approaches are promising treatments for lung cancer. However, despite the development of targeted therapies using Tyrosine Kinase ... ...

Abstract	Eighty-five percent of patients with lung cancer present with Non-small Cell Lung Cancer (NSCLC). Targeted therapy approaches are promising treatments for lung cancer. However, despite the development of targeted therapies using Tyrosine Kinase Inhibitors (TKI) as well as monoclonal antibodies, the five-year relative survival rate for lung cancer patients is still only 18%, and patients inevitably become resistant to therapy. Mutations in Kirsten Ras Sarcoma viral homolog (KRAS) and epidermal growth factor receptor (EGFR) are the two most common genetic events in lung adenocarcinoma; they account for 25% and 20% of cases, respectively. Anaplastic Lymphoma Kinase (ALK) is a transmembrane receptor tyrosine kinase, and ALK rearrangements are responsible for 3-7% of NSCLC, predominantly of the adenocarcinoma subtype, and occur in a mutually exclusive manner with KRAS and EGFR mutations. Among drug-resistant NSCLC patients, nearly half exhibit the T790M mutation in exon 20 of EGFR. This review focuses on some basic aspects of molecules involved in NSCLC, the development of resistance to treatments in NSCLC, and advances in lung cancer therapy in the past ten years. Some recent developments such as PD-1-PD-L1 checkpoint-based immunotherapy for NSCLC are also covered.
MeSH term(s)	Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/genetics ; ErbB Receptors/genetics ; Genotype ; Humans ; Immunotherapy ; Lung Neoplasms/drug therapy ; Lung Neoplasms/genetics ; Mutation ; Protein Kinase Inhibitors/therapeutic use
Chemical Substances	Protein Kinase Inhibitors ; ErbB Receptors (EC 2.7.10.1)
Language	English
Publishing date	2019-03-10
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	1319315-6
ISSN	1875-533X ; 0929-8673
ISSN (online)	1875-533X
ISSN	0929-8673
DOI	10.2174/0929867326666190222183219
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Article: Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy.

Naik, Himgauri / Sonju, Jafrin Jobayer / Singh, Sitanshu / Chatzistamou, Ioulia / Shrestha, Leeza / Gauthier, Ted / Jois, Seetharama

Pharmaceuticals (Basel, Switzerland)

2021 Volume 14, Issue 3

Abstract: The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer ... ...

Abstract	The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer cells. In this study, we prepared a peptidomimetic conjugate (SA-5)-tagged doxorubicin (Dox) incorporated liposome (LP) formulation (SA-5-Dox-LP) to evaluate the targeted delivery potential of SA-5 in human epidermal growth factor receptor-2 (HER2) overexpressed non-small-cell lung cancer (NSCLC) and breast cancer cell lines. The liposome was prepared using thin lipid film hydration and was characterized for particle size, encapsulation efficiency, cell viability, and targeted cellular uptake. In vivo evaluation of the liposomal formulation was performed in a mice model of NSCLC. The cell viability studies revealed that targeted SA-5-Dox-LP showed better antiproliferative activity than non-targeted Dox liposomes (Dox-LP). HER2-targeted liposome delivery showed selective cellular uptake compared to non-targeted liposomes on cancer cells. In vitro drug release studies indicated that Dox was released slowly from the formulations over 24 h, and there was no difference in Dox release between Dox-LP formulation and SA-5-Dox-LP formulation. In vivo studies in an NSCLC model of mice indicated that SA-5-Dox-LP could reduce the lung tumors significantly compared to vehicle control and Dox. In conclusion, this study demonstrated that the SA-5-Dox-LP liposome has the potential to increase therapeutic efficiency and targeted delivery of Dox in HER2 overexpressing cancer.
Language	English
Publishing date	2021-03-06
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph14030221
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