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Article ; Online: Evaluation of a hapten conjugate vaccine against the "zombie drug" xylazine.

Lin, Mingliang / Eubanks, Lisa M / Zhou, Bin / Janda, Kim D

Chemical communications (Cambridge, England)

2024 Volume 60, Issue 35, Page(s) 4711–4714

Abstract: Xylazine has emerged as a primary adulterant in fentanyl, exacerbating the complexity of the opioid crisis. Yet, there is no approved drug that can reverse xylazine's pathophysiology. As a prelude to monoclonal antibodies being assessed as a viable ... ...

Abstract	Xylazine has emerged as a primary adulterant in fentanyl, exacerbating the complexity of the opioid crisis. Yet, there is no approved drug that can reverse xylazine's pathophysiology. As a prelude to monoclonal antibodies being assessed as a viable therapeutic, a vaccine inquiry was conducted evaluating the immune response in reversing xylazine induced behavior effects.
MeSH term(s)	Xylazine/chemistry ; Xylazine/pharmacology ; Haptens/chemistry ; Haptens/immunology ; Animals ; Vaccines, Conjugate/chemistry ; Vaccines, Conjugate/immunology ; Mice
Chemical Substances	Xylazine (2KFG9TP5V8) ; Haptens ; Vaccines, Conjugate
Language	English
Publishing date	2024-04-25
Publishing country	England
Document type	Journal Article
ZDB-ID	1472881-3
ISSN	1364-548X ; 1359-7345 ; 0009-241X
ISSN (online)	1364-548X
ISSN	1359-7345 ; 0009-241X
DOI	10.1039/d4cc00883a
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Demystifying the Druggability of the MYC Family of Oncogenes.

Karadkhelkar, Nishant M / Lin, Mingliang / Eubanks, Lisa M / Janda, Kim D

Journal of the American Chemical Society

2023 Volume 145, Issue 6, Page(s) 3259–3269

Abstract: The MYC family of oncogenes (MYC, MYCN, and MYCL) encodes a basic helix-loop-helix leucine zipper (bHLHLZ) transcriptional regulator that is responsible for moving the cell through the restriction point. Through the HLHZIP domain, MYC heterodimerizes ... ...

Abstract	The MYC family of oncogenes (MYC, MYCN, and MYCL) encodes a basic helix-loop-helix leucine zipper (bHLHLZ) transcriptional regulator that is responsible for moving the cell through the restriction point. Through the HLHZIP domain, MYC heterodimerizes with the bHLHLZ protein MAX, which enables this MYC-MAX complex to bind to E-box regulatory DNA elements thereby controlling transcription of a large group of genes and their proteins. Translationally, MYC is one of the foremost oncogenic targets, and deregulation of expression of the MYC family gene/proteins occurs in over half of all human tumors and is recognized as a hallmark of cancer initiation and maintenance. Additionally, unexpected roles for this oncoprotein have been found in cancers that nominally have a non-MYC etiology. Although MYC is rarely mutated, its gain of function in cancer results from overexpression or from amplification. Moreover, MYC is a pleiotropic transcription factor possessing broad pathogenic prominence making it a coveted cancer target. A widely held notion within the biomedical research community is that the reliable modulation of MYC represents a tremendous therapeutic opportunity given its role in directly potentiating oncogenesis. However, the MYC-MAX heterodimer interaction contains a large surface area with a lack of well-defined binding sites creating the perception that targeting of MYC-MAX is forbidding. Here, we discuss the biochemistry behind MYC and MYC-MAX as it relates to cancer progression associated with these transcription factors. We also discuss the notion that MYC should no longer be regarded as undruggable, providing examples that a therapeutic window is achievable despite global MYC inhibition.
MeSH term(s)	Humans ; Basic Helix-Loop-Helix Leucine Zipper Transcription Factors/genetics ; Proto-Oncogene Proteins c-myc/chemistry ; Transcription Factors/metabolism ; Oncogenes ; Neoplasms/drug therapy ; Neoplasms/genetics
Chemical Substances	Basic Helix-Loop-Helix Leucine Zipper Transcription Factors ; Proto-Oncogene Proteins c-myc ; Transcription Factors
Language	English
Publishing date	2023-02-03
Publishing country	United States
Document type	Journal Article ; Review ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	3155-0
ISSN	1520-5126 ; 0002-7863
ISSN (online)	1520-5126
ISSN	0002-7863
DOI	10.1021/jacs.2c12732
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Catalytic Antibody Blunts Carfentanil-Induced Respiratory Depression.

