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Article: Novel Therapeutic Targets in Melanoma.

Cerezo, Michaël / Rocchi, Stéphane

2023 Volume 15, Issue 3

Abstract: Melanoma is the most aggressive skin cancer type and ranks amongst the deadliest cancers due to its ability to develop resistance to current therapies [ ... ]. ...

Abstract	Melanoma is the most aggressive skin cancer type and ranks amongst the deadliest cancers due to its ability to develop resistance to current therapies [...].
Language	English
Publishing date	2023-01-25
Publishing country	Switzerland
Document type	Editorial
ZDB-ID	2527080-1
ISSN	2072-6694
ISSN	2072-6694
DOI	10.3390/cancers15030747
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Article ; Online: Design, Synthesis and Biological Evaluation of Novel Anticancer Amidinourea Analogues via Unexpected 1,3,5-Triazin-2-one Ring Opening.

Grytsai, Oleksandr / Hamouda-Tekaya, Nedra / Botton, Thomas / Rocchi, Stéphane / Benhida, Rachid / Ronco, Cyril

ChemMedChem

2024 Volume 19, Issue 3, Page(s) e202300493

Abstract: Amidinoureas are an understudied class of molecules with unique structural properties and biological activities. A simple methodology has been developed for the synthesis of aliphatic substituted amidinoureas via unexpected cycle opening of benzothiazolo- ...

Abstract	Amidinoureas are an understudied class of molecules with unique structural properties and biological activities. A simple methodology has been developed for the synthesis of aliphatic substituted amidinoureas via unexpected cycle opening of benzothiazolo-1,3,5-triazine-2-ones and transamination reaction of N-(N-(benzo[d]thiazol-2-yl)carbamimidoyl)aniline-1-carboxamide in good yields. A novel series of amidinoureas derivatives was designed, synthesized, and evaluated for its antiproliferative activity on an aggressive metastatic melanoma A375 cell line model. This evaluation reveals antiproliferative activities in the low micromolar range and establishes a first structure-activity relationship. In addition, analogues selected for their structural diversity were assayed on a panel of cancer cell lines through the DTP-NCI60, on which they showed effectiveness on various cancer types, with promising activities on melanoma cells for two hit compounds. This work paves the way for further optimization of this family of compounds towards the development of potent antimelanoma agents.
MeSH term(s)	Humans ; Cell Line, Tumor ; Antineoplastic Agents/chemistry ; Triazines/chemistry ; Melanoma ; Structure-Activity Relationship ; Cell Proliferation ; Drug Screening Assays, Antitumor ; Molecular Structure ; Urea/analogs & derivatives ; Guanidine/analogs & derivatives
Chemical Substances	guanidine carboxamide (141-83-3) ; Antineoplastic Agents ; Triazines ; Urea (8W8T17847W) ; Guanidine (JU58VJ6Y3B)
Language	English
Publishing date	2024-01-15
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.202300493
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Article ; Online: Cancer cell metabolic reprogramming: a keystone for the response to immunotherapy.

Cerezo, Michaël / Rocchi, Stéphane

Cell death & disease

2020 Volume 11, Issue 11, Page(s) 964

Abstract: By targeting the tumor microenvironment to stimulate antitumor immunity, immunotherapies have revolutionized cancer treatment. However, many patients do not respond initially or develop secondary resistance. Based on the limited resources in the tumor ... ...

Abstract	By targeting the tumor microenvironment to stimulate antitumor immunity, immunotherapies have revolutionized cancer treatment. However, many patients do not respond initially or develop secondary resistance. Based on the limited resources in the tumor microenvironment and competition between tumor and immune cells, the field of immune metabolism has produced extensive knowledge showing that targeting metabolism could help to modulate antitumor immunity. However, among all the different potentially targetable metabolic pathways, it remains unclear which have more potential to overcome resistance to immune checkpoint inhibitors. Here, we explore metabolic reprogramming in cancer cells, which might inhibit antitumor immunity, and strategies that can be used to favor the antitumor response.
MeSH term(s)	Animals ; Cellular Reprogramming Techniques ; Humans ; Immunotherapy/methods ; Neoplasms/metabolism ; Neoplasms/therapy ; Tumor Microenvironment/immunology
Language	English
Publishing date	2020-11-11
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2541626-1
ISSN	2041-4889 ; 2041-4889
ISSN (online)	2041-4889
ISSN	2041-4889
DOI	10.1038/s41419-020-03175-5
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Article: Metformin: Focus on Melanoma.

