Increased Soft Tissue in the Posterior Cervical and Upper Back Area of Patients on HIV-1 Protease Inhibitors

1999 ◽  
Vol 3 (4) ◽  
pp. 211-217 ◽  
Author(s):  
Kathleen Smith ◽  
Marguerite Germain ◽  
Catherine Decker ◽  
Josef Yeager ◽  
Henry Skelton
Keyword(s):  
Soft Tissue ◽  
Protease Inhibitors ◽  
Steroid Receptors ◽  
Steroid Hormone ◽  
Matrix Material ◽  
Subcutaneous Fat ◽  
The Body ◽  
Factor Xiiia ◽  
Hormone Metabolism ◽  
Hiv 1

Background: Corticosteroids as well as sex hormones affect the redistribution of subcutaneous fat and the percentage of lean body mass. In addition, some stromal cells express steroid receptors, and the quantity and distribution of these receptors vary at different body sites and between sexes. Inhibitors of HIV-1 protease may affect steroid hormone metabolism through their effect on cytochrome P450. Objectives: To determine the changes in the tissue of the back in three HIV-1+ patients who developed increased soft tissue in posterior cervical and upper back areas while on HIV-1 protease inhibitors. Methods: Punch biopsies of the involved posterior cervical and upper back areas were done. These included subcutaneous adipose tissue. Routine hematoxylin and eosin-stained sections, along with special stains for elastic and stromal mucin, and immunohistochemical stains for CD34 (HPCA-1 and Factor XIIIa) were evaluated. Results: Histologically all three patients showed identical features. There was expansion of the dermis with decreased periadnexal fat and marked widening of the fibrous septa within the expanded subcutaneous fat. Conclusions: The posterior cervical and upper back area appears to be a common site for localization of mesenchymal tumours that show some fat differentiation and produce an increase in stromal matrix material. Mesenchymal cell populations within this area are also affected by systemic diseases. A male predominance pattern occurs with these conditions, and steroid receptors are expressed on some mesenchymal cells, that vary with the body location. Thus, this observation may be related to the effects of protease inhibitors on steroid hormone metabolism through their inhibition of cytochrome P-450.

THE INFLUENCE OF CHORIONIC GONADOTROPHIN ON THE STEROID METABOLISM OF SEXUALLY RETARDED MEN

1957 ◽  
Vol 16 (2) ◽  
pp. 156-163 ◽  
Author(s):  
I. D. K. HALKERSTON ◽  
JANET HILLMAN ◽  
D. PALMER ◽  
M. REISS ◽  
A. RUNDLE
Keyword(s):  
Excretion Rate ◽  
Steroid Hormone ◽  
Body Fluids ◽  
Chorionic Gonadotrophin ◽  
The Body ◽  
Steroid Metabolism ◽  
Secondary Effects ◽  
Hormone Metabolism ◽  
Excretion Pattern ◽  
Main Effect

SUMMARY The action of chorionic gonadotrophin (CG) on the steroid hormone metabolism of sexually retarded men was investigated. The increase observed in the excretion rate of 17-ketosteroids (17-KS) was due to a rise in the excretion of the 17α-KS androsterone and aetiocholanolone, and represents the main effect of CG on the excretion pattern of urinary 17-KS. Other changes in the steroid hormone metabolism after treatment with CG, such as the increase in excretion of oestrogens and corticoids, occur much less regularly, and are regarded as secondary effects of the increased concentration of testosterone in the body fluids. Attention is drawn to the way in which certain types of sexual retardation and immaturity develop.

STEROID HORMONE METABOLISM IN RESPONSIVE TISSUES IN VITRO

1971 ◽  
Vol 68 (1_Suppl) ◽  
pp. S279-S294 ◽  
Author(s):  
Paul Robel
Keyword(s):  
Steroid Hormone ◽  
Physiological Activity ◽  
Physiological State ◽  
Target Cells ◽  
Target Tissue ◽  
Hormone Metabolism ◽  
Metabolizing Enzymes ◽  
Relationship Of

ABSTRACT Of the information available on steroid hormone metabolism in responsive tissues, only that relating hormone metabolism to physiological activity is reviewed, i. e. metabolite activity in isolated in vitro systems, binding of metabolites to target tissue receptors, specific steroid hormone metabolizing enzymes and relationship of hormone metabolism to target organ physiological state. Further, evidence is presented in the androgen field, demonstrating 5α-reduced metabolites, formed inside the target cells, as active compounds. This has led to a consideration of testosterone as a »prehormone«. The possibility that similar events take place in tissues responding to progesterone is discussed. Finally, the role of hormone metabolism in the regulation of hormone availability and/or renewal in target cells is discussed. In this context, reference is made to the potential role of plasma binding proteins and cytosol receptors.