Lin, Mingliang / Eubanks, Lisa M / Karadkhelkar, Nishant M / Blake, Steven / Janda, Kim D

ACS pharmacology & translational science

2023 Volume 6, Issue 5, Page(s) 802–811

Abstract: Carfentanil, the most potent of the fentanyl analogues, is at the forefront of synthetic opioid-related deaths, second to fentanyl. Moreover, the administration of the opioid receptor antagonist naloxone has proven inadequate for an increasing number of ... ...

Abstract	Carfentanil, the most potent of the fentanyl analogues, is at the forefront of synthetic opioid-related deaths, second to fentanyl. Moreover, the administration of the opioid receptor antagonist naloxone has proven inadequate for an increasing number of opioid-related conditions, often requiring higher/additional doses to be effective, as such interest in alternative strategies to combat more potent synthetic opioids has intensified. Increasing drug metabolism would be one strategy to detoxify carfentanil; however, carfentanil's major metabolic pathways involve
Language	English
Publishing date	2023-04-17
Publishing country	United States
Document type	Journal Article
ISSN	2575-9108
ISSN (online)	2575-9108
DOI	10.1021/acsptsci.3c00031
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Article: Development of a vaccine against the synthetic opioid U-47700.

Park, Hyeri / Lin, Mingliang / Zhou, Jian / Eubanks, Lisa M / Zhou, Bin / Janda, Kim D

Frontiers in pharmacology

2023 Volume 14, Page(s) 1219985

Abstract: Opioid use disorders and overdose have become a major public health concern in recent years. U-47700, a New psychoactive substances (NPS) opioid, also known as "pinky" or "pink" has been identified as a new threat in the drug supply because of its ... ...

Abstract	Opioid use disorders and overdose have become a major public health concern in recent years. U-47700, a New psychoactive substances (NPS) opioid, also known as "pinky" or "pink" has been identified as a new threat in the drug supply because of its potency and abuse potential. Conjugate vaccines that can produce antibodies against target drug molecules have emerged as a promising tool to treat substance use disorders. Herein, we report the design, synthesis, and
Language	English
Publishing date	2023-07-10
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2587355-6
ISSN	1663-9812
ISSN	1663-9812
DOI	10.3389/fphar.2023.1219985
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Article: Development of an Effective Monoclonal Antibody against Heroin and Its Metabolites Reveals Therapies Have Mistargeted 6-Monoacetylmorphine and Morphine over Heroin.

Lee, Jinny Claire / Eubanks, Lisa M / Zhou, Bin / Janda, Kim D

ACS central science

2022 Volume 8, Issue 10, Page(s) 1464–1470

Abstract: The opioid epidemic is a global public health crisis that has failed to abate with current pharmaceutical treatments. Moreover, these FDA-approved drugs possess numerous problems such as adverse side effects, short half-lives, abuse potential, and ... ...