Jaune, Emilie / Rocchi, Stéphane

Frontiers in endocrinology

2018 Volume 9, Page(s) 472

Abstract: Metformin is the most common biguanide used in the treatment of diabetes, with 120 million treated patients worldwide. Metformin decreases hyperglycemia without inducing hypoglycemia in diabetic patients and is very well tolerated. The principal effects ... ...

Abstract	Metformin is the most common biguanide used in the treatment of diabetes, with 120 million treated patients worldwide. Metformin decreases hyperglycemia without inducing hypoglycemia in diabetic patients and is very well tolerated. The principal effects of metformin are to decrease hepatic gluconeogenesis and increase glucose absorption by skeletal muscles. These effects are primarily due to metformin's action on mitochondria, which requires the activation of metabolic checkpoint AMP-activated protein kinase (AMPK). AMPK is implicated in several pathways, and following metformin activation, it decreases protein synthesis and cell proliferation. Many studies have examined the role of metformin in the regulation of cancer cells, particularly its effects on cancer cell proliferation and cell death. Encouraging results have been obtained in different types of cancers, including prostate, breast, lung, and skin cancers (melanoma). Furthermore, many retrospective epidemiological studies in diabetes patients have shown that metformin treatment decreased the risk of cancers compared with other antidiabetic treatments. In this review, we will discuss the effects of metformin on melanoma cells. Together, our novel data demonstrate the importance of developing metformin and new biguanide-derived compounds as potential treatments against a number of different cancers, particularly melanoma.
Language	English
Publishing date	2018-08-21
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2592084-4
ISSN	1664-2392
ISSN	1664-2392
DOI	10.3389/fendo.2018.00472
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Article ; Online: Biguanides drugs: Past success stories and promising future for drug discovery.

Grytsai, Oleksandr / Myrgorodska, Iuliia / Rocchi, Stéphane / Ronco, Cyril / Benhida, Rachid

European journal of medicinal chemistry

2021 Volume 224, Page(s) 113726

Abstract: Biguanides have attracted much attention a century ago and showed resurgent interest in recent years after a long period of dormancy. They constitute an important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. ... ...

Abstract	Biguanides have attracted much attention a century ago and showed resurgent interest in recent years after a long period of dormancy. They constitute an important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. Therapeutic indications of biguanides include antidiabetic, antimalarial, antiviral, antiplaque, and bactericidal applications. This review presents an extensive overview of the biological activity of biguanides and different mechanisms of action of currently marketed biguanide-containing drugs, as well as their pharmacological properties when applicable. We highlight the recent developments in research on biguanide compounds, with a primary focus on studies on metformin in the field of oncology. We aim to provide a critical overview of all main bioactive biguanide compounds and discuss future perspectives for the design of new drugs based on the biguanide fragment.
MeSH term(s)	Biguanides/pharmacology ; Biguanides/therapeutic use ; Drug Discovery/methods ; Humans ; Hypoglycemic Agents/pharmacology ; Hypoglycemic Agents/therapeutic use ; Molecular Structure
Chemical Substances	Biguanides ; Hypoglycemic Agents
Language	English
Publishing date	2021-07-29
Publishing country	France
Document type	Journal Article ; Review
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.2021.113726
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Article ; Online: Comment on 'Testing for BRAF fusions in patients with advanced BRAF/NRAS/KIT wild-type melanomas permits to identify patients who could benefit of anti-MEK targeted therapy'.

Botton, Thomas / Passeron, Thierry / Rocchi, Stéphane

Journal of clinical pathology

2019 Volume 73, Issue 8, Page(s) 524–525

MeSH term(s)	GTP Phosphohydrolases ; Humans ; Melanoma ; Membrane Proteins ; Proto-Oncogene Proteins B-raf
Chemical Substances	Membrane Proteins ; BRAF protein, human (EC 2.7.11.1) ; Proto-Oncogene Proteins B-raf (EC 2.7.11.1) ; GTP Phosphohydrolases (EC 3.6.1.-) ; NRAS protein, human (EC 3.6.1.-)
Language	English
Publishing date	2019-12-18
Publishing country	England
Document type	Letter ; Comment
ZDB-ID	80261-x
ISSN	1472-4146 ; 0021-9746
ISSN (online)	1472-4146
ISSN	0021-9746
DOI	10.1136/jclinpath-2019-206366
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Article ; Online: New anti-cancer molecules targeting HSPA5/BIP to induce endoplasmic reticulum stress, autophagy and apoptosis.