An oral high dose of cholecalciferol restores vitamin D status in deficient postmenopausal HIV-1 infected women independently of protease inhibitors therapy

2015 ◽  
Author(s):  
Jessica Pepe ◽  
Ivano Mezzaroma ◽  
Alessandra Fantauzzi ◽  
Mario Falciano ◽  
Alessandra Salotti ◽  
...  
Keyword(s):  
Vitamin D ◽  
Protease Inhibitors ◽  
High Dose ◽  
Vitamin D Status ◽  
Hiv 1

A convergent synthesis of the spiroketal moiety of the HIV-1 protease inhibitors didemnaketals

Tetrahedron ◽  
2002 ◽  
Vol 58 (9) ◽  
pp. 1697-1708 ◽  
Author(s):  
Yan Xing Jia ◽  
Xin Li ◽  
Bin Wu ◽  
Xue Zhi Zhao ◽  
Yong Qiang Tu
Keyword(s):  
Protease Inhibitors ◽  
Convergent Synthesis ◽  
Hiv 1

scholarly journals Substrate Envelope-Designed Potent HIV-1 Protease Inhibitors to Avoid Drug Resistance

2013 ◽  
Vol 20 (9) ◽  
pp. 1116-1124 ◽  
Author(s):  
Madhavi N.L. Nalam ◽  
Akbar Ali ◽  
G.S. Kiran Kumar Reddy ◽  
Hong Cao ◽  
Saima G. Anjum ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Protease Inhibitors ◽  
Hiv 1 ◽  
Substrate Envelope

Design and Evaluation of Novel Piperidine HIV-1 Protease Inhibitors with Potency against DRV-resistant Variants

2021 ◽  
pp. 113450
Author(s):  
Mei Zhu ◽  
Huiyu Zhou ◽  
Ling Ma ◽  
Biao Dong ◽  
Jinming Zhou ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1

ChemInform Abstract: HIV-1 Protease Inhibitors Based on Acyclic Carbohydrates.

ChemInform ◽  
2010 ◽  
Vol 29 (49) ◽  
pp. no-no
Author(s):  
B. SAMUELSSON ◽  
ET AL. ET AL.
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1

scholarly journals Major drug resistance mutations to HIV-1 protease inhibitors (PI) among patients exposed to PI class failing antiretroviral therapy in São Paulo State, Brazil

PLoS ONE ◽  
2019 ◽  
Vol 14 (10) ◽  
pp. e0223210
Author(s):  
Giselle de Faria Romero Soldi ◽  
Isadora Coutinho Ribeiro ◽  
Cintia Mayumi Ahagon ◽  
Luana Portes Ozório Coelho ◽  
Gabriela Bastos Cabral ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antiretroviral Therapy ◽  
Protease Inhibitors ◽  
Sao Paulo ◽  
Resistance Mutations ◽  
Paulo State ◽  
Drug Resistance Mutations ◽  
São Paulo State ◽  
Major Drug ◽  
Hiv 1

scholarly journals Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants

2020 ◽  
Vol 11 (6) ◽  
pp. 1196-1204
Author(s):  
Mei Zhu ◽  
Yue Dou ◽  
Ling Ma ◽  
Biao Dong ◽  
Fan Zhang ◽  
...  
Keyword(s):  
Protease Inhibitors ◽  
Hiv 1 ◽  
Enhance Activity

scholarly journals Multiple Mutations in the Human Immunodeficiency Virus Protease Gene Are Responsible for Decreased Susceptibility to Protease Inhibitors

1995 ◽  
Vol 6 (2) ◽  
pp. 80-88 ◽  
Author(s):  
R. W. King ◽  
S. Garber ◽  
D. L. Winslow ◽  
C. Reid ◽  
L. T. Bacheler ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Clinical Isolate ◽  
Protease Gene ◽  
Human Immunodeficiency Virus Protease ◽  
Fold Reduction ◽  
Antiretroviral Drug ◽  
Immunodeficiency Virus ◽  
Hiv 1

The protease (PR) of the human immunodeficiency virus (HIV) is essential for replication of the virus, and accordingly has become an attractive target for the development of an antiretroviral drug. We have previously reported that passage of HIV-1 in the presence of increasing concentrations of the C-2 symmetrical, linear diol P9941 resulted in the isolation of virus with a valine-to-alanine change at position 82 (V82A) of the PR, and reduced sensitivity to certain PR inhibitors. In this study, we passaged four different variants of HIV-1 in increasing concentrations of XM323, and isolated variants with reduced sensitivity to inhibitors of PR. Twenty-three passages of HIV-1 (RF) in the presence of XM323 resulted in a variant that exhibited an approximately 100-fold reduction in susceptibility to XM323 and that contained V82F and I84V changes. When two other viruses, HIV-1 (RF41D2) and HIV-1(RF41E4), previously derived from HIV-1 (RF) by passage in the presence of P9941, were passaged in the presence of XM323, variants with V82A/L97V and M46L/V82A/L97V changes, respectively, were obtained. The M46L/V82A/L97V variant showed a 6-fold reduction in sensitivity to XM323, whereas the susceptibility of the V82A/L97V mutant remained unchanged. Seventeen passages of a clinical isolate of HIV-1, HIV-1 (Pat.E), in the presence of XM323 produced a V82F/L97V mutant with an approximately 9-fold reduction in sensitivity to XM323.

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