Abstract	The opioid epidemic is a global public health crisis that has failed to abate with current pharmaceutical treatments. Moreover, these FDA-approved drugs possess numerous problems such as adverse side effects, short half-lives, abuse potential, and recidivism after discontinued use. An alternative treatment model for opioid use disorders is immunopharmacotherapy, where antibodies are produced to inhibit illicit substances by sequestering the drug in the periphery. Immunopharmacotherapeutics against heroin have engaged both active and passive vaccines targeting heroin's metabolites, 6-monoacetylmorphine (6-AM) and morphine, since decades of research have stated that heroin's psychoactive and lethal effects are mainly attributed to these compounds. However, concerted efforts to develop effective immunopharmacotherapies against heroin abuse have faced little clinical advancement, suggesting a need for reassessing drug target selection. To address this issue, four unique monoclonal antibodies were procured with distinct affinity to either heroin, 6-AM, or morphine. Examination of these antibodies through
Language	English
Publishing date	2022-10-06
Publishing country	United States
Document type	Journal Article
ISSN	2374-7943
ISSN	2374-7943
DOI	10.1021/acscentsci.2c00977
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Article ; Online: Pharmacokinetic Approach to Combat the Synthetic Cannabinoid PB-22.

Lin, Mingliang / Ellis, Beverly / Eubanks, Lisa M / Janda, Kim D

ACS chemical neuroscience

2021 Volume 12, Issue 14, Page(s) 2573–2579

Abstract: Synthetic cannabinoids are part of a group of drugs called new psychoactive substances. Most of these cannabinoids are unregulated, and there are no therapeutic treatments for their addictive properties or reversing a potential overdose. Vaccination and ... ...

Abstract	Synthetic cannabinoids are part of a group of drugs called new psychoactive substances. Most of these cannabinoids are unregulated, and there are no therapeutic treatments for their addictive properties or reversing a potential overdose. Vaccination and catalytic antibodies strategies were investigated to assess their ability to blunt the psychoactive properties of the cannabinoid PB-22. To complement these antibody concentric investigations, we also disclose the discovery of the enzymatic degradation of this cannabinoid. Serum factors including albumin and carboxylesterase were found to catalyze the hydrolysis of PB-22. Affinity, kinetics, animal behavior, and biodistribution studies were utilized to evaluate the efficiency of these pharmacokinetic approaches. Our findings suggest simple antibody binding as the most efficacious means for altering PB-22's effect on the brain. Catalytic approaches only translated to esterases being capable of PB-22's degradation with a catalytic antibody approach providing no proclivity for PB-22's hydrolysis. Pharmacokinetic approaches provide a powerful strategy for treating substance abuse disorders and overdose for drugs where no therapeutic is available.
MeSH term(s)	Animals ; Cannabinoids ; Drug Overdose ; Tissue Distribution
Chemical Substances	Cannabinoids
Language	English
Publishing date	2021-07-13
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.1c00360
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Article ; Online: Polyphosphazene: A New Adjuvant Platform for Cocaine Vaccine Development.

Lin, Mingliang / Marin, Alexander / Ellis, Beverly / Eubanks, Lisa M / Andrianov, Alexander K / Janda, Kim D

Molecular pharmaceutics

2022 Volume 19, Issue 9, Page(s) 3358–3366

Abstract: Cocaine is a highly addictive drug that has seen a steady uptrend causing severe health problems worldwide. Currently, there are no approved therapeutics for treating cocaine use disorder; hence, there is an urgent need to identify new medications. ... ...