Cerezo, Michaël / Rocchi, Stéphane

Autophagy

2016 Volume 13, Issue 1, Page(s) 216–217

Abstract: Treatment of melanoma has significantly advanced over the last decade, with the development of targeted therapies against the MAPK pathway and immunotherapies to reactivate antitumor immunity. Unfortunately, currently more than 50% of patients are in ... ...

Abstract	Treatment of melanoma has significantly advanced over the last decade, with the development of targeted therapies against the MAPK pathway and immunotherapies to reactivate antitumor immunity. Unfortunately, currently more than 50% of patients are in treatment failure. Thus, identification of new common cellular vulnerability among melanoma cells is an urgent need and will help in the discovery of more efficient treatments against melanoma. We have focused our study on protein processing and have identified a new compound, HA15, targeting HSPA5/BiP, the master regulator of the unfolded protein response (UPR). By inhibiting HSPA5 specifically, our molecule increases the UPR and leads to the death of cancer cells by concomitant induction of autophagy and apoptosis, an effect seen both in vitro and in vivo. Our study provides compelling evidence to support the idea that endoplasmic reticulum (ER) stress inducers could be useful as a new therapeutic approach in melanoma treatment.
MeSH term(s)	Antineoplastic Agents/pharmacology ; Apoptosis ; Autophagy ; Cell Death ; Cell Line, Tumor ; Disease Progression ; Endoplasmic Reticulum/metabolism ; Endoplasmic Reticulum Chaperone BiP ; Endoplasmic Reticulum Stress ; Heat-Shock Proteins/antagonists & inhibitors ; Heat-Shock Proteins/metabolism ; Humans ; Melanoma/drug therapy ; Skin Neoplasms/drug therapy ; Structure-Activity Relationship ; Sulfonamides/chemistry ; Thiazoles/chemistry ; Unfolded Protein Response ; Benzenesulfonamides
Chemical Substances	Antineoplastic Agents ; Endoplasmic Reticulum Chaperone BiP ; HSPA5 protein, human ; Heat-Shock Proteins ; Sulfonamides ; Thiazoles
Language	English
Publishing date	2016-10-28
Publishing country	United States
Document type	Journal Article
ZDB-ID	2454135-7
ISSN	1554-8635 ; 1554-8627
ISSN (online)	1554-8635
ISSN	1554-8627
DOI	10.1080/15548627.2016.1246107
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Article ; Online: Increased Activation of Innate Immunity and Pro-Apoptotic CXCR3B in Normal-Appearing Skin on the Lesional Site of Patients with Segmental Vitiligo.

Passeron, Thierry / Malmqvst, Valentina E A / Bzioueche, Hanene / Marchetti, Sandrine / Rocchi, Stephane / Tulic, Meri K

The Journal of investigative dermatology

2021 Volume 142, Issue 2, Page(s) 480–483.e2

MeSH term(s)	Adult ; Apoptosis/immunology ; Biopsy ; Case-Control Studies ; Disease Progression ; Female ; Healthy Volunteers ; Humans ; Immunity, Innate ; Male ; Melanocytes/immunology ; Melanocytes/pathology ; Middle Aged ; Receptors, CXCR3/metabolism ; Skin/immunology ; Skin/metabolism ; Skin/pathology ; Vitiligo/immunology ; Vitiligo/pathology ; Young Adult
Chemical Substances	CXCR3 protein, human ; Receptors, CXCR3
Language	English
Publishing date	2021-07-31
Publishing country	United States
Document type	Letter ; Observational Study
ZDB-ID	80136-7
ISSN	1523-1747 ; 0022-202X
ISSN (online)	1523-1747
ISSN	0022-202X
DOI	10.1016/j.jid.2021.07.157
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Article ; Online: Impact of topical emollient, steroids alone or combined with calcipotriol, on the immune infiltrate and clinical outcome in psoriasis.

Heim, Marjorie / Irondelle, Marie / Duteil, Luc / Cardot-Leccia, Nathalie / Rocchi, Stéphane / Passeron, Thierry / Tulic, Meri K

Experimental dermatology

2022 Volume 31, Issue 11, Page(s) 1764–1778

Abstract: Psoriasis is a chronic inflammatory disease whereby long-term disease control remains a challenge for the patients. Latest evidence suggests that combined topical treatment with steroids and vitamin D analogue foam (Calcipotriol/Betamethasone) is ... ...

