Peter S Dragovich
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Explore the profile of Peter S Dragovich including associated specialties, affiliations and a list of published articles.
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77
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1133
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Recent Articles
1.
Zhang D, Ma B, Dragovich P, Ma L, Chen S, Chen E, et al.
Commun Med (Lond)
. 2024 May;
4(1):87.
PMID: 38755248
Background: Proteolysis-targeting chimeras (PROTACs) are being developed for therapeutic use. However, they have poor pharmacokinetic profiles and their tissue distribution kinetics are not known. Methods: A typical von Hippel-Lindau tumor...
2.
Lewis G, Li G, Guo J, Yu S, Fields C, Lee G, et al.
Nat Commun
. 2024 Jan;
15(1):466.
PMID: 38212321
Approved antibody-drug conjugates (ADCs) for HER2-positive breast cancer include trastuzumab emtansine and trastuzumab deruxtecan. To develop a differentiated HER2 ADC, we chose an antibody that does not compete with trastuzumab...
3.
Berlin M, Cantley J, Bookbinder M, Bortolon E, Broccatelli F, Cadelina G, et al.
J Med Chem
. 2024 Jan;
67(2):1262-1313.
PMID: 38180485
The identification of VHL-binding proteolysis targeting chimeras (PROTACs) that potently degrade the BRM protein (also known as SMARCA2) in SW1573 cell-based experiments is described. These molecules exhibit between 10- and...
4.
Kschonsak M, Jao C, Arthur C, Rohou A, Bergeron P, Ortwine D, et al.
Elife
. 2023 Mar;
12.
PMID: 36975198
The voltage-gated sodium (Na) channel Na1.7 has been identified as a potential novel analgesic target due to its involvement in human pain syndromes. However, clinically available Na channel-blocking drugs are...
5.
Cantley J, Ye X, Rousseau E, Januario T, Hamman B, Rose C, et al.
Nat Commun
. 2022 Nov;
13(1):6814.
PMID: 36357397
The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4 is frequently mutated in cancer and inactivation results in a cellular dependence on its paralog, SMARCA2, thus making SMARCA2 an attractive synthetic lethal...
6.
Dragovich P
Chem Soc Rev
. 2022 May;
51(10):3886-3897.
PMID: 35506708
Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis targeting chimera (PROTAC) payload with a monoclonal antibody some type of chemical linker. This review provides a current summary of...
7.
Dragovich P
J Med Chem
. 2022 Mar;
65(6):4496-4499.
PMID: 35285623
The application of antibody-drug conjugates (ADCs) to fields outside of oncology is increasing but is still relatively uncommon. A recent publication describes the conjugation of glucocorticoid receptor modulators to antibodies...
8.
Dragovich P, Haap W, Mulvihill M, Plancher J, Stepan A
J Med Chem
. 2022 Feb;
65(4):3606-3615.
PMID: 35138850
The origin of small-molecule leads that were pursued across the independent research organizations Roche and Genentech from 2009 to 2020 is described. The identified chemical series are derived from a...
9.
Wei B, Robarge K, Labadie S, Chen J, Corson L, DiPasquale A, et al.
Bioorg Med Chem Lett
. 2022 Jan;
59:128576.
PMID: 35065235
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement...
10.
Vollmar B, Frantz C, Schutten M, Zhong F, Rosario G, Go M, et al.
Mol Cancer Ther
. 2021 Mar;
20(6):1112-1120.
PMID: 33722856
Calicheamicin antibody-drug conjugates (ADCs) are effective therapeutics for leukemias with two recently approved in the United States: Mylotarg (gemtuzumab ozogamicin) targeting CD33 for acute myeloid leukemia and Besponsa (inotuzumab ozogamicin)...