Abstract	Cocaine is a highly addictive drug that has seen a steady uptrend causing severe health problems worldwide. Currently, there are no approved therapeutics for treating cocaine use disorder; hence, there is an urgent need to identify new medications. Immunopharmacotherapeutics is a promising approach utilizing endogenous antibodies generated through active vaccination, and if properly programmed, can blunt a drug's psychoactive and addictive effects. However, drug vaccine efficacy has largely been limited by the modest levels of antibodies induced. Herein, we explored an adjuvant system consisting of a polyphosphazene macromolecule, specifically poly[di(carboxylatoethylphenoxy)-phosphazene] (PCEP), a biocompatible synthetic polymer that was solicited for improved cocaine conjugate vaccine delivery performance. Our results demonstrated PCEP's superior assembling efficiency with a cocaine hapten as well as with the combined adjuvant CpG oligodeoxynucleotide (ODN). Importantly, this combination led to a higher titer response, balanced immunity, successful sequestering of cocaine in the blood, and a reduction in the drug in the brain. Moreover, a PCEP-cocaine conjugate vaccine was also found to function well via intranasal administration, where its efficacy was demonstrated through the antibody titer, affinity, mucosal IgA production, and a reduction in cocaine's locomotor activity. Overall, a comprehensive evaluation of PCEP integrated within a cocaine vaccine established an advance in the use of synthetic adjuvants in the drugs of abuse vaccine field.
MeSH term(s)	Adjuvants, Immunologic ; Adjuvants, Pharmaceutic/pharmacology ; Cocaine ; Organophosphorus Compounds ; Polymers ; Vaccine Development ; Vaccines, Conjugate
Chemical Substances	Adjuvants, Immunologic ; Adjuvants, Pharmaceutic ; Organophosphorus Compounds ; Polymers ; Vaccines, Conjugate ; poly(phosphazene) ; Cocaine (I5Y540LHVR)
Language	English
Publishing date	2022-08-19
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2138405-8
ISSN	1543-8392 ; 1543-8384
ISSN (online)	1543-8392
ISSN	1543-8384
DOI	10.1021/acs.molpharmaceut.2c00489
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Article ; Online: A Vaccine against Benzimidazole-Derived New Psychoactive Substances That Are More Potent Than Fentanyl.

Lee, Jinny Claire / Park, Hyeri / Eubanks, Lisa M / Ellis, Beverly / Zhou, Bin / Janda, Kim D

Journal of medicinal chemistry

2022 Volume 65, Issue 3, Page(s) 2522–2531

Abstract: New psychoactive substance (NPS) opioids have proliferated within the international drug market. While synthetic opioids are traditionally composed of fentanyl analogues, benzimidazole-derived isotonitazene and its derivatives are the current NPS opioids ...

Abstract	New psychoactive substance (NPS) opioids have proliferated within the international drug market. While synthetic opioids are traditionally composed of fentanyl analogues, benzimidazole-derived isotonitazene and its derivatives are the current NPS opioids of concern. Hence, in this study, we implement immunopharmacotherapy wherein antibodies are produced with high titers and nanomolar affinity to multiple benzimidazole-derived NPS opioids (BNO). Notably, these antibodies blunt psychoactive and physiological repercussions from BNO exposure, which was observed through antinociception, whole-body plethysmography, and blood-brain biodistribution studies. Moreover, we detail previously unreported pharmacokinetics of these drugs, which explains the struggle of traditional pharmaceutical opioid antagonists against BNO substances. These findings provide further insight into the
MeSH term(s)	Analgesics, Opioid/chemical synthesis ; Analgesics, Opioid/immunology ; Analgesics, Opioid/pharmacokinetics ; Animals ; Benzimidazoles/chemical synthesis ; Benzimidazoles/immunology ; Benzimidazoles/pharmacokinetics ; Female ; Haptens/chemistry ; Haptens/immunology ; Hemocyanins/chemistry ; Hemocyanins/immunology ; Illicit Drugs/chemical synthesis ; Illicit Drugs/immunology ; Illicit Drugs/pharmacokinetics ; Mice, Inbred BALB C ; Nociception/drug effects ; Respiratory Insufficiency/chemically induced ; Respiratory Insufficiency/prevention & control ; Vaccines, Conjugate/chemistry ; Vaccines, Conjugate/immunology ; Mice
Chemical Substances	Analgesics, Opioid ; Benzimidazoles ; Haptens ; Illicit Drugs ; Vaccines, Conjugate ; isotonitazene ; Hemocyanins (9013-72-3) ; etonitazene (9U3GT3353T) ; keyhole-limpet hemocyanin (FV4Y0JO2CX)
Language	English
Publishing date	2022-01-07
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/acs.jmedchem.1c01967
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Article: An Engineered Human-Antibody Fragment with Fentanyl Pan-Specificity that Reverses Carfentanil-Induced Respiratory Depression.