Abstract	Psoriasis is a chronic inflammatory disease whereby long-term disease control remains a challenge for the patients. Latest evidence suggests that combined topical treatment with steroids and vitamin D analogue foam (Calcipotriol/Betamethasone) is efficient in long-term management of the disease and reducing the number of relapses. Its effects on cellular inflammation and cytokine production remain to be explored. We set out to examine the effect of topical therapies on cellular infiltrate and cytokine profile in the lesional skin of psoriasis patients. This was a monocentric, double-blind, randomized trial with 30 patients. Patients were treated with the combined Calcipotriol/Betamethasone foam, Betamethasone foam alone, Clobetasol Propionate ointment or placebo. 4 mm skin biopsies from lesional and non-lesional sites were taken before and 4 weeks after treatment. Cellular infiltrate, IFNγ and IL-17 were studied by immunofluorescence. Each patient was their own control. Evolution in skin inflammation was studied in parallel with changes in patient's epidermal thickness and their tPASI clinical score. Lesional skin was characterized by increased epidermal thickness, increased number of IL-17 and IFNγ producing CD8+ T cells, NK cells and neutrophils. All treatment reduced epidermal thickness and improved patients tPASI scores. Only the combined Calcipotriol/Betamethasone foam completely abolished epidermal and dermal influx of CD8+ T cells, reduced number of CD8 + IFNγ+ cells (but not CD8 + IL-17+ cells) and significantly reduced the number of MPO+ neutrophils which were predominantly IL-17+. None of the treatments had effect on NK cells. We have shown the combined topical treatment with Calcipotriol/Betamethasone foam to be effective in reducing cellular influx into lesional skin of psoriasis patients and this effect to be superior to emollient or Betamethasone alone. Its previously described efficacy in the clinic may be attributed to its unique and rapid ability to inhibit both adaptive CD8+ T cell and innate immune neutrophilia influx into the skin, which was not observed for the other treatments.
MeSH term(s)	Humans ; Interleukin-17 ; Emollients/therapeutic use ; Ointments/therapeutic use ; Calcitriol ; Psoriasis/drug therapy ; Betamethasone/therapeutic use ; Inflammation/drug therapy
Chemical Substances	calcipotriene (143NQ3779B) ; Interleukin-17 ; Emollients ; Ointments ; Calcitriol (FXC9231JVH) ; Betamethasone (9842X06Q6M)
Language	English
Publishing date	2022-08-19
Publishing country	Denmark
Document type	Randomized Controlled Trial ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1130936-2
ISSN	1600-0625 ; 0906-6705
ISSN (online)	1600-0625
ISSN	0906-6705
DOI	10.1111/exd.14657
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Article ; Online: Sulfonylguanidine Derivatives as Potential Antimelanoma Agents.

Baladi, Tom / Hamouda-Tekaya, Nedra / Gonçalves, Leticia Christina Pires / Rocchi, Stéphane / Ronco, Cyril / Benhida, Rachid

ChemMedChem

2020 Volume 15, Issue 13, Page(s) 1113–1117

Abstract: Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2-Aminobenzazole-based structures are well employed in the development of new anticancer drugs. Two series of novel N- ... ...

Abstract	Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2-Aminobenzazole-based structures are well employed in the development of new anticancer drugs. Two series of novel N-benzazol-2-yl-N'-sulfonyl guanidine derivatives were synthesized with the sulfonylguanidine in either an extra- or intracyclic frame. They were evaluated for their antiproliferative activity against malignant melanoma tumor cells, thus allowing structure-activity relationships to be defined. Additionally, NCI-60 screening was performed for the best analogue to study its efficiency against a panel of other cancer cell lines. The stability profile of this promising compound was then validated. During the synthetic process, an unexpected new deamidination of the sulfonylguanidine towards sulfonamide function was also identified.
MeSH term(s)	Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Guanidine/analogs & derivatives ; Guanidine/chemical synthesis ; Guanidine/chemistry ; Guanidine/pharmacology ; Humans ; Hydrogen-Ion Concentration ; Melanoma/drug therapy ; Melanoma/pathology ; Molecular Docking Simulation ; Molecular Structure ; Skin Neoplasms/drug therapy ; Skin Neoplasms/pathology ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; sulfonylguanidine ; Guanidine (JU58VJ6Y3B)
Language	English
Publishing date	2020-05-12
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.202000218
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