Eubanks, Lisa M / Pholcharee, Tossapol / Oyen, David / Natori, Yoshihiro / Zhou, Bin / Wilson, Ian A / Janda, Kim D

bioRxiv : the preprint server for biology

2023

Abstract: The opioid overdose crisis primarily driven by potent synthetic opioids resulted in more than 500,000 deaths in the US over the last 20 years. Though naloxone, a short acting medication, remains the primary treatment option for temporarily reversing ... ...

Abstract	The opioid overdose crisis primarily driven by potent synthetic opioids resulted in more than 500,000 deaths in the US over the last 20 years. Though naloxone, a short acting medication, remains the primary treatment option for temporarily reversing opioid overdose effects, alternative countermeasures are needed. Monoclonal antibodies present a versatile therapeutic opportunity that can be tailored for synthetic opioids and that can help prevent post-treatment renarcotization. The ultrapotent analog carfentanil, is especially concerning due to its unique pharmacological properties. With this in mind, we generated a fully human antibody through a drug-specific B cell sorting strategy with a combination of carfentanil and fentanyl probes. The resulting pan-specific antibody was further optimized through scFv phage display. This antibody, C10-S66K, displays high affinity to carfentanil, fentanyl, and other analogs, and reversed carfentanil-induced respiratory depression. Additionally, x-ray crystal structures with carfentanil and fentanyl bound provided structural insight into key drug:antibody interactions.
Language	English
Publishing date	2023-07-04
Publishing country	United States
Document type	Preprint
DOI	10.1101/2023.07.04.547721
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Article ; Online: An Engineered Human-Antibody Fragment with Fentanyl Pan-Specificity That Reverses Carfentanil-Induced Respiratory Depression.

Eubanks, Lisa M / Pholcharee, Tossapol / Oyen, David / Natori, Yoshihiro / Zhou, Bin / Wilson, Ian A / Janda, Kim D

ACS chemical neuroscience

2023 Volume 14, Issue 16, Page(s) 2849–2856

Abstract: The opioid overdose crisis primarily driven by potent synthetic opioids resulted in more than 500,000 deaths in the US over the last 20 years. Though naloxone, a short-acting medication, remains the primary treatment option for temporarily reversing ... ...

Abstract	The opioid overdose crisis primarily driven by potent synthetic opioids resulted in more than 500,000 deaths in the US over the last 20 years. Though naloxone, a short-acting medication, remains the primary treatment option for temporarily reversing opioid overdose effects, alternative countermeasures are needed. Monoclonal antibodies present a versatile therapeutic opportunity that can be tailored to synthetic opioids and help prevent post-treatment renarcotization. The ultrapotent analog carfentanil is especially concerning due to its unique pharmacological properties. With this in mind, we generated a fully human antibody through a drug-specific B cell sorting strategy with a combination of carfentanil and fentanyl probes. The resulting pan-specific antibody was further optimized through scFv phage display, producing C10-S66K. This monoclonal antibody displays high affinity to carfentanil, fentanyl, and other analogs and reversed carfentanil-induced respiratory depression. Additionally, X-ray crystal structures with carfentanil and fentanyl bound provided structural insight into key drug:antibody interactions.
MeSH term(s)	Humans ; Analgesics, Opioid/therapeutic use ; Immunoglobulin Fragments ; Opiate Overdose/drug therapy ; Fentanyl ; Drug Overdose ; Respiratory Insufficiency/chemically induced ; Respiratory Insufficiency/drug therapy
Chemical Substances	carfentanil (LA9DTA2L8F) ; Analgesics, Opioid ; Immunoglobulin Fragments ; Fentanyl (UF599785JZ)
Language	English
Publishing date	2023-08-03
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
ISSN	1948-7193
ISSN (online)	1948-7193
DOI	10.1021/acschemneuro.3c00455
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